PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 7576830-10 1995 The pyridostigmine inhibited AChE recovered only in the 100 mumol kg-1 kg oxime groups at the end of the experiment. Oximes 74-79 acetylcholinesterase Cavia porcellus 29-33 7476018-0 1995 Successive organophosphate inhibition and oxime reactivation reveals distinct responses of recombinant human cholinesterase variants. Oximes 42-47 butyrylcholinesterase Homo sapiens 109-123 7799993-8 1995 In humans, the efficacy of oximes in AChE reactivation can be determined rapidly using electrophysiologic studies. Oximes 27-33 acetylcholinesterase (Cartwright blood group) Homo sapiens 37-41 7840615-1 1995 The oxolanosterol oxime 3 beta-hydroxylanost-7-en-15-one 15-oxime and the structurally similar 3 beta-hydroxylanost-7-en-15-one are dual-action inhibitors of cholesterol synthesis which cause both inhibition of lanosterol 14 alpha-methyl demethylase and suppression of the rate-limiting enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR). Oximes 18-23 3-hydroxy-3-methylglutaryl-CoA reductase Homo sapiens 294-341 7840615-1 1995 The oxolanosterol oxime 3 beta-hydroxylanost-7-en-15-one 15-oxime and the structurally similar 3 beta-hydroxylanost-7-en-15-one are dual-action inhibitors of cholesterol synthesis which cause both inhibition of lanosterol 14 alpha-methyl demethylase and suppression of the rate-limiting enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR). Oximes 18-23 high mobility group AT-hook 1 Homo sapiens 343-347 7654137-14 1995 The oxime efficacy in reactivating diaphragm AChE decreased in the order sarin > VX without significant differences between pretreated and non-pretreated groups. Oximes 4-9 acetylcholinesterase Cavia porcellus 45-49 8750900-4 1995 With HI 6 alone, the portion of AChE activity which could be reactivated 25 min after the start of ageing decreased rapidly with the delay of the oxime addition (100% of the original activity at immediate addition), the half-life being approximately 2.5 min. Oximes 146-151 acetylcholinesterase (Cartwright blood group) Homo sapiens 32-36 7670367-0 1995 Oxime effects on the rate constants of carbamylation and decarbamylation of acetylcholinesterase for pyridostigmine, physostigmine and insecticidal carbamates. Oximes 0-5 acetylcholinesterase Bos taurus 76-96 7778760-1 1995 We have developed an assay for pyridoxal kinase which takes advantage of the intense fluorescence yield of the oxime of pyridoxal or pyridoxal-5"-phosphate and the substantial difference in the rates of formation of these two oximes. Oximes 111-116 pyridoxal kinase Homo sapiens 31-47 7778760-1 1995 We have developed an assay for pyridoxal kinase which takes advantage of the intense fluorescence yield of the oxime of pyridoxal or pyridoxal-5"-phosphate and the substantial difference in the rates of formation of these two oximes. Oximes 226-232 pyridoxal kinase Homo sapiens 31-47 7758210-8 1995 Reactivation of carbamylated cholinesterase is obtained by the incubation of diluted enzyme at 37 degrees C for 2.5 h prior to assay, whereas phosphorylated (non-aged) enzyme is reactivated by a 30 min incubation with oximes. Oximes 218-224 butyrylcholinesterase Homo sapiens 29-43 8161944-0 1994 Rate constants of carbamylation and decarbamylation of acetylcholinesterase for physostigmine and carbaryl in the presence of an oxime. Oximes 129-134 acetylcholinesterase Bos taurus 55-75 8134223-13 1994 In vitro, oximes reactivated acetylcholinesterase inhibited with paraoxon, whereas no significant effect of oximes on carbamylated enzyme activity was observed. Oximes 10-16 acetylcholinesterase (Cartwright blood group) Homo sapiens 29-49 8161944-7 1994 The results extend those in a recent report by other authors who studied the half-life of carbamylation for acetylcholinesterase and butyrylcholinesterase in an attempt to understand the mechanism by which oximes increase the toxicity of carbaryl in vivo. Oximes 206-212 acetylcholinesterase Bos taurus 108-128 8304979-3 1994 To improve the efficacy of cholinesterases as pretreatment drugs, we have developed an approach in which the catalytic activity of OP-inhibited FBS AChE was rapidly and continuously restored, thus detoxifying the OP and minimizing enzyme aging by having sufficient amounts of appropriate oxime present. Oximes 288-293 acetylcholinesterase Mus musculus 148-152 8291056-13 1994 Both paraoxon- and DFP-exposed cultures recovered ACHE activity immediately following OP exposure if treated postexposure with an oxime reactivator, 2-pralidoxime. Oximes 130-135 acetylcholinesterase (Cartwright blood group) Gallus gallus 50-54 7857205-0 1994 In vitro oxime-induced reactivation of various molecular forms of soman-inhibited acetylcholinesterase in striated muscle from rat, monkey and human. Oximes 9-14 acetylcholinesterase (Cartwright blood group) Homo sapiens 82-102 7857205-3 1994 In the Pre-Post mode the oxime effects would result from a combination of not only shielding of acetylcholinesterase from soman inhibition but also from immediate reactivation of soman-inhibited acetylcholinesterase. Oximes 25-30 acetylcholinesterase (Cartwright blood group) Homo sapiens 96-116 7857205-3 1994 In the Pre-Post mode the oxime effects would result from a combination of not only shielding of acetylcholinesterase from soman inhibition but also from immediate reactivation of soman-inhibited acetylcholinesterase. Oximes 25-30 acetylcholinesterase (Cartwright blood group) Homo sapiens 195-215 7857205-9 1994 Effectiveness of oxime-induced reactivation of soman-inhibited acetylcholinesterase could be estimated from the total acetylcholinesterase activity which appears to reflect the results found with the individual molecular forms of acetylcholinesterase. Oximes 17-22 acetylcholinesterase (Cartwright blood group) Homo sapiens 63-83 7857205-9 1994 Effectiveness of oxime-induced reactivation of soman-inhibited acetylcholinesterase could be estimated from the total acetylcholinesterase activity which appears to reflect the results found with the individual molecular forms of acetylcholinesterase. Oximes 17-22 acetylcholinesterase (Cartwright blood group) Homo sapiens 118-138 7857205-9 1994 Effectiveness of oxime-induced reactivation of soman-inhibited acetylcholinesterase could be estimated from the total acetylcholinesterase activity which appears to reflect the results found with the individual molecular forms of acetylcholinesterase. Oximes 17-22 acetylcholinesterase (Cartwright blood group) Homo sapiens 118-138 8308950-6 1994 We propose that stability of the plasma cholinesterase at 6 to 8 h after temporarily suspending oxime provides a rapid guide to the duration of therapy, especially in patients whose complications make clinical assessment difficult. Oximes 96-101 butyrylcholinesterase Homo sapiens 40-54 8344000-1 1993 O-Ethyl-O-4-nitrophenylphosphoramidate is a short-acting anticholinesterase and a possible candidate for a prophylactic agent against nerve agents since human acetylcholinesterase inhibited by this agent undergoes rapid spontaneous reactivation which can be accelerated further, if necessary, by treatment with oximes. Oximes 311-317 acetylcholinesterase (Cartwright blood group) Homo sapiens 159-179 8292752-5 1993 The rat brain acetylcholinesterase spontaneous (k0 = approximately 13.0 x 10(-3) min-1) and oxime-mediated (koxime) = 51.0 x 10(-3) min-1) reactivation rate constants following inhibition by isomalathion stereoisomers with the R configuration at phosphorus were comparable to spontaneous (11.3 x 10(-3) min-1) and oxime-mediated (50.2 x 10(-3) min-1) reactivation rates obtained for (S)-isoparathion methyl. Oximes 92-97 acetylcholinesterase Rattus norvegicus 14-34 8292752-5 1993 The rat brain acetylcholinesterase spontaneous (k0 = approximately 13.0 x 10(-3) min-1) and oxime-mediated (koxime) = 51.0 x 10(-3) min-1) reactivation rate constants following inhibition by isomalathion stereoisomers with the R configuration at phosphorus were comparable to spontaneous (11.3 x 10(-3) min-1) and oxime-mediated (50.2 x 10(-3) min-1) reactivation rates obtained for (S)-isoparathion methyl. Oximes 109-114 acetylcholinesterase Rattus norvegicus 14-34 1361555-5 1992 The reactivation of cholinesterase in cerebral cortex by the oximes, in spite of their being quaternary salts is a notable feature. Oximes 61-67 butyrylcholinesterase Homo sapiens 20-34 8311691-1 1993 The ability of three oximes, HI-6, MMB-4 and ICD-467, to reactivate cholinesterase (ChE) inhibited by the organophosphorus compound soman was compared in blood (plasma and erythrocytes), brain regions (including spinal cord) and peripheral tissues of rats. Oximes 21-27 butyrylcholinesterase Rattus norvegicus 84-87 8494501-11 1993 Combination of pyridostigmine pretreatment and oxime treatment enhanced the recovery of the tracheal contraction response and the ChE activity in the trachea compared to treatment with oximes alone. Oximes 47-52 butyrylcholinesterase Rattus norvegicus 130-133 8448346-3 1993 Following inhibition of rat brain AChE by (SPRC)- or (SPSC)-isomalathion, k0 and k(oxime) values were obtained that were comparable to (SP)-isoparathion methyl, indicating that the same mechanism of inhibition was shared, namely, formation of an O,S-dimethyl phosphorothiolated enzyme. Oximes 83-88 acetylcholinesterase Rattus norvegicus 34-38 1664202-1 1991 Isolated rat diaphragm preparations treated with soman or with the irreversible and oxime resistant cholinesterase (ChE) inhibitor S27 showed a considerable recovery of neuromuscular transmission (NMT) during incubation with the (bis)pyridinium oximes HI-6, HGG-12, P2S and obidoxime. Oximes 84-89 butyrylcholinesterase Rattus norvegicus 100-114 8441737-7 1993 The addition of HI-6, an AChE-reactivating oxime, to atropine + diazepam therapy further increased the survival in soman-poisoned and physostigmine-pretreated rats, yielding the highest protective ratio of 6.4. Oximes 43-48 acetylcholinesterase Rattus norvegicus 25-29 1631893-1 1992 The therapeutic efficacy of the oxime HI-6 against intoxication with the irreversible cholinesterase (ChE) inhibitor soman was tested in marmoset monkeys. Oximes 32-37 cholinesterase Callithrix jacchus 86-100 1631893-1 1992 The therapeutic efficacy of the oxime HI-6 against intoxication with the irreversible cholinesterase (ChE) inhibitor soman was tested in marmoset monkeys. Oximes 32-37 cholinesterase Callithrix jacchus 102-105 1733041-0 1992 Central activity of acetylcholinesterase oxime reactivators. Oximes 41-46 acetylcholinesterase (Cartwright blood group) Homo sapiens 20-40 1733041-1 1992 The ability of various oximes to antagonize the sarin-induced hypothermia and reactivate phosphorylated acetylcholinesterase was used as an indicator of the central activity of oximes. Oximes 23-29 acetylcholinesterase (Cartwright blood group) Homo sapiens 104-124 1778361-1 1991 Phrenic nerve diaphragm muscles of young adult rats were used to study the ability of the oximes 2-PAM and HI-6 to recover muscle function depressed by organophosphate (OP) agents. Oximes 90-96 peptidylglycine alpha-amidating monooxygenase Rattus norvegicus 99-102 1890690-6 1991 The oxime HI-6 reactivated soman phosphonylated enzymes to a considerably greater extent than other oximes, and FBS AChE was notably more responsive to HI-6 than to other oximes. Oximes 171-177 acetylcholinesterase (Cartwright blood group) Homo sapiens 116-120 1890690-8 1991 In general, oxime potency and some rank order varied with each inhibitor and with each AChE, although there was some similarity in oxime rank order between the two mammalian AChEs. Oximes 12-17 acetylcholinesterase (Cartwright blood group) Homo sapiens 87-91 1664331-0 1991 On the mechanism whereby HI-6 improves neuromuscular function after oxime-resistant acetylcholinesterase inhibition and subsequent impairment of neuromuscular transmission. Oximes 68-73 acetylcholinesterase Rattus norvegicus 84-104 1664331-1 1991 Experiments were performed to elucidate the mechanism of action by which the oxime HI-6 causes a recovery of neuromuscular function after oxime-resistant inhibition of acetylcholinesterase by the organophosphate S27. Oximes 77-82 acetylcholinesterase Rattus norvegicus 168-188 1412499-4 1992 We have found that the inhibition of both eel acetylcholinesterase (eel AChE, EC 3.1.1.7) and human serum cholinesterase (human BuChE, EC 3.1.1.8) by carbaryl was enhanced by several oximes. Oximes 183-189 acetylcholinesterase (Cartwright blood group) Homo sapiens 72-76 1412499-4 1992 We have found that the inhibition of both eel acetylcholinesterase (eel AChE, EC 3.1.1.7) and human serum cholinesterase (human BuChE, EC 3.1.1.8) by carbaryl was enhanced by several oximes. Oximes 183-189 butyrylcholinesterase Homo sapiens 52-66 1599796-6 1992 The method of introducing the amino functionality at the C-4 methylene group described herein provides an alternative to that currently in use (reduction of oximes). Oximes 157-163 complement C4A (Rodgers blood group) Homo sapiens 57-60 1459041-4 1992 In assessing therapeutic efficacy and oxime-induced reactivation of blood AChE, rats were pretreated with PYR, challenged with agent and treated with atropine (16 mg/kg, im) and HI-6 or 2-PAM (100 umoles/kg, im) 30 sec post agent. Oximes 38-43 acetylcholinesterase Rattus norvegicus 74-78 2029909-3 1991 Displaying inhibition constants of 0.45 microM and 0.62 microM, for the animal and plant enzyme, respectively, the simple oxime 2 was about equally potent as the parent lactone 1, and 50-400 times more efficient than two recently described new beta-N-acetylglucosaminidase inhibitors. Oximes 122-127 O-GlcNAcase Homo sapiens 244-272 2052186-2 1991 The maximal protection produced by the oximes PAM and HI-6 varied as much as 6-fold between these species. Oximes 39-45 peptidylglycine alpha-amidating monooxygenase Mus musculus 46-49 1664202-1 1991 Isolated rat diaphragm preparations treated with soman or with the irreversible and oxime resistant cholinesterase (ChE) inhibitor S27 showed a considerable recovery of neuromuscular transmission (NMT) during incubation with the (bis)pyridinium oximes HI-6, HGG-12, P2S and obidoxime. Oximes 84-89 butyrylcholinesterase Rattus norvegicus 116-119 1664202-3 1991 Atropinized rats were artificially ventilated after injection with 3 x LD50 soman for 3 h and then treated with HI-6, i.e. at a time when oxime reactivation of soman inhibited ChE is no longer possible. Oximes 138-143 butyrylcholinesterase Rattus norvegicus 176-179 2046471-1 1991 To assess the utility of phosphinates as pretreatments against nerve agents, experiments were conducted to determine whether oximes can reactivate phosphinate-inhibited guinea pig acetylcholinesterase (AChE) and whether the toxicity of phosphinates is reduced by treatment with atropine and/or oxime. Oximes 125-131 acetylcholinesterase Cavia porcellus 202-206 2046471-1 1991 To assess the utility of phosphinates as pretreatments against nerve agents, experiments were conducted to determine whether oximes can reactivate phosphinate-inhibited guinea pig acetylcholinesterase (AChE) and whether the toxicity of phosphinates is reduced by treatment with atropine and/or oxime. Oximes 125-130 acetylcholinesterase Cavia porcellus 202-206 2046471-4 1991 Both oximes significantly reactivated MPP- or CMPP-inhibited AChE; however, HI-6 was the better reactivator in both cases. Oximes 5-11 acetylcholinesterase Cavia porcellus 61-65 1992286-1 1991 C-6 derivatives--hydrazones, phenylhydrazones, dinitrophenylhydrazones, oximes and semicarbazones--of morphinane-6-ones were synthesized and their binding characteristics were studied on rat brain membranes. Oximes 72-78 complement C6 Rattus norvegicus 0-3 1658986-3 1991 CRS-inhibited AChE appeared to age very rapidly, because in vitro addition of oximes immediately following inhibition, did not result in any AChE reactivation. Oximes 78-84 acetylcholinesterase Rattus norvegicus 14-18 2260991-0 1990 Evaluation of several oximes as reactivators of unaged soman-inhibited whole blood acetylcholinesterase in rabbits. Oximes 22-28 ACE-1 Oryctolagus cuniculus 83-103 2260991-1 1990 The antidotal benefit of oximes against organophosphorus (OP) anticholinesterase intoxication is thought to be due to reactivation of the OP-inhibited acetylcholinesterase (AChE). Oximes 25-31 ACE-1 Oryctolagus cuniculus 151-171 2260991-1 1990 The antidotal benefit of oximes against organophosphorus (OP) anticholinesterase intoxication is thought to be due to reactivation of the OP-inhibited acetylcholinesterase (AChE). Oximes 25-31 ACE-1 Oryctolagus cuniculus 173-177 2260991-2 1990 This study was conducted to determine whether the antidotal efficacy against soman by the oximes 2-hydroxyiminomethyl-3-methyl-1-[2-(3-methyl-3-nitrobutyl oxymethyl)]-imidazolium Cl (ICD 467) and 1,1"-methylenebis[4-(hydroxyiminomethyl) pyridinium] di-Cl (MMB-4) resulted, in part, from reactivation of the inhibited AChE. Oximes 90-96 ACE-1 Oryctolagus cuniculus 317-321 2260991-3 1990 These oximes were tested in parallel with pralidoxime Cl (2-PAM) and 1-(2-hydroxyiminomethyl-1-pyridinio-3-(4-carbamoyl-1-pyridinio+ ++)-2-oxapropane di-Cl (HI-6). Oximes 6-12 peptidyl-glycine alpha-amidating monooxygenase Oryctolagus cuniculus 60-63 2362084-0 1990 Oxime-induced reactivation of acetylcholinesterase inhibited by organophosphinates. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 30-50 2362084-1 1990 The comparative potency of oximes for reactivation of inhibited eel acetylcholinesterase (AChE) in vitro is dependent on the organophosphinate inhibitor. Oximes 27-33 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-88 2362084-1 1990 The comparative potency of oximes for reactivation of inhibited eel acetylcholinesterase (AChE) in vitro is dependent on the organophosphinate inhibitor. Oximes 27-33 acetylcholinesterase (Cartwright blood group) Homo sapiens 90-94 2362084-3 1990 This work was done to identify more clearly the nature of phosphinylated AChE with regard to oxime reactivation potency and the potential of phosphinates as pretreatment drugs to protect AChE against organophosphonate poisoning. Oximes 93-98 acetylcholinesterase (Cartwright blood group) Homo sapiens 73-77 2362084-6 1990 Incubation of the inhibited enzyme (I-AChE) at 25 degrees C was with 0.30 microM oxime for PMP, 3.0 microM oxime for sarin and CPMP and 100 microM oxime for the two remaining phosphinates. Oximes 81-86 acetylcholinesterase (Cartwright blood group) Homo sapiens 38-42 2362084-6 1990 Incubation of the inhibited enzyme (I-AChE) at 25 degrees C was with 0.30 microM oxime for PMP, 3.0 microM oxime for sarin and CPMP and 100 microM oxime for the two remaining phosphinates. Oximes 107-112 acetylcholinesterase (Cartwright blood group) Homo sapiens 38-42 2362084-6 1990 Incubation of the inhibited enzyme (I-AChE) at 25 degrees C was with 0.30 microM oxime for PMP, 3.0 microM oxime for sarin and CPMP and 100 microM oxime for the two remaining phosphinates. Oximes 107-112 acetylcholinesterase (Cartwright blood group) Homo sapiens 38-42 2403479-1 1990 The use of oxime reactivators of inhibited cholinesterase enzymes in poisoning by carbamate compounds has received mixed reviews in the medical literature. Oximes 11-16 butyrylcholinesterase Homo sapiens 43-57 33802843-11 2021 Our present data, together with previous results on other OPCs, indicate that the experimental oximes K-27 and K-48 are very promising pretreatment compounds. Oximes 95-101 keratin 27 Rattus norvegicus 102-106 33872504-2 2021 Our convergent synthesis features a [3+2] dipolar cycloaddition of an olefin-bearing 1,3-syn diol unit and an oxime segment containing 1,2-syn diol functionality as the key step. Oximes 110-115 synemin Homo sapiens 15-18 33588047-3 2021 We report the QSAR regression model for the estimation of potency of a set of 94 structurally diverse compounds (oximes, N-hydroxyiminoacetamides, 4-aminoquinolines and flavonoids) to inhibit AChE, pKi (AChE). Oximes 113-119 acetylcholinesterase (Cartwright blood group) Homo sapiens 192-196 33588047-3 2021 We report the QSAR regression model for the estimation of potency of a set of 94 structurally diverse compounds (oximes, N-hydroxyiminoacetamides, 4-aminoquinolines and flavonoids) to inhibit AChE, pKi (AChE). Oximes 113-119 acetylcholinesterase (Cartwright blood group) Homo sapiens 203-207 34846842-4 2021 The labeled O-GlcNAc glycopeptides could be efficiently enriched based on the equilibrium between the hydrazine and oxime bonds. Oximes 116-121 O-linked N-acetylglucosamine (GlcNAc) transferase Homo sapiens 12-20 34968725-8 2022 To this end, we conjugated aldehyde-tagged Env with Propargyl-PEG3-aminooxy linker (oxime ligation; Step-one) and coupled these conjugates by copper-catalyzed azide-alkyne cycloaddition (Click reaction; Step-two) to calcium phosphate nanoparticles (CaPs) functionalized with terminal azide groups. Oximes 84-89 endogenous retrovirus group W member 1, envelope Homo sapiens 43-46 34844036-0 2022 Novel O-acylated (E)-3-aryl-6,7-dihydrobenzisoxazol-4(5H)-one oximes targeting HSP90-HER2 axis in breast cancer cells. Oximes 62-68 heat shock protein 90 alpha family class A member 1 Homo sapiens 79-84 34844036-0 2022 Novel O-acylated (E)-3-aryl-6,7-dihydrobenzisoxazol-4(5H)-one oximes targeting HSP90-HER2 axis in breast cancer cells. Oximes 62-68 erb-b2 receptor tyrosine kinase 2 Homo sapiens 85-89 34844036-1 2022 Novel O-acylated (E)-3-aryl-6,7-dihydrobenzisoxazol-4(5H)-one oximes were designed as potential HSP90 inhibitors. Oximes 62-68 heat shock protein 90 alpha family class A member 1 Homo sapiens 96-101 34145064-2 2021 In considering dosing requirements for oxime antidotes in OP exposures that inactivate AChE, clearance of proton ionizable, zwitterionic antidotes is rapid and proceeds with largely the parent antidotal compound being cleared by renal transporters. Oximes 39-44 acetylcholinesterase Mus musculus 87-91 34796899-7 2021 The stable oxime makes extensive interactions with ODC but cannot be catabolized, explaining APA"s high potency in ODC inhibition. Oximes 11-16 ornithine decarboxylase 1 Homo sapiens 51-54 34796899-7 2021 The stable oxime makes extensive interactions with ODC but cannot be catabolized, explaining APA"s high potency in ODC inhibition. Oximes 11-16 ornithine decarboxylase 1 Homo sapiens 115-118 34399903-3 2021 Based on chemoselective formation of oximes by solid phase immobilized hydroxylamine derivatives we proposed the protocol for derivatization and selective detection of carbonylated compounds in human serum albumin hydrolysate as a complex peptide mixture and of testosterone in urine samples. Oximes 37-43 albumin Homo sapiens 200-213 34773452-1 2021 A series of 5-(4-pyridyl)-1,2,4-triazoles hybrids with acetophenones and their oxime derivatives was rationally designed and synthesized as epidermal growth factor receptor (EGFR) kinase inhibitors. Oximes 79-84 epidermal growth factor receptor Homo sapiens 140-172 34773452-1 2021 A series of 5-(4-pyridyl)-1,2,4-triazoles hybrids with acetophenones and their oxime derivatives was rationally designed and synthesized as epidermal growth factor receptor (EGFR) kinase inhibitors. Oximes 79-84 epidermal growth factor receptor Homo sapiens 174-178 34558680-0 2022 Caged Oxime Reactivators Designed for the Light Control of Acetylcholinesterase Reactivation. Oximes 6-11 acetylcholinesterase (Cartwright blood group) Homo sapiens 59-79 34558680-2 2022 Here, we describe synthesis, photochemical properties, and biochemical activities of two caged oxime compounds applied in the photocontrolled reactivation of the AChE inactivated by reactive organophosphate. Oximes 95-100 acetylcholinesterase (Cartwright blood group) Homo sapiens 162-166 34558680-3 2022 Each of these consists of a photocleavable coumarin cage tethered to a known oxime reactivator for AChE that belongs in an either 2-(hydroxyimino)acetamide or pyridiniumaldoxime class. Oximes 77-82 acetylcholinesterase (Cartwright blood group) Homo sapiens 99-103 34577159-3 2021 We synthesized 13 derivatives of our reported JNK inhibitor 11H-indeno(1,2-b)quinoxalin-11-one oxime and evaluated their binding to the three JNK isoforms and their biological effects. Oximes 95-100 mitogen-activated protein kinase 8 Homo sapiens 46-49 34577159-3 2021 We synthesized 13 derivatives of our reported JNK inhibitor 11H-indeno(1,2-b)quinoxalin-11-one oxime and evaluated their binding to the three JNK isoforms and their biological effects. Oximes 95-100 mitogen-activated protein kinase 8 Homo sapiens 142-145 34541552-3 2021 Reactivation of inhibited hAChE can be achieved with nucleophilic antidotes, such as oximes. Oximes 85-91 acetylcholinesterase (Cartwright blood group) Homo sapiens 26-31 34541552-5 2021 Here we report X-ray structures of hAChE conjugated with a reversible covalent inhibitor 4K-TMA (4K-TMA:hAChE) at 2.8 A resolution and of 4K-TMA:hAChE conjugate with oxime reactivator methoxime, MMB4 (4K-TMA:hAChE:MMB4) at 2.6 A resolution, both at physiologically relevant room temperature, as well as cryo-crystallographic structure of 4K-TMA:hAChE at 2.4 A resolution. Oximes 166-171 acetylcholinesterase (Cartwright blood group) Homo sapiens 145-150 34324828-5 2021 We also demonstrate the dissociation of organophosphate (OP)-conjugated dimers is reversed by structurally diverse oximes 2PAM, HI6 or RS194B, as demonstrated by SAXS of diethylphosphoryl-hAChE. Oximes 115-121 acetylcholinesterase (Cartwright blood group) Homo sapiens 188-193 34324828-6 2021 However, binding of oximes to the native ligand-free hAChE, binding of high-affinity reversible ligands, or formation of a SP-sarin-hAChE conjugate had no effect on homodimerization. Oximes 20-26 acetylcholinesterase (Cartwright blood group) Homo sapiens 53-58 34671741-0 2021 Dual acting oximes designed for therapeutic decontamination of reactive organophosphates via catalytic inactivation and acetylcholinesterase reactivation. Oximes 12-18 acetylcholinesterase (Cartwright blood group) Homo sapiens 120-140 34671741-5 2021 This library was screened by enzyme assays performed with human and electric eel subtypes of OP-inactivated AChE, which led to identifying three oxime leads that displayed significant enhancements in reactivation activity comparable to 2-PAM. Oximes 145-150 acetylcholinesterase (Cartwright blood group) Homo sapiens 108-112 34067242-4 2021 Some oximes are inhibitors of lipoxygenase 5, human neutrophil elastase, and proteinase 3. Oximes 5-11 elastase, neutrophil expressed Homo sapiens 52-71 34330964-2 2021 The current standard treatment against their effects relies on the use of small molecule-based oximes that can efficiently restore acetylcholinesterase (AChE) activity. Oximes 95-101 acetylcholinesterase (Cartwright blood group) Homo sapiens 131-151 34330964-2 2021 The current standard treatment against their effects relies on the use of small molecule-based oximes that can efficiently restore acetylcholinesterase (AChE) activity. Oximes 95-101 acetylcholinesterase (Cartwright blood group) Homo sapiens 153-157 34067242-4 2021 Some oximes are inhibitors of lipoxygenase 5, human neutrophil elastase, and proteinase 3. Oximes 5-11 proteinase 3 Homo sapiens 77-89 35628301-0 2022 Oxygen Binding by Co(II) Complexes with Oxime-Containing Schiff Bases in Solution. Oximes 40-45 mitochondrially encoded cytochrome c oxidase II Homo sapiens 18-24 35489467-0 2022 Theoretical assessment of the performances of commercial oximes on the reactivation of acetylcholinesterase inhibited by the nerve agent A-242 (novichok). Oximes 57-63 acetylcholinesterase (Cartwright blood group) Homo sapiens 87-107 35526478-2 2022 Compared to non-halogenated oximes, halogenated oximes showed lower pKa of the oxime group (fluorinated < chlorinated < non-halogenated) along with higher level of oximate anion formation at the physiological pH, and had a higher binding affinity of both AChE and BChE. Oximes 28-34 acetylcholinesterase (Cartwright blood group) Homo sapiens 255-259 35631423-3 2022 The oxime radiotracers were produced by condensation of an aminooxy functionalized PSMA-inhibitor Lys-Urea-Glu scaffold with fluorine-18-labeled aldehydes. Oximes 4-9 folate hydrolase 1 Homo sapiens 83-87 35525902-0 2022 Oxime derivative TFOBO promotes cell death by modulating reactive oxygen species and regulating NADPH oxidase activity in myeloid leukemia. Oximes 0-5 dual oxidase 2 Homo sapiens 96-109 35526478-2 2022 Compared to non-halogenated oximes, halogenated oximes showed lower pKa of the oxime group (fluorinated < chlorinated < non-halogenated) along with higher level of oximate anion formation at the physiological pH, and had a higher binding affinity of both AChE and BChE. Oximes 28-34 butyrylcholinesterase Homo sapiens 264-268 35526478-2 2022 Compared to non-halogenated oximes, halogenated oximes showed lower pKa of the oxime group (fluorinated < chlorinated < non-halogenated) along with higher level of oximate anion formation at the physiological pH, and had a higher binding affinity of both AChE and BChE. Oximes 48-54 acetylcholinesterase (Cartwright blood group) Homo sapiens 255-259 35526478-2 2022 Compared to non-halogenated oximes, halogenated oximes showed lower pKa of the oxime group (fluorinated < chlorinated < non-halogenated) along with higher level of oximate anion formation at the physiological pH, and had a higher binding affinity of both AChE and BChE. Oximes 48-54 butyrylcholinesterase Homo sapiens 264-268 35526478-2 2022 Compared to non-halogenated oximes, halogenated oximes showed lower pKa of the oxime group (fluorinated < chlorinated < non-halogenated) along with higher level of oximate anion formation at the physiological pH, and had a higher binding affinity of both AChE and BChE. Oximes 79-84 acetylcholinesterase (Cartwright blood group) Homo sapiens 255-259 35526478-2 2022 Compared to non-halogenated oximes, halogenated oximes showed lower pKa of the oxime group (fluorinated < chlorinated < non-halogenated) along with higher level of oximate anion formation at the physiological pH, and had a higher binding affinity of both AChE and BChE. Oximes 79-84 butyrylcholinesterase Homo sapiens 264-268 35526478-6 2022 The advantage of halogen substituents in the stabilization of oxime in a position optimal for in-line nucleophilic attack were confirmed by extensive molecular modelling of pre-reactivation complexes between the analogue oximes and phosphorylated AChE and BChE. Oximes 62-67 acetylcholinesterase (Cartwright blood group) Homo sapiens 247-251 35526478-6 2022 The advantage of halogen substituents in the stabilization of oxime in a position optimal for in-line nucleophilic attack were confirmed by extensive molecular modelling of pre-reactivation complexes between the analogue oximes and phosphorylated AChE and BChE. Oximes 62-67 butyrylcholinesterase Homo sapiens 256-260 35526478-6 2022 The advantage of halogen substituents in the stabilization of oxime in a position optimal for in-line nucleophilic attack were confirmed by extensive molecular modelling of pre-reactivation complexes between the analogue oximes and phosphorylated AChE and BChE. Oximes 221-227 acetylcholinesterase (Cartwright blood group) Homo sapiens 247-251 35526478-6 2022 The advantage of halogen substituents in the stabilization of oxime in a position optimal for in-line nucleophilic attack were confirmed by extensive molecular modelling of pre-reactivation complexes between the analogue oximes and phosphorylated AChE and BChE. Oximes 221-227 butyrylcholinesterase Homo sapiens 256-260 2818204-2 1989 The pharmacokinetics of a cholinesterase reactivating oxime, 2-PAM, was comparatively studied in healthy volunteers and in persons suffering from poisoning by organophosphorus insecticides. Oximes 54-59 peptidylglycine alpha-amidating monooxygenase Homo sapiens 63-66 35164361-1 2022 A family of novel efficient non-oxime compounds exhibited promising reactivation efficacy for VX and sarin inhibited human acetylcholinesterase was discovered. Oximes 32-37 acetylcholinesterase (Cartwright blood group) Homo sapiens 123-143 35527825-2 2022 We developed a novel QSAR regression model for estimating potency to inhibit AChE, pK i, on a set of 75 structurally different compounds including oximes, N-hydroxyiminoacetamides, 4-aminoquinolines and flavonoids. Oximes 147-153 acetylcholinesterase (Cartwright blood group) Homo sapiens 77-81 35025136-5 2022 Here, we combined genetic code expansion with oxime ligation to generate p53 site-specifically mono-ubiquitylated at position 120. Oximes 46-51 tumor protein p53 Homo sapiens 73-76 2613337-4 1989 The most notable differences in substrate profiles between the extended broad spectrum enzymes and TEM-2 enzymes occurred with oxime-containing antibiotics. Oximes 127-132 RASD family member 2 Homo sapiens 99-104 2605226-6 1989 The maximum of the difference spectrum between either chicken red or rhodopsin and its photoproduct (all-trans-retinal oxime plus opsin) was determined to be 571 or 503 nm, respectively. Oximes 119-124 rhodopsin Gallus gallus 69-78 2605226-6 1989 The maximum of the difference spectrum between either chicken red or rhodopsin and its photoproduct (all-trans-retinal oxime plus opsin) was determined to be 571 or 503 nm, respectively. Oximes 119-124 opsin 1 (cone pigments), short-wave-sensitive (violet cone opsin) Gallus gallus 73-78 2494778-0 1989 The relationship between oxime-induced reactivation of carbamylated acetylcholinesterase and antidotal efficacy against carbamate intoxication. Oximes 25-30 acetylcholinesterase Rattus norvegicus 68-88 2917984-2 1989 With the exception of the conjugate formed from reaction of AchE with RP-cycloheptyl methylphosphonyl thiocholine, all enantiomeric conjugates underwent oxime reactivation at rates that were within 2-3-fold of each other. Oximes 153-158 acetylcholinesterase (Cartwright blood group) Homo sapiens 60-64 2596267-1 1989 It has been reported recently that some oximes reactivating acetylcholinesterase (AChE) exhibit concomitant ganglion-blocking effects which presumably could contribute independently to their powerful antidotal action in organophosphate inhibitor (OPI) poisoning, thus mimicking some unrelated substances which are effective antidotes without reactivating AChE. Oximes 40-46 acetylcholinesterase (Cartwright blood group) Homo sapiens 60-80 2596267-1 1989 It has been reported recently that some oximes reactivating acetylcholinesterase (AChE) exhibit concomitant ganglion-blocking effects which presumably could contribute independently to their powerful antidotal action in organophosphate inhibitor (OPI) poisoning, thus mimicking some unrelated substances which are effective antidotes without reactivating AChE. Oximes 40-46 acetylcholinesterase (Cartwright blood group) Homo sapiens 82-86 2596267-1 1989 It has been reported recently that some oximes reactivating acetylcholinesterase (AChE) exhibit concomitant ganglion-blocking effects which presumably could contribute independently to their powerful antidotal action in organophosphate inhibitor (OPI) poisoning, thus mimicking some unrelated substances which are effective antidotes without reactivating AChE. Oximes 40-46 acetylcholinesterase (Cartwright blood group) Homo sapiens 355-359 2796731-8 1989 The use of oximes (PAM and Toxobidine) considerably contributed to reactivation of AChE and ChE and to normalization of the test marker enzymes. Oximes 11-17 acetylcholinesterase Rattus norvegicus 83-87 2903553-1 1988 A peptide 60 residues in length that corresponds to the homeo domain of Antennapedia (Antp), a protein governing development in Drosophila, was synthesized by segment condensation with protected peptide segments prepared on an oxime resin. Oximes 227-232 Antennapedia Drosophila melanogaster 72-84 2903553-1 1988 A peptide 60 residues in length that corresponds to the homeo domain of Antennapedia (Antp), a protein governing development in Drosophila, was synthesized by segment condensation with protected peptide segments prepared on an oxime resin. Oximes 227-232 Antennapedia Drosophila melanogaster 86-90 2452874-1 1988 Interactions of the oximes pyridine-2-aldoxime (2-PAM) and 1-(2-hydroxyiminomethyl-1-pyridino)-3-(4-carbamoyl-1-pyridino++ +)-2-oxapropane dichloride (HI-6), reactivators of phosphorylated acetylcholinesterase enzyme, with the nicotinic acetylcholine receptor-ion channel complex were studied using electrophysiological techniques. Oximes 20-26 peptidylglycine alpha-amidating monooxygenase Homo sapiens 50-53 3057326-4 1988 The mechanism of action of organophosphates has been determined in some depth; the understanding of the toxic effects resulting from the inhibition of cholinesterase activity, causing accumulation of acetylcholine at nerve endings has played a major part in providing a rationale for specific antidote treatment using atropine and oximes. Oximes 331-337 butyrylcholinesterase Homo sapiens 151-165 3345199-1 1988 Acetylcholinesterase (AChE) inhibited by the organophosphate soman (1,2,2-trimethyl-propylmethylphosphonofluoridate) rapidly becomes resistant to reactivation by oximes due to dealkylation of the soman-enzyme complex. Oximes 162-168 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-20 3345199-1 1988 Acetylcholinesterase (AChE) inhibited by the organophosphate soman (1,2,2-trimethyl-propylmethylphosphonofluoridate) rapidly becomes resistant to reactivation by oximes due to dealkylation of the soman-enzyme complex. Oximes 162-168 acetylcholinesterase (Cartwright blood group) Homo sapiens 22-26 3827595-6 1986 The concentration of the oxime in CSF increased rapidly during the absorption phase (by 30 min after injection). Oximes 25-30 colony stimulating factor 2 Canis lupus familiaris 34-37 3299873-5 1987 The serum oxime concentrations (ED50 values) for HI-6, obidoxime, and PAM against a 3 LD50 dose of sarin were 0.72, 9.05, and 2.56 micrograms/ml, respectively. Oximes 10-15 peptidylglycine alpha-amidating monooxygenase Rattus norvegicus 70-73 3566284-0 1987 Oxime-metabolizing activity of liver aldehyde oxidase. Oximes 0-5 aldehyde oxidase 1 Homo sapiens 37-53 3566284-1 1987 Liver aldehyde oxidase in the presence of its electron donor exhibited a significant oxime-metabolizing activity toward some different types of oximes under anaerobic conditions. Oximes 85-90 aldehyde oxidase 1 Homo sapiens 6-22 3566284-1 1987 Liver aldehyde oxidase in the presence of its electron donor exhibited a significant oxime-metabolizing activity toward some different types of oximes under anaerobic conditions. Oximes 144-150 aldehyde oxidase 1 Homo sapiens 6-22 3566284-5 1987 We propose a mechanism of oxime biotransformation that liver aldehyde oxidase catalyzes the reduction of oximes to the corresponding ketimines which in turn undergo, depending on their chemical stability, nonenzymatic hydrolysis to the corresponding oxo compounds and ammonia. Oximes 26-31 aldehyde oxidase 1 Homo sapiens 61-77 3566284-5 1987 We propose a mechanism of oxime biotransformation that liver aldehyde oxidase catalyzes the reduction of oximes to the corresponding ketimines which in turn undergo, depending on their chemical stability, nonenzymatic hydrolysis to the corresponding oxo compounds and ammonia. Oximes 105-111 aldehyde oxidase 1 Homo sapiens 61-77 3807651-1 1987 The generally accepted explanation for the effects of oximes in countering organophosphorus (OP) anticholinesterase is reactivation of the inhibited acetylcholinesterase (AChE). Oximes 54-60 acetylcholinesterase Cavia porcellus 149-169 3807651-1 1987 The generally accepted explanation for the effects of oximes in countering organophosphorus (OP) anticholinesterase is reactivation of the inhibited acetylcholinesterase (AChE). Oximes 54-60 acetylcholinesterase Cavia porcellus 171-175 3807651-2 1987 With soman, the inhibited AChE rapidly becomes resistant to oxime reactivation due to a phenomenon called aging. Oximes 60-65 acetylcholinesterase Cavia porcellus 26-30 3807651-9 1987 The data from in vitro and in vivo experiments revealed that oximes accelerated the decarbamylation (p less than 0.05) of inhibited AChE. Oximes 61-67 acetylcholinesterase Cavia porcellus 132-136 2452874-8 1988 Our study demonstrates a direct molecular interaction of the oximes HI-6 and 2-PAM with the natural agonist molecule and with the acetylcholine receptor-ion channel complex. Oximes 61-67 peptidylglycine alpha-amidating monooxygenase Homo sapiens 79-82 3746817-5 1986 In this series, varying R substituents on the aryl ring produced compounds with oxime pKa values from 6.8 to 8.0, optimum for an AChE reactivator. Oximes 80-85 acetylcholinesterase (Cartwright blood group) Homo sapiens 129-133 3954783-3 1986 The rates of inhibition of AChE by these phosphylated oximes and the parent (and related) organophosphates have also been measured. Oximes 54-60 acetylcholinesterase (Cartwright blood group) Homo sapiens 27-31 2423865-8 1986 Monoclonal antibodies raised against the oxime conjugate such as 258(2)-1 (herein referred to as mAb D) primarily recognized chemical determinants in ring 2 and the tertiary amino group of the piperidine ring. Oximes 41-46 H2-K region expressed gene 6 Mus musculus 150-156 3751113-5 1986 The oxime metabolites were formed as mixtures of two geometric isomers, Z (syn-phenyl) and E (anti-phenyl), wherein the phenyl and hydroxyl group are cis and trans to each other respectively. Oximes 4-9 synemin Homo sapiens 75-78 3972833-6 1985 NBD-aminoethyl methylphosphono-acetylcholinesterase undergoes oxime-induced as well as spontaneous reactivation at rates that are 3.6 and 35 times faster, respectively, than the corresponding rates measured for the NBD-aminopentyl conjugate. Oximes 62-67 acetylcholinesterase (Cartwright blood group) Homo sapiens 31-51 3951676-2 1986 However, a partial protection of AChE in brain against inhibition by soman was obtained in anaesthetized, atropinized rats by the oxime injected into the cerebral ventricle 5 min before parenteral exposure to soman. Oximes 130-135 acetylcholinesterase Rattus norvegicus 33-37 6389867-6 1984 Thus structural changes at the C-6 position to produce diaziridines, oximes, and oxime O-methyl ethers provide compounds retaining expected opioid activity. Oximes 69-75 complement C6 Homo sapiens 31-34 6710513-3 1984 Atropine and the oximes were less effective as profenofos antidotes, indicating that profenofos-inhibited AChE may undergo rapid aging. Oximes 17-23 acetylcholinesterase Mus musculus 106-110 6497906-0 1984 The reactivation by oximes of phosphonylated acetylcholinesterase: the possible erroneous interpretation of reactivating potency. Oximes 20-26 acetylcholinesterase (Cartwright blood group) Homo sapiens 45-65 6497906-1 1984 A comparative study of the reactivation by two oximes of acetylcholinesterase inhibited by several organophosphates has been made, with particular reference to the dependence of the degree of reactivation produced by an oxime (reactivating potency) upon the concentration of inhibited enzyme. Oximes 47-53 acetylcholinesterase (Cartwright blood group) Homo sapiens 57-77 6497906-1 1984 A comparative study of the reactivation by two oximes of acetylcholinesterase inhibited by several organophosphates has been made, with particular reference to the dependence of the degree of reactivation produced by an oxime (reactivating potency) upon the concentration of inhibited enzyme. Oximes 47-52 acetylcholinesterase (Cartwright blood group) Homo sapiens 57-77 6151379-0 1984 [Adrenergic beta 1 and beta 2 blocking activity of new aminopropanols derived from oximes and esters]. Oximes 83-89 potassium calcium-activated channel subfamily M regulatory beta subunit 2 Homo sapiens 0-29 6098298-2 1984 The difference absorption spectrum between the cyclopentatrienylidene 11-cis-locked-rhodopsin and its retinal oxime had its maximum at 495 nm (P-495). Oximes 110-115 rhodopsin Bos taurus 84-93 20487840-4 1981 Rapid hydrolysis of phosphonylated acetylcholinesterase can be brought about by oximes, but dealkylation of the phosphonyl group on the enzyme (known as ageing) renders the inhibited enzyme insensitive to oximes. Oximes 80-86 acetylcholinesterase (Cartwright blood group) Homo sapiens 35-55 6871372-2 1983 In both chloroform and carbon tetrachloride solutions, the exocyclic N4-methoxy group of N4-methoxycytosine, and of 5-methyl N4-methoxycytosine (which is in the oxime form under these conditions), is so oriented that it is predominantly syn to the ring N(3), and neither compound forms planar auto-associates. Oximes 161-166 synemin Homo sapiens 237-240 6628257-5 1983 The effectiveness of these oximes in restoration of VX-inactivated ChE in vivo offers an explanation as to why conventional atropine/oxime therapy is so effective against VX intoxication. Oximes 27-33 butyrylcholinesterase Rattus norvegicus 67-70 6628257-5 1983 The effectiveness of these oximes in restoration of VX-inactivated ChE in vivo offers an explanation as to why conventional atropine/oxime therapy is so effective against VX intoxication. Oximes 27-32 butyrylcholinesterase Rattus norvegicus 67-70 6655549-0 1983 Antigenic properties of estriol 3-glucuronide-[C-6]-bovine serum albumin conjugates having oxime bridges. Oximes 91-96 LOW QUALITY PROTEIN: complement component C6 Oryctolagus cuniculus 47-50 6655549-0 1983 Antigenic properties of estriol 3-glucuronide-[C-6]-bovine serum albumin conjugates having oxime bridges. Oximes 91-96 albumin Oryctolagus cuniculus 59-72 7100228-0 1982 Modification of the level of acetylcholinesterase activity by two oximes in certain brain regions and peripheral tissues of paraoxon treated rats. Oximes 66-72 acetylcholinesterase Rattus norvegicus 29-49 6461392-1 1982 A method is described for the extraction of urinary organic acids in children, their conversion to TMS and oxime TMS derivatives and their separation by gas liquid chromatography on a packed column of 10% OV 101. Oximes 107-112 PYD and CARD domain containing Homo sapiens 113-116 7014032-7 1981 Moreover, the glucose oxidase and the oxime methods for determination of glucose and urea were found to give significantly lower values than the hexokinase and urease methods, respectively. Oximes 38-43 hexokinase 1 Homo sapiens 145-155 6262099-2 1981 It was found that the oxime-mediated recovery of function in both tissues of the rat and guinea pig was composed of direct oxime actions, AChE reactivation and adaptation. Oximes 22-27 acetylcholinesterase Cavia porcellus 138-142 7281197-0 1981 Continual monitoring of the reactivation effect of oximes on blood acetylcholinesterase in the rats poisoned with organophosphates. Oximes 51-57 acetylcholinesterase Rattus norvegicus 67-87 7426043-0 1980 Reactivation of acetylcholinesterase inhibited by 1,2,2"-trimethylpropyl methylphosphonofluoridate (soman) with HI-6 and related oximes. Oximes 129-135 acetylcholinesterase (Cartwright blood group) Homo sapiens 16-36 799866-2 1976 Described is an activating affect (observed for the first time in vivo) on ChE preduced by low and very low concentrations of reactivators of the group of oximes. Oximes 155-161 butyrylcholinesterase Rattus norvegicus 75-78 1015993-0 1976 Potential acetylcholinesterase reactivators: oxime and amidoxime derivatives. Oximes 45-50 acetylcholinesterase (Cartwright blood group) Homo sapiens 10-30 1015993-1 1976 Out of 12 oximes and amidoximes (3 of which were new to the literature) the following showed a distinct antilethal effect in DFP poisoning: RA14 (1-methylbenzimidazole-2-aldoxime methiodide), RA14 (pyridine-4-aldoxime dodecyl bromide), and RA24 (pyridine-2-aldoxime dodecyl bromide). Oximes 10-16 RA14 Homo sapiens 140-144 497002-0 1979 Some adjuncts to oxime-atropine therapy for organophosphate intoxication--their effects on acetylcholinesterase. Oximes 17-22 acetylcholinesterase (Cartwright blood group) Homo sapiens 91-111 435080-5 1979 The oximes with a hydroxyiminomethyl group in position 4 in the pyridinium ring were good reactivators of both phosphorylated and phosphonylated acetylcholinesterase. Oximes 4-10 acetylcholinesterase (Cartwright blood group) Homo sapiens 145-165 799866-4 1976 The low concentrations of the specific oxime ractivators of ChE, followed up by ChDT, can be used as sensitive quantitative indicators of the activity of ChE. Oximes 39-44 butyrylcholinesterase Rattus norvegicus 60-63 799866-4 1976 The low concentrations of the specific oxime ractivators of ChE, followed up by ChDT, can be used as sensitive quantitative indicators of the activity of ChE. Oximes 39-44 butyrylcholinesterase Rattus norvegicus 154-157 18961635-1 1975 A rapid method of simultaneous spectrophotometric determination of up to 4 ppm of iron(II) and 20 ppm of copper(II) in a mixture by chloroform extraction of the syn-phenyl-alpha-pyridyl ketoxime complexes at pH 10.0, is developed. Oximes 186-194 synemin Homo sapiens 161-164 4363351-0 1973 [Proceedings: Relationship of serum cholinesterase level in chronic alcoholic liver disease and appearance of delirium tremens: therapeutic effect of oximes]. Oximes 150-156 butyrylcholinesterase Homo sapiens 36-50 4751672-0 1973 Reactivation of phosphorylated cholinesterase by some imidazole-substituted oximes. Oximes 76-82 butyrylcholinesterase Homo sapiens 31-45 4669224-0 1972 [Competition of an oxime in the binding of cholinesterase and tetanus toxin]. Oximes 19-24 butyrylcholinesterase Homo sapiens 43-57 4110154-11 1972 A wet paste of rhodopsin-digitonin micelles, sheared between glass slides, becomes highly oriented, the rhodopsin chromophores lining up in the direction of shear, the retinal oxime produced by bleaching orienting more perpendicularly to the shear. Oximes 176-181 rhodopsin Homo sapiens 15-24 4110154-11 1972 A wet paste of rhodopsin-digitonin micelles, sheared between glass slides, becomes highly oriented, the rhodopsin chromophores lining up in the direction of shear, the retinal oxime produced by bleaching orienting more perpendicularly to the shear. Oximes 176-181 rhodopsin Homo sapiens 104-113 14249424-0 1964 OXIMES ANTAGONISTIC TO INHIBITORS OF CHOLINESTERASE. Oximes 0-6 butyrylcholinesterase Homo sapiens 37-51 5315345-2 1971 From a comparison of the hypothermia-reducing effects of five cholinesterase-reactivating oximes when injected intraperitoneally or subarachnoidally into rats pretreated with DFP or soman it was possible to distinguish central and peripheral actions of the oximes. Oximes 90-96 butyrylcholinesterase Rattus norvegicus 62-76 5315345-2 1971 From a comparison of the hypothermia-reducing effects of five cholinesterase-reactivating oximes when injected intraperitoneally or subarachnoidally into rats pretreated with DFP or soman it was possible to distinguish central and peripheral actions of the oximes. Oximes 257-263 butyrylcholinesterase Rattus norvegicus 62-76 5439615-0 1970 [Acetylcholinesterase at the motor end plate of the rat diaphragm after poisoning with Paraoxon and Soman during application of oximes]. Oximes 128-134 acetylcholinesterase Rattus norvegicus 0-21 5702864-0 1968 [Behavior of cholinesterase in the blood in relation to treatment with oximes in a case of acute rogor poisoning]. Oximes 71-77 butyrylcholinesterase Homo sapiens 13-27 5594205-0 1967 [Study of the action in vitro of some new oximes on normal cholinesterase and cholinesterase blocked by toxic organophosphoric compounds]. Oximes 42-48 butyrylcholinesterase Homo sapiens 59-73 5594205-0 1967 [Study of the action in vitro of some new oximes on normal cholinesterase and cholinesterase blocked by toxic organophosphoric compounds]. Oximes 42-48 butyrylcholinesterase Homo sapiens 78-92 6027243-0 1967 Oxime reactivation of diethylphosphoryl human serum cholinesterase. Oximes 0-5 butyrylcholinesterase Homo sapiens 52-66 5881660-0 1965 Oxime reactivation of erythrocyte cholinesterase inhibited by ethyl p-nitrophenyl ethylphosphonate. Oximes 0-5 butyrylcholinesterase Homo sapiens 34-48 14234924-0 1964 OXIMES ANTAGONISTIC TO INHIBITORS OF CHOLINESTERASE. Oximes 0-6 butyrylcholinesterase Homo sapiens 37-51 14450082-0 1961 The neutralization of cholinesterase inhibition by various oximes and by atropine. Oximes 59-65 butyrylcholinesterase Homo sapiens 22-36 14126349-0 1964 [EFFECT OF VARIOUS OXIMES DERIVED FROM 1-PHENYL, 1-BENZYL AND 1-PHENACYL PYRIDINE AND ANALOGUES OF 4-FORMYL PYRIDINE IN PARAOXON INTOXICATION]. Oximes 19-25 WD repeat and HMG-box DNA binding protein 1 Homo sapiens 58-63 14026286-3 1962 Prophylactic oxime (2 g. PAM chloride orally) is recommended if the situation permits. Oximes 13-18 peptidylglycine alpha-amidating monooxygenase Homo sapiens 25-28 14463753-5 1962 Strips treated with a high concentration of oxime, sufficient to cause 100% reactivation of cholinesterase, exhibit normal control tone and motility after washing. Oximes 44-49 cholinesterase Oryctolagus cuniculus 92-106 13918437-0 1961 Pharmacological studies of cholinesterase reactivating oximes. Oximes 55-61 butyrylcholinesterase Homo sapiens 27-41 14442184-0 1959 Oxime reactivation studies of inhibited true and pseudo cholinesterase. Oximes 0-5 butyrylcholinesterase Homo sapiens 56-70 14442185-0 1959 Oxime reactivation studies of inhibited true and pseudo cholinesterase. Oximes 0-5 butyrylcholinesterase Homo sapiens 56-70 13355845-0 1956 The kinetics of reactivation, by oximes, of cholinesterase inhibited by organophosphorus compounds. Oximes 33-39 butyrylcholinesterase Homo sapiens 44-58 13526753-0 1957 [Organization of medical aid in phosgene-oxime poisoning]. Oximes 41-46 activation induced cytidine deaminase Homo sapiens 25-28 13276605-0 1955 The reactivation by oximes and hydroxamic acids of cholinesterase inhibited by organo-phosphorus compounds. Oximes 20-26 butyrylcholinesterase Homo sapiens 51-65 33990679-0 2021 Non-quaternary oximes detoxify nerve agents and reactivate nerve agent-inhibited human butyrylcholinesterase. Oximes 15-21 butyrylcholinesterase Homo sapiens 87-108 34019427-0 2021 Effect of Oxime Encapsulation on Acetylcholinesterase Reactivation: Pharmacokinetic Study of the Asoxime-Cucurbit[7]uril Complex in Mice Using Hydrophilic Interaction Liquid Chromatography-Mass Spectrometry. Oximes 10-15 acetylcholinesterase Mus musculus 33-53 34019427-1 2021 Oxime-based molecules are used for the treatment of patients to reactivate acetylcholinesterase (AChE) function after organophosphate intoxication. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 75-95 34019427-1 2021 Oxime-based molecules are used for the treatment of patients to reactivate acetylcholinesterase (AChE) function after organophosphate intoxication. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 97-101 33990679-2 2021 Oxime reactivators of organophosphate (OP)-inhibited acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) serve as antidotes toward poisoning by OPNAs. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 75-79 33990679-2 2021 Oxime reactivators of organophosphate (OP)-inhibited acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) serve as antidotes toward poisoning by OPNAs. Oximes 0-5 butyrylcholinesterase Homo sapiens 85-106 33990679-2 2021 Oxime reactivators of organophosphate (OP)-inhibited acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) serve as antidotes toward poisoning by OPNAs. Oximes 0-5 butyrylcholinesterase Homo sapiens 108-112 33990679-6 2021 EMP-MeCyC detoxification and EMP-BChE reactivation screening campaigns of ~155,000 small molecules resulted in the identification of 33 nucleophile candidates, including non-quaternary oximes. Oximes 185-191 butyrylcholinesterase Homo sapiens 33-37 33990679-7 2021 Four of the oximes were reactivators of both Sarin- and VX-inhibited BChE and directly detoxified Sarin. Oximes 12-18 butyrylcholinesterase Homo sapiens 69-73 33540058-4 2021 For this, (3Z)-5-Chloro-3-(hydroxyimino)indolin-2-one (Cl-HIN), a compound that has properties of isatin and oxime in its structure, have shown reactivating properties in the activity of AChE that have been added to antidepressant-like effects in rats exposed to malathion in acute protocol. Oximes 109-114 acetylcholinesterase Rattus norvegicus 187-191 33545185-0 2021 Determination of K869, a novel oxime reactivator of acetylcholinesterase, in rat body fluids and tissues by liquid-chromatography methods: Pharmacokinetic study. Oximes 31-36 acetylcholinesterase Rattus norvegicus 52-72 33545185-1 2021 Oxime reactivators of acetylcholinesterase (AChE) represent an integral part of standard antidote treatment of organophosphate poisoning. Oximes 0-5 acetylcholinesterase Rattus norvegicus 22-42 33545185-1 2021 Oxime reactivators of acetylcholinesterase (AChE) represent an integral part of standard antidote treatment of organophosphate poisoning. Oximes 0-5 acetylcholinesterase Rattus norvegicus 44-48 33540058-12 2021 Collectively, the results of this study suggest that Cl-HIN is an oxime capable of reactivating AChE inhibited and presents na antidepressant-like effect in cases of prolonged exposure to malathion. Oximes 66-71 acetylcholinesterase Rattus norvegicus 96-100 33592259-9 2021 Novel oxime 15 demonstrated significant broad spectrum reactivation of OP-inhibited rat serum BChE while novel oxime 20 demonstrated significant broad spectrum reactivation of OP-inhibited human serum BChE. Oximes 111-116 butyrylcholinesterase Homo sapiens 201-205 33592259-0 2021 Reactivation of Organophosphate-inhibited Serum Butyrylcholinesterase by Novel Substituted Phenoxyalkyl Pyridinium Oximes and Traditional Oximes. Oximes 115-121 butyrylcholinesterase Homo sapiens 48-69 33592259-3 2021 Oximes are a critical piece to the therapeutic regimen which remove the OP from the inhibited AChE and restore normal cholinergic function. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 94-98 33592259-9 2021 Novel oxime 15 demonstrated significant broad spectrum reactivation of OP-inhibited rat serum BChE while novel oxime 20 demonstrated significant broad spectrum reactivation of OP-inhibited human serum BChE. Oximes 6-11 butyrylcholinesterase Homo sapiens 94-98 33566584-0 2021 Effects of Charged Oxime Reactivators on the HK-2 Cell Line in Renal Toxicity Screening. Oximes 19-24 hexokinase 2 Homo sapiens 45-49 33548273-2 2021 However, available oxime antidote 2-PAM only reactivates OP-inhibited AChE in peripheral tissues. Oximes 19-24 peptidyl-glycine alpha-amidating monooxygenase Cavia porcellus 36-39 33548273-2 2021 However, available oxime antidote 2-PAM only reactivates OP-inhibited AChE in peripheral tissues. Oximes 19-24 acetylcholinesterase Cavia porcellus 70-74 33548273-3 2021 Monoisonitrosoacetone (MINA), a tertiary oxime, reportedly reactivates AChE in the central nervous system (CNS). Oximes 41-46 acetylcholinesterase Cavia porcellus 71-75 33682265-10 2021 Compared with 2-PAM, Oxime 20 stimulated Bcl2l1 expression more and returned expression closer to the vehicle control values. Oximes 21-26 Bcl2-like 1 Rattus norvegicus 41-47 33592259-10 2021 All tested oximes were poor reactivators of OP-inhibited guinea pig serum BChE. Oximes 11-17 butyrylcholinesterase Homo sapiens 74-78 33672922-5 2021 Furthermore, species-specific amino acid differences in acetylcholinesterase confound studies that use oximes or other compounds to restore its function after inhibition by CWNA. Oximes 103-109 acetylcholinesterase Mus musculus 56-76 33135362-0 2021 MS-based screening of small amino acid derived oxime libraries for hGAT3 inhibitors. Oximes 47-52 solute carrier family 6 member 11 Homo sapiens 67-72 33135362-1 2021 Aiming at the identification of new hGAT3 inhibitors, oxime libraries comprising a total of more than 1100 compounds were generated by reaction of various aldehyde and ketone libraries with hydroxylamines that comprised isoserine, 4-amino-2-hydroxybutyric acid, 4-amino-3-hydroxybutyric or nipecotic acid subunits. Oximes 54-59 solute carrier family 6 member 11 Homo sapiens 36-41 33135362-2 2021 The formed oxime libraries were tested for their inhibitory potency at hGAT3 using an MS transporter assay. Oximes 11-16 solute carrier family 6 member 11 Homo sapiens 71-76 33135362-5 2021 1-[2-({[bis(4-chlorophenyl)methylene]amino}oxy)ethyl]piperidine-3-carboxylic acid was found to be the most potent compound of tested oxime (pIC 50 = 5.17 +- 0.12) displaying an inhibitory potency close to the potency of the enantiopure benchmark hGAT3 inhibitor ( S )-SNAP-5114. Oximes 133-138 solute carrier family 6 member 11 Homo sapiens 247-252 33563155-15 2022 The binding of oximes with bovine serum albumin (BSA) revealed static quenching of intrinsic fluorescence of BSA by oxime. Oximes 15-21 albumin Homo sapiens 34-47 33563155-15 2022 The binding of oximes with bovine serum albumin (BSA) revealed static quenching of intrinsic fluorescence of BSA by oxime. Oximes 15-20 albumin Homo sapiens 34-47 33223264-0 2021 Development of programmable gemcitabine-GnRH pro-drugs bearing linker controllable "click" oxime bond tethers and preclinical evaluation against prostate cancer. Oximes 91-96 gonadotropin releasing hormone 1 Mus musculus 40-44 33681810-2 2020 Four sugars, sialic acid, and the dimer through tetramer of alpha-2 8-linked oligosialic acid were added to an aminooxy-terminated hexavalent dendrimer core using a chemoselective oxime-forming reaction. Oximes 180-185 glycoprotein hormone subunit alpha 2 Homo sapiens 60-67 33563155-11 2022 The binding of oximes with bovine serum albumin (BSA) was also investigated by UV-Vis spectrophotometer. Oximes 15-21 albumin Homo sapiens 34-47 33563155-14 2022 Further, in-vitro enzymatic assay indicated reasonable reactivation potential of the oximes against paraoxon-inhibited AChE. Oximes 85-91 acetylcholinesterase (Cartwright blood group) Homo sapiens 119-123 33257873-3 2021 This phosphorylation is a unique cryptic modification as it is introduced in the third of seven steps during aminohexuronic acid (AHA) nucleoside biosynthesis, retained throughout the pathway"s duration, and is removed in the last step of the pathway. Oximes 130-133 cripto, FRL-1, cryptic family 1 Homo sapiens 33-40 32334495-3 2021 When AChE is inhibited by OPs, its reactivation can be usually performed through cationic oximes. Oximes 90-96 acetylcholinesterase (Cartwright blood group) Homo sapiens 5-9 33213094-2 2020 The primary mechanism of organophosphorus toxicity is through inhibition of the enzyme acetylcholinesterase, with current emergency treatment including anticholinergics, benzodiazepines, and oxime reactivators. Oximes 191-196 acetylcholinesterase Danio rerio 87-107 33213094-7 2020 Additionally, the organophosphorus-specific response for oxime reactivation of acetylcholinesterase was comparable to what has been previously reported. Oximes 57-62 acetylcholinesterase Danio rerio 79-99 32896797-0 2020 Combination of MS Binding Assays and affinity selection mass spectrometry for screening of structurally homogenous libraries as exemplified for a focused oxime library addressing the neuronal GABA transporter 1. Oximes 154-159 solute carrier family 6 member 1 Homo sapiens 192-210 32896797-2 2020 After reaction of a nipecotic acid derivative possessing a hydroxylamine functionality with aldehydes, the resulting oxime library was screened accordingly toward the GABA transporter subtype 1 (GAT1), a drug target for several neurological disorders. Oximes 117-122 solute carrier family 6 member 1 Homo sapiens 167-193 32896797-2 2020 After reaction of a nipecotic acid derivative possessing a hydroxylamine functionality with aldehydes, the resulting oxime library was screened accordingly toward the GABA transporter subtype 1 (GAT1), a drug target for several neurological disorders. Oximes 117-122 solute carrier family 6 member 1 Homo sapiens 195-199 32198755-6 2020 Therapeutic guidance concerning the duration and success of the current oxime therapy via determination of the cholinesterase status can contribute to an optimal use of resources. Oximes 72-77 butyrylcholinesterase Homo sapiens 111-125 32319115-1 2020 Oximes remain a long-standing element of the therapy for nerve agents, organophosphates (OPs) that poison by inhibiting the enzyme acetylcholinesterase (AChE), resulting in hypercholinergic activity both centrally and peripherally. Oximes 0-6 acetylcholinesterase Rattus norvegicus 131-151 32319115-1 2020 Oximes remain a long-standing element of the therapy for nerve agents, organophosphates (OPs) that poison by inhibiting the enzyme acetylcholinesterase (AChE), resulting in hypercholinergic activity both centrally and peripherally. Oximes 0-6 acetylcholinesterase Rattus norvegicus 153-157 32319115-2 2020 Oximes, such as the pyridinium oxime pralidoxime (2-PAM) in the United States, can reactivate the inhibited AChE and restore cholinergic function. Oximes 0-6 acetylcholinesterase Rattus norvegicus 108-112 32319115-5 2020 Using high sublethal dosages of the OPs, the novel oximes were observed to attenuate seizure-like behavior in rats and to reduce the levels of glial fibrillary acidic protein (an indicator of glial scarring) to control levels, in contrast to levels observed with 2-PAM or no oxime therapy. Oximes 51-57 glial fibrillary acidic protein Rattus norvegicus 143-174 32319115-5 2020 Using high sublethal dosages of the OPs, the novel oximes were observed to attenuate seizure-like behavior in rats and to reduce the levels of glial fibrillary acidic protein (an indicator of glial scarring) to control levels, in contrast to levels observed with 2-PAM or no oxime therapy. Oximes 51-56 glial fibrillary acidic protein Rattus norvegicus 143-174 32436233-1 2020 Oxime antidotes regenerate organophosphate-inhibited acetylcholinesterase (AChE). Oximes 0-5 acetylcholinesterase Rattus norvegicus 53-73 32436233-1 2020 Oxime antidotes regenerate organophosphate-inhibited acetylcholinesterase (AChE). Oximes 0-5 acetylcholinesterase Rattus norvegicus 75-79 32436233-2 2020 Although they share a common mechanism of AChE reactivation, the rate and amount of oxime that enters the brain are critical to the efficacy, a process linked to the oxime structure and charge. Oximes 84-89 acetylcholinesterase Rattus norvegicus 42-46 32436233-2 2020 Although they share a common mechanism of AChE reactivation, the rate and amount of oxime that enters the brain are critical to the efficacy, a process linked to the oxime structure and charge. Oximes 166-171 acetylcholinesterase Rattus norvegicus 42-46 32544483-0 2020 Oxime-mediated reactivation of organophosphate-inhibited acetylcholinesterase with emphasis on centrally-active oximes. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 57-77 33105595-4 2020 Interestingly, its analogue, an oxime ether with a benzobicyclo[3.2.1]-skeleton, compound 32 was one of the most potent BChE inhibitors in this study (IC50 = 31 microM), but not as potent as endo-43, an ether derivative of the benzobicyclo[3.2.1]octene with an additional phenyl substituent (IC50 = 17 microM). Oximes 32-37 butyrylcholinesterase Homo sapiens 120-124 32835730-0 2020 Effect of P-glycoprotein on the availability of oxime reactivators in the brain. Oximes 48-53 ATP binding cassette subfamily B member 1 Homo sapiens 10-24 32835730-6 2020 A major drawback of currently available oxime reactivators is their inability to reactivate AChE in the central nervous system (CNS) as they are unable to cross the blood-brain barrier. Oximes 40-45 acetylcholinesterase (Cartwright blood group) Homo sapiens 92-96 32835730-8 2020 The aim of this study was to evaluate the effect of P-gp on the permeation of oximes into the brain. Oximes 78-84 ATP binding cassette subfamily B member 1 Homo sapiens 52-56 32544483-0 2020 Oxime-mediated reactivation of organophosphate-inhibited acetylcholinesterase with emphasis on centrally-active oximes. Oximes 112-118 acetylcholinesterase (Cartwright blood group) Homo sapiens 57-77 32786529-5 2020 The activity of the BChE-polymer-oxime conjugates was dependent on the degree of oxime loading within the copolymer side chains. Oximes 33-38 butyrylcholinesterase Homo sapiens 20-24 32786529-6 2020 The covalent modification of oxime-containing copolymers prolonged the activity of BChE in the presence of the VX- and cyclosarin-fluorogenic analogues EMP-MeCyC and CMP-MeCyC, respectively. Oximes 29-34 butyrylcholinesterase Homo sapiens 83-87 32502538-2 2020 Atropine-oximes therapy is commonly used; however, the efficacy of oximes in the reactivation of AChE has been inconsistent. Oximes 67-73 acetylcholinesterase Rattus norvegicus 97-101 32899591-7 2020 Comparing theoretical and experimental data, it is possible to notice that the oxime, in most cases, showed better reactivation percentages at higher concentrations, with the best result for the reactivation of the AChE-VX adduct. Oximes 79-84 acetylcholinesterase (Cartwright blood group) Homo sapiens 215-219 32583098-5 2020 Furthermore, this oxime in combination with BChE exhibited a capability to act as a bioscavenger of cyclosarin, degrading within 2 h up to 100-fold excess of cyclosarin concentration over the enzyme. Oximes 18-23 butyrylcholinesterase Homo sapiens 44-48 32583098-6 2020 Molecular modeling revealed that the position of the cyclohexyl moiety conjugated with the active site serine of BChE directs the favorable positioning of the quinuclidinium ring and the bromophenyl moiety of Q8, which makes phosphonylated-serine easily accessible for the nucleophilic displacement by the oxime group of Q8. Oximes 306-311 butyrylcholinesterase Homo sapiens 113-117 32388435-0 2020 Design, synthesis and evaluation of novel nonquaternary and 3 non-oxime reactivators for acetylcholinesterase inhibited by organophosphates. Oximes 66-71 acetylcholinesterase (Cartwright blood group) Homo sapiens 89-109 32388435-4 2020 It was also found that some non-oxime derivatives of Mannich phenols displayed obvious reactivation potency for VX, sarin and pesticides inhibited hAChE even in very low concentration. Oximes 32-37 acetylcholinesterase (Cartwright blood group) Homo sapiens 147-152 32267631-1 2020 Oximes like pralidoxime (2-PAM), obidoxime (Obi) and HI-6 are the only currently available therapeutics to reactivate inhibited acetylcholinesterase (AChE) in case of intoxications with organophosphorus (OP) compounds. Oximes 0-6 peptidylglycine alpha-amidating monooxygenase Homo sapiens 27-30 32267631-1 2020 Oximes like pralidoxime (2-PAM), obidoxime (Obi) and HI-6 are the only currently available therapeutics to reactivate inhibited acetylcholinesterase (AChE) in case of intoxications with organophosphorus (OP) compounds. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 128-148 32267631-1 2020 Oximes like pralidoxime (2-PAM), obidoxime (Obi) and HI-6 are the only currently available therapeutics to reactivate inhibited acetylcholinesterase (AChE) in case of intoxications with organophosphorus (OP) compounds. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 150-154 32639532-3 2020 The crystal structure was determined for the complex of oxime III within human BChE, confirming that all three binding groups interacted with active site residues. Oximes 56-61 butyrylcholinesterase Homo sapiens 79-83 32639532-4 2020 In the case of BChE inhibited by GF, oximes I (kr = 207 M-1 min-1) and III (kr = 213 M-1 min-1) showed better reactivation efficiency than the reference oxime 2-PAM. Oximes 37-43 butyrylcholinesterase Homo sapiens 15-19 32639532-5 2020 Finally, the key mechanistic steps in the reactivation of GF-inhibited BChE with oxime III were modelled using the PM7R6 method, stressing the importance of proton transfer from Nepsilon of His438 to Ogamma of Ser203 for achieving successful reactivation. Oximes 81-86 butyrylcholinesterase Homo sapiens 71-75 32454005-0 2020 Synthesis and in vitro evaluation of novel non-oximes for the reactivation of nerve agent inhibited human acetylcholinesterase. Oximes 47-53 acetylcholinesterase (Cartwright blood group) Homo sapiens 106-126 32454005-1 2020 Since several decades oximes have been used as part of treatment of nerve agent intoxication with the aim to restore the biological function of the enzyme acetylcholinesterase after its covalent inhibition by organophosphorus compounds such as pesticides and nerve agents. Oximes 22-28 acetylcholinesterase (Cartwright blood group) Homo sapiens 155-175 32388435-1 2020 A new series of novel nonquaternary conjugates and non-oxime reactivators for reactivation of both nerve agents and pesticides inhibited hAChE were described in this paper. Oximes 55-60 acetylcholinesterase (Cartwright blood group) Homo sapiens 137-142 31954867-3 2020 Three common oximes are available: HI-6, Pralidoxime (2-PAM) and Obidoxime (Obi), all possess a nucleophile that can break the NA-AChE covalent bond. Oximes 13-19 peptidyl-glycine alpha-amidating monooxygenase Cavia porcellus 56-59 32512884-2 2020 One therapeutic approach is the reactivation of inhibited acetylcholinesterase by oximes. Oximes 82-88 acetylcholinesterase Mus musculus 58-78 32333945-0 2020 Efficient detoxification of nerve agents by oxime-assisted reactivation of acetylcholinesterase mutants. Oximes 44-49 acetylcholinesterase (Cartwright blood group) Homo sapiens 75-95 32333945-5 2020 Therefore, this review focuses on oxime-assisted catalysis by AChE mutants that provides a potential means for degradation of organophosphates in the plasma before reaching the cellular target site. Oximes 34-39 acetylcholinesterase (Cartwright blood group) Homo sapiens 62-66 32437172-7 2020 At low molar ratios (1 U:1 AAO/BAO and 1 U:2 AAO/BAO) the dominant species is the uranyl coordinated via the eta1-oxygen atom of the oxime group, while at high molar ratios (1 U:3 AAO/BAO and 1 U:4 AAO/BAO) the dominant species are a tetrameric uranyl-mu3-O-eta1-amidoxime complex similar to compounds 5 and 6 and a uranyl-eta2-amidoxime complex similar to compounds 3 and 4. Oximes 133-138 secreted phosphoprotein 1 Homo sapiens 109-113 31954867-3 2020 Three common oximes are available: HI-6, Pralidoxime (2-PAM) and Obidoxime (Obi), all possess a nucleophile that can break the NA-AChE covalent bond. Oximes 13-19 acetylcholinesterase Cavia porcellus 130-134 32380126-3 2020 Oximes reactivate AChE in both the peripheral nervous system and the CNS. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 18-22 31694074-2 2020 Although inconsistent, the standard treatment consists of a muscarinic receptor antagonist (atropine) and AChE-reactivating molecules such as oximes. Oximes 142-148 acetylcholinesterase Rattus norvegicus 106-110 32281011-5 2020 RESULTS: We found the activity of caspases and serum MDA and TAC were significantly increased after OP poisoning and decreased after the appropriate atropine and oxime treatment course. Oximes 162-167 caspase 9 Homo sapiens 34-42 32105443-2 2020 Oxime reactivators of AChE are used in medical practice in the treatment of nerve agent poisoning, but the search for novel improved reactivators with central activity is an ongoing pursuit. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 22-26 32086265-5 2020 However, in most clinics only determination of plasma butyrylcholinesterase (BChE) is established which lacks a pathophysiological correlate, shows higher variability in the population and behaves different regarding inhibition by OP and reactivation by oximes. Oximes 254-260 butyrylcholinesterase Homo sapiens 77-81 32086265-6 2020 The ChE test kit helped to diagnose atypical cases of OP poisoning, for example, missing of typical muscarinic symptoms, and resulted in administration of pralidoxime, the oxime used in Serbia. Oximes 161-166 butyrylcholinesterase Homo sapiens 4-7 32086265-7 2020 The ChE test kit also allows an initial assessment whether an oxime therapy is successful. Oximes 62-67 butyrylcholinesterase Homo sapiens 4-7 32086265-8 2020 In one case report, AChE activity increased after oxime administration indicating therapeutic success whereas BChE activity did not. Oximes 50-55 acetylcholinesterase (Cartwright blood group) Homo sapiens 20-24 31830555-2 2020 Current post-exposure nerve agent treatment includes atropine to treat overstimulation at muscarinic synapses, a benzodiazepine anti-convulsant, and an oxime to restore the function of AChE. Oximes 152-157 acetylcholinesterase (Cartwright blood group) Homo sapiens 185-189 32236245-1 2020 A near-IR perylene diimide probe (OPR-PDI) containing an oxime-propargyl hybrid moiety at the bay position, was designed and synthesized for detection of Pd species and Cu2+ ions in 90% water, the solid state and MG-63 live cells. Oximes 57-62 peptidyl arginine deiminase 1 Homo sapiens 38-41 32019865-0 2020 Rational design, synthesis and evaluation of uncharged, "smart" bis-oxime antidotes of organophosphate-inhibited human acetylcholinesterase. Oximes 64-73 acetylcholinesterase (Cartwright blood group) Homo sapiens 119-139 32019865-5 2020 On the basis of X-ray structures of a CNS-penetrating reactivator, monoxime RS194B, reversibly bound to native and venomous agent X (VX)-inhibited human AChE (hAChE), here we created seven uncharged acetamido bis-oximes as candidate antidotes. Oximes 199-219 acetylcholinesterase (Cartwright blood group) Homo sapiens 153-157 32175496-0 2020 Molecular Modeling Study of Uncharged Oximes Compared to HI-6 and 2-PAM Inside Human AChE Sarin and VX Conjugates. Oximes 38-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 85-89 32178264-4 2020 Within the most outstanding reactivators, the substances denominated oximes stand out, showing good performance for reactivating AChE and restoring the normal synaptic acetylcholine (ACh) levels. Oximes 69-75 acetylcholinesterase (Cartwright blood group) Homo sapiens 129-133 31971800-0 2020 O-Perfluoropyridin-4-yl Oximes: Iminyl Radical Precursors for Photo- or Thermal-Induced N-O Cleavage in C(sp2)-C(sp3) Bond Formation. Oximes 0-30 Sp2 transcription factor Homo sapiens 104-109 31971800-2 2020 A range of O-perfluoropyridin-4-yl oximes were successfully utilized in C(sp2)-C(sp3) bond formations of quinoxalin-2(1H)-ones and alkenes, providing facile accesses to a range of functionalized alkylnitriles. Oximes 11-41 Sp2 transcription factor Homo sapiens 72-77 31999451-0 2020 Bifunctional Naphthoquinone Aromatic Amide-Oxime Derivatives Exert Combined Immunotherapeutic and Antitumor Effects through Simultaneous Targeting of Indoleamine-2,3-dioxygenase and Signal Transducer and Activator of Transcription 3. Oximes 13-48 signal transducer and activator of transcription 3 Homo sapiens 182-232 31999451-2 2020 In the present study, a set of naphthoquinone aromatic amide-oxime derivatives were designed, which stimulated the immune response via IDO1 inhibition and simultaneously displayed powerful antitumor activity against three selected cancer cell lines through suppressing STAT3 signaling. Oximes 31-66 indoleamine 2,3-dioxygenase 1 Homo sapiens 135-139 32175496-3 2020 HI-6 and 2-PAM are cationic oximes proved to be effective for the reactivation of AChE inhibited by the nerve agents VX and sarin (GB). Oximes 28-34 peptidylglycine alpha-amidating monooxygenase Homo sapiens 11-14 32175496-3 2020 HI-6 and 2-PAM are cationic oximes proved to be effective for the reactivation of AChE inhibited by the nerve agents VX and sarin (GB). Oximes 28-34 acetylcholinesterase (Cartwright blood group) Homo sapiens 82-86 32175496-5 2020 Uncharged oximes appear as an interesting alternative to solve this problem, but the development and enhancement of more efficient uncharged oximes capable of reactivating human AChE is still necessary. Oximes 10-16 acetylcholinesterase (Cartwright blood group) Homo sapiens 178-182 32175496-5 2020 Uncharged oximes appear as an interesting alternative to solve this problem, but the development and enhancement of more efficient uncharged oximes capable of reactivating human AChE is still necessary. Oximes 141-147 acetylcholinesterase (Cartwright blood group) Homo sapiens 178-182 32175496-7 2020 In order to investigate the interaction and behavior of cationic and uncharged oximes, we performed here molecular docking, molecular dynamics simulations, and binding energies calculations of the known cationic oximes HI-6 and 2-PAM plus four uncharged oximes found in the literature, complexed with human AChE (HssACHE) conjugated with the nerve agents VX and GB. Oximes 79-85 peptidylglycine alpha-amidating monooxygenase Homo sapiens 230-233 32175496-8 2020 The uncharged oximes showed different behaviors, especially RS194B, which presented stability inside AChE-VX, but presented free binding energy lower than cationic oximes, suggesting that structural alterations could favor its interactions with these complexes. Oximes 14-20 acetylcholinesterase (Cartwright blood group) Homo sapiens 101-105 32175496-9 2020 In contrast, HI-6 and 2-PAM showed higher affinities with more negative binding energy values and larger contribution of the amino acid Asp74, demonstrating the importance of the quaternary nitrogen to the affinity and interaction of oximes with AChE-GB and AChE-VX conjugates. Oximes 234-240 peptidylglycine alpha-amidating monooxygenase Homo sapiens 24-27 32175496-9 2020 In contrast, HI-6 and 2-PAM showed higher affinities with more negative binding energy values and larger contribution of the amino acid Asp74, demonstrating the importance of the quaternary nitrogen to the affinity and interaction of oximes with AChE-GB and AChE-VX conjugates. Oximes 234-240 acetylcholinesterase (Cartwright blood group) Homo sapiens 246-250 31784187-3 2020 We designed and synthesized a series of substituted nitric oxide (NO)-releasing quinolone-1,2,4-triazole/oxime hybrids, hypothesizing that the introduction of a STAT3 binding scaffold would augment their cytotoxicity. Oximes 105-110 signal transducer and activator of transcription 3 Mus musculus 161-166 31999451-2 2020 In the present study, a set of naphthoquinone aromatic amide-oxime derivatives were designed, which stimulated the immune response via IDO1 inhibition and simultaneously displayed powerful antitumor activity against three selected cancer cell lines through suppressing STAT3 signaling. Oximes 31-66 signal transducer and activator of transcription 3 Homo sapiens 269-274 31158460-0 2020 Novel centrally active oxime reactivators of acetylcholinesterase inhibited by surrogates of sarin and VX. Oximes 23-28 acetylcholinesterase Rattus norvegicus 45-65 31022458-1 2020 There is a unique in vivo interplay involving the mechanism of inactivation of acetylcholinesterase (AChE) by toxic organophosphorus (OP) compounds and the restoration of AChE activity by oxime antidotes. Oximes 188-193 acetylcholinesterase (Cartwright blood group) Homo sapiens 171-175 31022458-2 2020 OP compounds form covalent adducts to this critical enzyme target and oximes are introduced to directly displace the OP from AChE. Oximes 70-76 acetylcholinesterase (Cartwright blood group) Homo sapiens 125-129 31586705-0 2019 Oleanolic acid oxime derivatives and their conjugates with aspirin modulate the NF-kappaB-mediated transcription in HepG2 hepatoma cells. Oximes 0-20 nuclear factor kappa B subunit 1 Homo sapiens 80-89 31586705-1 2019 The aim of this study was to evaluate the effect of new oleanolic acid oxime (OAO) derivatives and their conjugates with aspirin (ASP) on the expression and activation of NF-kappaB in human hepatoma HepG2 cells. Oximes 56-76 nuclear factor kappa B subunit 1 Homo sapiens 171-180 31586705-1 2019 The aim of this study was to evaluate the effect of new oleanolic acid oxime (OAO) derivatives and their conjugates with aspirin (ASP) on the expression and activation of NF-kappaB in human hepatoma HepG2 cells. Oximes 78-81 nuclear factor kappa B subunit 1 Homo sapiens 171-180 31586705-3 2019 Moreover, conjugation of OAO with ASP led to enhanced downregulation of NF-kappaB expression and activation. Oximes 25-28 nuclear factor kappa B subunit 1 Homo sapiens 72-81 31586705-6 2019 The results of this study indicate that the new derivatives of OAO and particularly their conjugates with ASP, downregulate the expression of COX-2 in HepG2 cells by modulating the NF-kappaB signaling pathway and suggest their potential application in the prevention of liver inflammation and cancer. Oximes 63-66 mitochondrially encoded cytochrome c oxidase II Homo sapiens 142-147 31586705-6 2019 The results of this study indicate that the new derivatives of OAO and particularly their conjugates with ASP, downregulate the expression of COX-2 in HepG2 cells by modulating the NF-kappaB signaling pathway and suggest their potential application in the prevention of liver inflammation and cancer. Oximes 63-66 nuclear factor kappa B subunit 1 Homo sapiens 181-190 31521263-2 2019 Herein, a synergetic targeted combination chemotherapy of doxorubicin (DOX) and cisplatin in breast cancer was realized by HER2 antibody-decorated nanoparticles assembled from aldehyde hyaluronic acid (AHA) and hydroxyethyl chitosan (HECS). Oximes 202-205 erb-b2 receptor tyrosine kinase 2 Homo sapiens 123-127 31074292-3 2019 To investigate these interactions, theoretical results from docking were first compared with experimental data of hybrid 5C, 4-PA, and two commercial oximes, on the reactivation of human AChE (HssAChE) inhibited by VX. Oximes 150-156 acetylcholinesterase (Cartwright blood group) Homo sapiens 187-191 31264735-7 2019 The other oximes reduced the RR to 0.13 (obidoxime), 0.20 (K-203), 0.21 (K-74), 0.24 (K-75) and 0.26 (pralidoxime), which were significantly more efficacious than 10-methylacridine (RR = 0.65). Oximes 10-16 keratin 74 Homo sapiens 73-77 31264735-7 2019 The other oximes reduced the RR to 0.13 (obidoxime), 0.20 (K-203), 0.21 (K-74), 0.24 (K-75) and 0.26 (pralidoxime), which were significantly more efficacious than 10-methylacridine (RR = 0.65). Oximes 10-16 keratin 75 Homo sapiens 86-90 31549708-1 2019 A tridentate ligand LH3 (C11H13N3O4) comprising o-vanillin, hydrazone and oxime donor groups has been employed to prepare a new class of di- and tetranuclear LnIII complexes. Oximes 74-79 procollagen-lysine,2-oxoglutarate 5-dioxygenase 3 Homo sapiens 20-23 31414695-4 2019 Here, we report the synthesis and biological evaluation of a novel bimodal oxime conjugate composed of a photosensitizing drug, red-emitting pheophorbide a, and nandrolone (NT), a steroid specifically binding the androgen receptor (AR) commonly overexpressed in various tumors. Oximes 75-80 androgen receptor Homo sapiens 213-230 31414695-4 2019 Here, we report the synthesis and biological evaluation of a novel bimodal oxime conjugate composed of a photosensitizing drug, red-emitting pheophorbide a, and nandrolone (NT), a steroid specifically binding the androgen receptor (AR) commonly overexpressed in various tumors. Oximes 75-80 androgen receptor Homo sapiens 232-234 31414695-12 2019 The oxime ether bond degradation was assayed in living cells by both real-time microscopy and a steroid receptor reporter assay using AR U-2 OS cells. Oximes 4-9 androgen receptor Homo sapiens 134-136 31540034-6 2019 Moreover, for the products containing electron-donating substituents (-CH3, -OCH3), the isomerization from the oxime anti to syn isomer under acidic conditions was discovered. Oximes 111-116 synemin Homo sapiens 125-128 31540034-8 2019 From NMR data the syn and anti structures of produced oximes were elucidated. Oximes 54-60 synemin Homo sapiens 18-21 31516541-2 2019 In this study, we investigated the effects of a new oxime, (3Z)-5-Chloro-3-(Hydroxyimino)indolin-2-one (OXIME) against the alterations induced by malathion, an OP insecticide, acute exposure on markers of hepatic damage, glucose homeostasis, oxidative stress in rats cholinesterase (ChE) activity in rats. Oximes 52-57 butyrylcholinesterase Rattus norvegicus 267-281 31516541-2 2019 In this study, we investigated the effects of a new oxime, (3Z)-5-Chloro-3-(Hydroxyimino)indolin-2-one (OXIME) against the alterations induced by malathion, an OP insecticide, acute exposure on markers of hepatic damage, glucose homeostasis, oxidative stress in rats cholinesterase (ChE) activity in rats. Oximes 52-57 butyrylcholinesterase Rattus norvegicus 283-286 31516541-2 2019 In this study, we investigated the effects of a new oxime, (3Z)-5-Chloro-3-(Hydroxyimino)indolin-2-one (OXIME) against the alterations induced by malathion, an OP insecticide, acute exposure on markers of hepatic damage, glucose homeostasis, oxidative stress in rats cholinesterase (ChE) activity in rats. Oximes 104-109 butyrylcholinesterase Rattus norvegicus 267-281 31516541-2 2019 In this study, we investigated the effects of a new oxime, (3Z)-5-Chloro-3-(Hydroxyimino)indolin-2-one (OXIME) against the alterations induced by malathion, an OP insecticide, acute exposure on markers of hepatic damage, glucose homeostasis, oxidative stress in rats cholinesterase (ChE) activity in rats. Oximes 104-109 butyrylcholinesterase Rattus norvegicus 283-286 31516541-7 2019 Results: The OXIME blocked the increase of plasma markers of hepatic function (AST and ALP) and the enzymatic inhibition of catalase and glutathione reductase in the liver of malathion-treated rats. Oximes 13-18 glutathione-disulfide reductase Rattus norvegicus 137-158 31276662-0 2019 Reactivation potency of two novel oximes (K456 and K733) against paraoxon-inhibited acetyl and butyrylcholinesterase: In silico and in vitro models. Oximes 34-40 butyrylcholinesterase Homo sapiens 95-116 31276662-3 2019 Present study evaluates reactivation potency of two newly developed oximes, K456 and K733, against paraoxon (POX)-inhibited human-RBC-AChE and human-plasma-BChE in comparison to reported reactivator, pralidoxime (2-PAM). Oximes 68-74 acetylcholinesterase (Cartwright blood group) Homo sapiens 134-138 31276662-3 2019 Present study evaluates reactivation potency of two newly developed oximes, K456 and K733, against paraoxon (POX)-inhibited human-RBC-AChE and human-plasma-BChE in comparison to reported reactivator, pralidoxime (2-PAM). Oximes 68-74 butyrylcholinesterase Homo sapiens 156-160 31176713-7 2019 Successful solution of the new room temperature 3.2 A resolution structure of BW284c51*hAChE complex from large P31 crystals enables us to proceed with studying room temperature structures of lower affinity complexes, such as oxime reactivators bound to hAChE, where temperature-related conformational diversity could be expected in both oxime and hAChE, which could lead to better informed structure-based design under conditions approaching physiological temperature. Oximes 226-231 acetylcholinesterase (Cartwright blood group) Homo sapiens 87-92 31276662-3 2019 Present study evaluates reactivation potency of two newly developed oximes, K456 and K733, against paraoxon (POX)-inhibited human-RBC-AChE and human-plasma-BChE in comparison to reported reactivator, pralidoxime (2-PAM). Oximes 68-74 peptidylglycine alpha-amidating monooxygenase Homo sapiens 215-218 31276662-4 2019 In vitro studies showed higher intrinsic toxicities of both oximes than 2-PAM for AChE. Oximes 60-66 acetylcholinesterase (Cartwright blood group) Homo sapiens 82-86 31176713-7 2019 Successful solution of the new room temperature 3.2 A resolution structure of BW284c51*hAChE complex from large P31 crystals enables us to proceed with studying room temperature structures of lower affinity complexes, such as oxime reactivators bound to hAChE, where temperature-related conformational diversity could be expected in both oxime and hAChE, which could lead to better informed structure-based design under conditions approaching physiological temperature. Oximes 226-231 ATPase H+ transporting V1 subunit E1 Homo sapiens 112-115 31207225-0 2019 Slight difference in the isomeric oximes K206 and K203 makes huge difference for the reactivation of organophosphorus-inhibited AChE: Theoretical and experimental aspects. Oximes 34-40 acetylcholinesterase Mus musculus 128-132 31176713-7 2019 Successful solution of the new room temperature 3.2 A resolution structure of BW284c51*hAChE complex from large P31 crystals enables us to proceed with studying room temperature structures of lower affinity complexes, such as oxime reactivators bound to hAChE, where temperature-related conformational diversity could be expected in both oxime and hAChE, which could lead to better informed structure-based design under conditions approaching physiological temperature. Oximes 338-343 acetylcholinesterase (Cartwright blood group) Homo sapiens 87-92 31207225-3 2019 Theoretical calculations were performed to assess the difference for the oxime activity with inhibited AChE-complexes and the factors that govern this difference. Oximes 73-78 acetylcholinesterase Mus musculus 103-107 31176713-7 2019 Successful solution of the new room temperature 3.2 A resolution structure of BW284c51*hAChE complex from large P31 crystals enables us to proceed with studying room temperature structures of lower affinity complexes, such as oxime reactivators bound to hAChE, where temperature-related conformational diversity could be expected in both oxime and hAChE, which could lead to better informed structure-based design under conditions approaching physiological temperature. Oximes 338-343 ATPase H+ transporting V1 subunit E1 Homo sapiens 112-115 31138650-0 2019 Productive reorientation of a bound oxime reactivator revealed in room temperature X-ray structures of native and VX-inhibited human acetylcholinesterase. Oximes 36-41 acetylcholinesterase (Cartwright blood group) Homo sapiens 133-153 31138650-4 2019 Current antidotes, including oxime reactivators that attack the OP-AChE conjugate to free the active enzyme, are inefficient. Oximes 29-34 acetylcholinesterase (Cartwright blood group) Homo sapiens 67-71 31138650-6 2019 Here, we present room temperature X-ray structures of native and VX-phosphonylated hAChE with an imidazole-based oxime reactivator, RS-170B. Oximes 113-118 acetylcholinesterase (Cartwright blood group) Homo sapiens 83-88 31097402-0 2019 Application of the concept of oxime library screening by mass spectrometry (MS) binding assays to pyrrolidine-3-carboxylic acid derivatives as potential inhibitors of gamma-aminobutyric acid transporter 1 (GAT1). Oximes 30-35 solute carrier family 6 member 1 Homo sapiens 167-204 31097402-0 2019 Application of the concept of oxime library screening by mass spectrometry (MS) binding assays to pyrrolidine-3-carboxylic acid derivatives as potential inhibitors of gamma-aminobutyric acid transporter 1 (GAT1). Oximes 30-35 solute carrier family 6 member 1 Homo sapiens 206-210 31097402-1 2019 In the present study, the concept of oxime library screening by MS Binding Assays was successfully extended to N-substituted lipophilic pyrrolidine-3-carboxylic acid derivatives in the pursuit of varying the amino acid motif in order to identify new inhibitors for GAT1 and to broaden structure-activity-relationships for this target, the most abundant GABA transporter in the central nervous system. Oximes 37-42 solute carrier family 6 member 1 Homo sapiens 265-269 31097402-5 2019 Thereby, oxime derivatives with a 1,1"-biphenyl moiety were found as the first inhibitors of mGAT1 comprising a pyrrolidine-3-carboxylic acid motif with affinities in the submicromolar range. Oximes 9-14 solute carrier family 6 (neurotransmitter transporter, GABA), member 1 Mus musculus 93-98 31004594-3 2019 Its BChE reactivation potency was showed to be promising when compared to the standard oximes used in medical practice, asoxime (HI-6) and pralidoxime (2-PAM), especially in case of sarin and tabun. Oximes 87-93 butyrylcholinesterase Homo sapiens 4-8 29722548-4 2019 To determine if P-gp affinity screening could be used to reduce animal use, we measured in vitro oxime-stimulated ATPase activity to see if the in vivo reactivation efficacies related to the oximes" functions as P-gp substrates. Oximes 191-197 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 16-20 29722548-4 2019 To determine if P-gp affinity screening could be used to reduce animal use, we measured in vitro oxime-stimulated ATPase activity to see if the in vivo reactivation efficacies related to the oximes" functions as P-gp substrates. Oximes 191-197 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 212-216 29722548-5 2019 High efficacy oximes were expected to be poor P-gp substrates, thus remaining in the brain longer. Oximes 14-20 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 46-50 29722548-6 2019 The high efficacy oximes (24-35% brain AChE reactivation) were worse P-gp substrates than the low efficacy oximes (0-7% brain AChE reactivation). Oximes 18-24 acetylcholinesterase Rattus norvegicus 39-43 29722548-6 2019 The high efficacy oximes (24-35% brain AChE reactivation) were worse P-gp substrates than the low efficacy oximes (0-7% brain AChE reactivation). Oximes 18-24 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 69-73 29722548-6 2019 The high efficacy oximes (24-35% brain AChE reactivation) were worse P-gp substrates than the low efficacy oximes (0-7% brain AChE reactivation). Oximes 18-24 acetylcholinesterase Rattus norvegicus 126-130 29722548-7 2019 However, the oxime group with medium in vivo reactivation of 10-17% were even worse P-gp substrates than the high efficacy group so their reactivation ability was not reflected by P-gp export. Oximes 13-18 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 84-88 29722548-8 2019 The results suggest that in vitro P-gp ATPase activity can remove the low efficacy oximes from in vivo testing, but is not sufficient to differentiate between the top two tiers. Oximes 83-89 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 34-38 31112674-5 2019 The central compartment is readily accessible by the OPs which are lipophilic bullets that can easily cross the BBB, whereas first-line therapeutics, namely oxime-based AChE reactivators and atropine, do not cross or do so rather slowly. Oximes 157-162 acetylcholinesterase (Cartwright blood group) Homo sapiens 169-173 31112674-6 2019 The limitation of oxime-based AChE reactivators can be ascribed to their chemical nature, bearing a positive charge which is essential either for their AChE affinity or their reactivating potency. Oximes 18-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 30-34 31112674-6 2019 The limitation of oxime-based AChE reactivators can be ascribed to their chemical nature, bearing a positive charge which is essential either for their AChE affinity or their reactivating potency. Oximes 18-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 152-156 30858091-12 2019 However, the oxime HI-6 as potent reactivator of cyclosarin-inhibited AChE was not able to prevent the FPDc prolongation in this model. Oximes 13-18 acetylcholinesterase (Cartwright blood group) Homo sapiens 70-74 31136186-2 2019 Under visible-light irradiation, single-electron transfer from fac-Ir(ppy)3 to related oxime takes place followed by a fast beta-fragment of C-C bond to yield aryl and aliphatic acyl radicals, subsequently captured by diverse Michael acceptors. Oximes 87-92 FA complementation group C Homo sapiens 63-66 30950246-3 2019 The current antidotes are oxime-based drugs that can regenerate the AChE catalytic activity. Oximes 26-31 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-72 30978400-2 2019 Currently used therapy in counteracting excessive cholinergic stimulation consists of a muscarinic antagonist (atropine) and an oxime reactivator of inhibited AChE, but the classical oximes are particularly ineffective in counteracting tabun exposure. Oximes 128-133 acetylcholinesterase (Cartwright blood group) Homo sapiens 159-163 30978400-3 2019 In a recent publication (Kovarik et al., 2019), we showed that several oximes prepared by the Huisgen 1,3 dipolar cycloaddition and related precursors efficiently reactivate the tabun-AChE conjugate. Oximes 71-77 acetylcholinesterase (Cartwright blood group) Homo sapiens 184-188 30978400-7 2019 Indeed, after initial screening of the triazole oxime library and its precursors for the reactivation efficacy on Y337A and Y337A/F338A human AChE mutants, we found potentially active oxime-mutant enzyme pairs capable of degrading tabun in cycles of inhibition and reactivation. Oximes 48-53 acetylcholinesterase (Cartwright blood group) Homo sapiens 142-146 30444932-5 2019 Oxime nucleophiles can reactivate select OP-inhibited acetylcholinesterase (AChE). Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 54-74 30444932-5 2019 Oxime nucleophiles can reactivate select OP-inhibited acetylcholinesterase (AChE). Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 76-80 30777661-1 2019 Generation and screening of oxime libraries by competitive MS Binding Assays represents a powerful tool for the identification of new compounds, with affinity to mGAT1, the most abundant plasma membrane bound GABA transporter in the CNS. Oximes 28-33 solute carrier family 6 (neurotransmitter transporter, GABA), member 1 Mus musculus 162-167 30777661-2 2019 By screening a guvacine derived oxime library, new potent inhibitors of mGAT1 had been revealed. Oximes 32-37 solute carrier family 6 (neurotransmitter transporter, GABA), member 1 Mus musculus 72-77 30777661-3 2019 In the present study, oxime libraries generated by reaction of a large excess of a rac-nipecotic acid derivative displaying a hydroxylamine functionality in which various aldehydes under suitable conditions, were examined for new potent inhibitors of mGAT1. Oximes 22-27 solute carrier family 6 (neurotransmitter transporter, GABA), member 1 Mus musculus 251-256 30682493-0 2019 Oxidative stress induced by oxime reactivators of acetylcholinesterase in vitro. Oximes 28-33 acetylcholinesterase (Cartwright blood group) Homo sapiens 50-70 30500087-0 2019 Novel quinoline derivatives carrying nitrones/oximes nitric oxide donors: Design, synthesis, antiproliferative and caspase-3 activation activities. Oximes 46-52 caspase 3 Homo sapiens 115-124 30458057-0 2019 Reversal of Tabun Toxicity Enabled by a Triazole-Annulated Oxime Library-Reactivators of Acetylcholinesterase. Oximes 59-64 acetylcholinesterase (Cartwright blood group) Homo sapiens 89-109 30458057-1 2019 Acetylcholinesterase (AChE), an enzyme that degrades the neurotransmitter acetylcholine, when covalently inhibited by organophosphorus compounds (OPs), such as nerve agents and pesticides, can be reactivated by oximes. Oximes 211-217 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-20 30458057-1 2019 Acetylcholinesterase (AChE), an enzyme that degrades the neurotransmitter acetylcholine, when covalently inhibited by organophosphorus compounds (OPs), such as nerve agents and pesticides, can be reactivated by oximes. Oximes 211-217 acetylcholinesterase (Cartwright blood group) Homo sapiens 22-26 30458057-5 2019 We identified several oximes with significantly improved in vitro reactivating potential for tabun-inhibited human AChE, and in vivo antidotal efficacies in tabun-exposed mice. Oximes 22-28 acetylcholinesterase (Cartwright blood group) Homo sapiens 115-119 30347329-5 2019 Molecular modeling suggested a mode of binding interaction at the JNK catalytic site and that the selected oxime derivatives were potentially competitive JNK inhibitors. Oximes 107-112 mitogen-activated protein kinase 8 Homo sapiens 66-69 30347329-5 2019 Molecular modeling suggested a mode of binding interaction at the JNK catalytic site and that the selected oxime derivatives were potentially competitive JNK inhibitors. Oximes 107-112 mitogen-activated protein kinase 8 Homo sapiens 154-157 30347329-7 2019 Thus, oximes with indenoquinoxaline and tryptanthrin nuclei can serve as specific small-molecule modulators for mechanistic studies of JNK, as well as potential leads for the development of anti-inflammatory drugs. Oximes 6-12 mitogen-activated protein kinase 8 Homo sapiens 135-138 30312685-0 2018 Interactions between acetylcholinesterase, toxic organophosphorus compounds and a short series of structurally related non-oxime reactivators: Analysis of reactivation and inhibition kinetics in vitro. Oximes 123-128 acetylcholinesterase (Cartwright blood group) Homo sapiens 21-41 30362667-1 2018 The current standard therapy to counteract organophosphate intoxication is not effective in equal measure against all types of organophosphorus compounds (OPCs), as the outcome of oxime-induced reactivation of inactivated acetylcholinesterase (AChE) strongly depends on the particular OPC. Oximes 180-185 acetylcholinesterase (Cartwright blood group) Homo sapiens 222-242 30362667-1 2018 The current standard therapy to counteract organophosphate intoxication is not effective in equal measure against all types of organophosphorus compounds (OPCs), as the outcome of oxime-induced reactivation of inactivated acetylcholinesterase (AChE) strongly depends on the particular OPC. Oximes 180-185 acetylcholinesterase (Cartwright blood group) Homo sapiens 244-248 30312685-2 2018 Insufficient efficacy of the standard therapy with atropine and AChE reactivators (oximes) against certain OP initiated synthesis of novel non-oxime reactivators basing on the common structure 4-amino-2-((diethylamino)methyl)phenol (ADOC). Oximes 83-89 acetylcholinesterase (Cartwright blood group) Homo sapiens 64-68 30312685-2 2018 Insufficient efficacy of the standard therapy with atropine and AChE reactivators (oximes) against certain OP initiated synthesis of novel non-oxime reactivators basing on the common structure 4-amino-2-((diethylamino)methyl)phenol (ADOC). Oximes 83-88 acetylcholinesterase (Cartwright blood group) Homo sapiens 64-68 30485691-1 2018 In this study, pyrrolidine-3-acetic acid derived oxime libraries were applied to the concept of library screening by MS Binding Assays, as a powerful technique to reveal new potent murine gamma-aminobutyric acid transporter subtype (mGAT1) inhibitors. Oximes 49-54 solute carrier family 6 (neurotransmitter transporter, GABA), member 1 Mus musculus 233-238 30485691-3 2018 The oxime libraries have been screened by means of competitive MS Binding Assays and, as a consequence, the most active libraries were further investigated through deconvolution experiments to identify single oximes responsible for the observed activity on the target mGAT1. Oximes 4-9 solute carrier family 6 (neurotransmitter transporter, GABA), member 1 Mus musculus 268-273 30485691-3 2018 The oxime libraries have been screened by means of competitive MS Binding Assays and, as a consequence, the most active libraries were further investigated through deconvolution experiments to identify single oximes responsible for the observed activity on the target mGAT1. Oximes 209-215 solute carrier family 6 (neurotransmitter transporter, GABA), member 1 Mus musculus 268-273 30218682-4 2018 HI-6 dimethanesulfonate (HI-6 DMS) is an oxime able to reactivate in vitro and in vivo VR-inhibited AChE. Oximes 41-46 acetylcholinesterase Macaca fascicularis 100-104 30265992-3 2018 The in vitro reactivation experiment for pesticides inhibited hAChE of these new synthesized oximes were conducted for the first time. Oximes 93-99 acetylcholinesterase (Cartwright blood group) Homo sapiens 62-67 30265992-5 2018 It was found that introduction of peripheral site ligands could increase oximes" binding affinity for inhibited hAChE in most cases, which resulted in greater reactivation ability. Oximes 73-79 acetylcholinesterase (Cartwright blood group) Homo sapiens 112-117 30424582-0 2018 Molecular Modeling and In Vitro Studies of a Neutral Oxime as a Potential Reactivator for Acetylcholinesterase Inhibited by Paraoxon. Oximes 53-58 acetylcholinesterase (Cartwright blood group) Homo sapiens 90-110 30496567-7 2018 However, the rats challenged with NIMP or NEMP plus therapy with our novel Oxime 20 (either a bromide or a mesylate salt) showed GFAP levels statistically undistinguishable from controls. Oximes 75-80 glial fibrillary acidic protein Rattus norvegicus 129-133 30176309-8 2018 Oxime K027 was shown to be 1.929-fold more potent considering that 58% increase in AChE activity was achived with the dose BMD58-K027 = 52 mumol/kg in contrast to BMD58-K203 = 100 mumol/kg. Oximes 0-5 Bone mineral density QTL 58 Rattus norvegicus 123-128 30176309-8 2018 Oxime K027 was shown to be 1.929-fold more potent considering that 58% increase in AChE activity was achived with the dose BMD58-K027 = 52 mumol/kg in contrast to BMD58-K203 = 100 mumol/kg. Oximes 0-5 Bone mineral density QTL 58 Rattus norvegicus 163-168 30122284-0 2018 Oximes short-acting CB1 receptor agonists. Oximes 0-6 cannabinoid receptor 1 Homo sapiens 20-23 30374056-0 2018 Dehydroabietic oximes halt pancreatic cancer cell growth in the G1 phase through induction of p27 and downregulation of cyclin D1. Oximes 15-21 dynactin subunit 6 Homo sapiens 94-97 30374056-0 2018 Dehydroabietic oximes halt pancreatic cancer cell growth in the G1 phase through induction of p27 and downregulation of cyclin D1. Oximes 15-21 cyclin D1 Homo sapiens 120-129 30064081-5 2018 The new zinc-binders, both of the oxime and sulfonamide types, showed a striking selective activity against the target hCA IX over ubiquitous hCA I and II, with diverse inhibitory ranges and ratio differing the two subsets. Oximes 34-39 HCA1 Homo sapiens 119-122 30064081-5 2018 The new zinc-binders, both of the oxime and sulfonamide types, showed a striking selective activity against the target hCA IX over ubiquitous hCA I and II, with diverse inhibitory ranges and ratio differing the two subsets. Oximes 34-39 cytochrome P450 family 24 subfamily A member 1 Homo sapiens 142-154 30122284-1 2018 New oximes short-acting CB1 agonists were explored by the introduction of an internal oxime and polar groups at the C3 alkyl tail of Delta8-THC. Oximes 4-10 cannabinoid receptor 1 Homo sapiens 24-27 30122284-1 2018 New oximes short-acting CB1 agonists were explored by the introduction of an internal oxime and polar groups at the C3 alkyl tail of Delta8-THC. Oximes 4-9 cannabinoid receptor 1 Homo sapiens 24-27 30122284-4 2018 All oxime analogs showed comparable affinity at the CB2 receptor, but surprisingly they were found to function as inverse agonists for CB2. Oximes 4-9 cannabinoid receptor 2 Homo sapiens 52-55 30122284-4 2018 All oxime analogs showed comparable affinity at the CB2 receptor, but surprisingly they were found to function as inverse agonists for CB2. Oximes 4-9 cannabinoid receptor 2 Homo sapiens 135-138 30122284-9 2018 We have selected oxime trans-8a based on its potency for CB1, and favorable pharmacodynamic profile, such as fast onset and predictable duration of pharmacological action, for evaluation in pre-clinical models of anorexia nervosa. Oximes 17-22 cannabinoid receptor 1 Homo sapiens 57-60 30125110-3 2018 A promising reactivator based on tetrahydroacridine linked to a nonquaternary oxime is also an undesired submicromolar reversible inhibitor of AChE. Oximes 78-83 acetylcholinesterase (Cartwright blood group) Homo sapiens 143-147 30056178-6 2018 2-PAM Cl is the U.S. FDA-approved standard-of-care oxime therapy for OP intoxication. Oximes 51-56 peptidyl-glycine alpha-amidating monooxygenase Cavia porcellus 2-5 30167602-4 2018 Here we report a stable Abeta oligomer mimic that is transformed into fibrils by a chemical stimulus, i.e., an oxime exchange reaction. Oximes 111-116 amyloid beta precursor protein Homo sapiens 24-29 30096649-0 2018 Discovery of a potent non-oxime reactivator of nerve agent inhibited human acetylcholinesterase. Oximes 26-31 acetylcholinesterase (Cartwright blood group) Homo sapiens 75-95 30096649-3 2018 The presently fielded oximes reactivate OP-inhibited AChE by liberating the phosphylated serine. Oximes 22-28 acetylcholinesterase (Cartwright blood group) Homo sapiens 53-57 30096649-6 2018 Recently, a number of non-oxime compounds was discovered in which the 4-amino-2-((diethylamino)methyl)phenol (ADOC) motif proved to be able to reactivate OP-inhibited AChE to some extent. Oximes 26-31 acetylcholinesterase (Cartwright blood group) Homo sapiens 167-171 30096649-8 2018 We here disclose that one of those compounds showed a remarkable ability to reactivate OP-inhibited hAChE in vitro and that it is the most potent non-oxime reported to date. Oximes 150-155 acetylcholinesterase (Cartwright blood group) Homo sapiens 100-105 30056178-12 2018 Furthermore, based on those ED50s, the TI trend of the various oximes against both GB and VX was MMB4 DMS > HLo-7 DMS > 2-PAM Cl, while against PHO, MMB4 DMS > 2-PAM Cl > HLo-7 DMS. Oximes 63-69 peptidyl-glycine alpha-amidating monooxygenase Cavia porcellus 128-131 30056178-12 2018 Furthermore, based on those ED50s, the TI trend of the various oximes against both GB and VX was MMB4 DMS > HLo-7 DMS > 2-PAM Cl, while against PHO, MMB4 DMS > 2-PAM Cl > HLo-7 DMS. Oximes 63-69 peptidyl-glycine alpha-amidating monooxygenase Cavia porcellus 171-174 30110162-3 2018 Phosphylation of acetylcholinesterase produces two adducts, an initial neutral adduct that can be reactivated with oxime nucleophiles, and a subsequent monoanionic adduct (called aged acetylcholinesterase) which has proven over two generations to be impervious to reactivation. Oximes 115-120 acetylcholinesterase (Cartwright blood group) Homo sapiens 17-37 28993240-1 2018 Acetylcholinesterase (AChE) inhibited by the organophosphorus nerve (OP) agent soman underlies a spontaneous and extremely rapid dealkylation ("aging") reaction which prevents reactivation by oximes. Oximes 192-198 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-20 28993240-1 2018 Acetylcholinesterase (AChE) inhibited by the organophosphorus nerve (OP) agent soman underlies a spontaneous and extremely rapid dealkylation ("aging") reaction which prevents reactivation by oximes. Oximes 192-198 acetylcholinesterase (Cartwright blood group) Homo sapiens 22-26 28993240-7 2018 In conclusion, the results of the present study indicate a negligible reactivation of soman-inhibited AChE by oximes at conditions simulating the in vivo poisoning by soman. Oximes 110-116 acetylcholinesterase (Cartwright blood group) Homo sapiens 102-106 29129798-1 2018 Post-exposure nerve agent treatment usually includes administration of an oxime, which acts to restore function of the enzyme acetylcholinesterase (AChE). Oximes 74-79 acetylcholinesterase Cavia porcellus 126-146 29129798-1 2018 Post-exposure nerve agent treatment usually includes administration of an oxime, which acts to restore function of the enzyme acetylcholinesterase (AChE). Oximes 74-79 acetylcholinesterase Cavia porcellus 148-152 29129798-4 2018 As such, there is a need to understand the relationship between dose rate, plasma concentration, reactivation of AChE activity and efficacy, to provide supporting evidence for oxime infusions in nerve agent poisoning. Oximes 176-181 acetylcholinesterase Cavia porcellus 113-117 29180286-0 2018 The estimation of oxime efficiency is affected by the experimental design of phosphylated acetylcholinesterase reactivation. Oximes 18-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 90-110 29180286-3 2018 The endeavor of many chemists to find more efficient reactivators resulted in thousands of newly-designed and synthesized oximes-potential reactivators of AChE. Oximes 122-128 acetylcholinesterase (Cartwright blood group) Homo sapiens 155-159 30176331-14 2018 The oxime acts as antidote against physostigmine and pyridostigmine poisoning by reactivating AChE in the brain and diaphragm, respectively. Oximes 4-9 acetylcholinesterase Rattus norvegicus 94-98 29626600-0 2018 Oxime-functionalized cryogel disks for catalase immobilization. Oximes 0-5 catalase Homo sapiens 39-47 29772260-0 2018 Oxime-assisted reactivation of tabun-inhibited acetylcholinesterase analysed by active site mutations. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 47-67 29772260-1 2018 The antidotal property of oximes is attributed to their ability to reactivate acetylcholinesterase (AChE) inhibited by organophosphorus compounds (OP) such as pesticides and nerve warfare agents. Oximes 26-32 acetylcholinesterase (Cartwright blood group) Homo sapiens 78-98 29772260-1 2018 The antidotal property of oximes is attributed to their ability to reactivate acetylcholinesterase (AChE) inhibited by organophosphorus compounds (OP) such as pesticides and nerve warfare agents. Oximes 26-32 acetylcholinesterase (Cartwright blood group) Homo sapiens 100-104 29626600-2 2018 In the current study, catalase immobilization was applied onto the oxime-functionalized cryogel disks. Oximes 67-72 catalase Homo sapiens 22-30 29626600-10 2018 Furthermore, catalase desorption was achieved by 1.0M NaSCN at pH8.0 successfully and catalase adsorption capacity of oxime-functionalized cryogel disk was decreased by 9.9% at the end of 5 adsorption-desorption cycle. Oximes 118-123 catalase Homo sapiens 13-21 29626600-10 2018 Furthermore, catalase desorption was achieved by 1.0M NaSCN at pH8.0 successfully and catalase adsorption capacity of oxime-functionalized cryogel disk was decreased by 9.9% at the end of 5 adsorption-desorption cycle. Oximes 118-123 catalase Homo sapiens 86-94 29614332-3 2018 Treatment for toxicity due to OPC exposure has been largely focused on the reactivation of AChE by oxime-based compounds via direct nucleophilic attack on the phosphorous center. Oximes 99-104 acetylcholinesterase (Cartwright blood group) Homo sapiens 91-95 29980922-0 2018 Influence of gauche effect on uncharged oxime reactivators for the reactivation of tabun-inhibited AChE: quantum chemical and steered molecular dynamics studies. Oximes 40-45 acetylcholinesterase (Cartwright blood group) Homo sapiens 99-103 29980922-1 2018 The neutral oxime reactivator RS194B with a seven-membered ring has shown better efficacy towards the tabun-inhibited AChE than that of RS69N with a six-membered ring and RS41A with a five-membered ring. Oximes 12-17 acetylcholinesterase (Cartwright blood group) Homo sapiens 118-122 28446076-2 2018 Some oximes such HI6 as 2-PAM are nucleophiles that are capable to reactivate inhibited human AChE under some conditions. Oximes 5-11 peptidylglycine alpha-amidating monooxygenase Homo sapiens 26-29 29773682-0 2018 Water structure changes in oxime-mediated reactivation process of phosphorylated human acetylcholinesterase. Oximes 27-32 acetylcholinesterase (Cartwright blood group) Homo sapiens 87-107 29773682-2 2018 To investigate oximate water structure changes in this reaction, reactivation of paraoxon-inhibited human acetylcholinesterase (AChE) was performed by the oxime asoxime (HI-6) at different pH in the presence and absence of lyotropic salts: a neutral salt (NaCl), a strong chaotropic salt (LiSCN) and strong kosmotropic salts (ammonium sulphate and phosphate HPO42-). Oximes 155-160 acetylcholinesterase (Cartwright blood group) Homo sapiens 106-126 29773682-2 2018 To investigate oximate water structure changes in this reaction, reactivation of paraoxon-inhibited human acetylcholinesterase (AChE) was performed by the oxime asoxime (HI-6) at different pH in the presence and absence of lyotropic salts: a neutral salt (NaCl), a strong chaotropic salt (LiSCN) and strong kosmotropic salts (ammonium sulphate and phosphate HPO42-). Oximes 155-160 acetylcholinesterase (Cartwright blood group) Homo sapiens 128-132 29920954-4 2018 This reaction was very selective for the syn-oxime. Oximes 45-50 synemin Homo sapiens 41-44 29735900-4 2018 Three novel oximes (K131, K142, K153) with an oxime group in position four of the pyridinium ring were designed and then tested for their potency to reactivate human (Homo sapiens sapiens) AChE (HssACHE) and BChE (HssBChE) inhibited by the pesticide paraoxon (diethyl 4-nitrophenyl phosphate). Oximes 12-18 acetylcholinesterase (Cartwright blood group) Homo sapiens 189-193 29735900-4 2018 Three novel oximes (K131, K142, K153) with an oxime group in position four of the pyridinium ring were designed and then tested for their potency to reactivate human (Homo sapiens sapiens) AChE (HssACHE) and BChE (HssBChE) inhibited by the pesticide paraoxon (diethyl 4-nitrophenyl phosphate). Oximes 12-18 butyrylcholinesterase Homo sapiens 208-212 29735900-4 2018 Three novel oximes (K131, K142, K153) with an oxime group in position four of the pyridinium ring were designed and then tested for their potency to reactivate human (Homo sapiens sapiens) AChE (HssACHE) and BChE (HssBChE) inhibited by the pesticide paraoxon (diethyl 4-nitrophenyl phosphate). Oximes 12-17 acetylcholinesterase (Cartwright blood group) Homo sapiens 189-193 29735900-4 2018 Three novel oximes (K131, K142, K153) with an oxime group in position four of the pyridinium ring were designed and then tested for their potency to reactivate human (Homo sapiens sapiens) AChE (HssACHE) and BChE (HssBChE) inhibited by the pesticide paraoxon (diethyl 4-nitrophenyl phosphate). Oximes 12-17 butyrylcholinesterase Homo sapiens 208-212 28446076-0 2018 Behavior of uncharged oximes compared to HI6 and 2-PAM in the human AChE-tabun conjugate: a molecular modeling approach. Oximes 22-28 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-72 28446076-2 2018 Some oximes such HI6 as 2-PAM are nucleophiles that are capable to reactivate inhibited human AChE under some conditions. Oximes 5-11 acetylcholinesterase (Cartwright blood group) Homo sapiens 94-98 29548566-2 2018 In this study, an unusual separation situation in comprehensive two dimensional GC where two dimensional interconversion (i.e. a raised plateau in both first and second dimension, 1D and 2D) was observed in analysis of oxime isomers. Oximes 219-224 leiomodin 1 Homo sapiens 180-189 29548566-5 2018 The simulated results were supported by experimental results obtained by a comprehensive heart-cut multidimensional GC (H/C MDGC) approach which was developed to clearly investigate isomerisation of E/Z oxime molecules in both 1D and 2D separations under different isothermal conditions. Oximes 203-208 leiomodin 1 Homo sapiens 227-236 29553731-0 2018 Dynamic Mechanism of a Fluorinated Oxime Reactivator Unbinding from AChE Gorge in Polarizable Water. Oximes 35-40 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-72 29577198-3 2018 Oxime-induced reactivation of acetylcholinesterase was most pronounced in dipyroxime and toxogonin: parameters of the kinetics of reduction of the phosphorylated enzyme differed by more than 2 times from the values received with the use of other reactivators. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 30-50 29719573-0 2018 Synthesis and in vitro biochemical evaluation of oxime bond-linked daunorubicin-GnRH-III conjugates developed for targeted drug delivery. Oximes 49-54 gonadotropin releasing hormone 1 Homo sapiens 80-84 27275644-3 2018 This part is devoted to non-aromatic molecules characterized by a lone pair located on a sp2 nitrogen atom, it embraces functional groups such as imines, amidines, guanidines, diazenes, hydrazines, oximes, and phosphazenes. Oximes 198-204 Sp2 transcription factor Homo sapiens 89-92 29482737-0 2018 Kinetic analysis of oxime-assisted reactivation of human, Guinea pig, and rat acetylcholinesterase inhibited by the organophosphorus pesticide metabolite phorate oxon (PHO). Oximes 20-25 acetylcholinesterase Rattus norvegicus 78-98 28971759-7 2018 RESULTS: Over the last decades the introduction of oxime groups in the steroid scaffold is originating molecules with relevant antitumor activities, as well as steroid sulfatase, aromatase, 17alpha-hydroxylase-17,20-lyase, 5alpha-reductase and 17beta-hydroxysteroid dehydrogenase type 1 inhibitory activities. Oximes 51-56 hydroxysteroid 17-beta dehydrogenase 1 Homo sapiens 244-286 28971759-8 2018 As relevant examples, pregnenolone 20-oximes showed high activity as 17alpha-hydroxylase-17,20-lyase and 5alpha-reductase inhibitors and the introduction of an oxime group at C-6 in androstane series also led to relevant results as aromatase inhibitors. Oximes 38-43 complement C6 Homo sapiens 175-178 29098328-2 2018 On the other hand, according to our best knowledge, possible antioxidant properties of oximes, the only causal antidotes to OP-inhibited AChE, have been examined only by a few studies. Oximes 87-93 acetylcholinesterase Rattus norvegicus 137-141 28812076-2 2017 The combination of [WZn3(H2O)2(ZnW9O34)2]12- and Co(ii) provides a synergistical catalytic way to promote oximation of aldehyde/ketone with in situ generated hydroxylamine that initially produces an oxime, which further either dehydrates into a nitrile or undergoes a Beckmann rearrangement to form an amide. Oximes 199-204 mitochondrially encoded cytochrome c oxidase II Homo sapiens 49-55 29216560-7 2018 Taken together, these efforts culminated in the discovery of oxime 2a as a potential SGLT2 inhibitor. Oximes 61-66 solute carrier family 5 member 2 Homo sapiens 85-90 29218520-4 2018 This process started with the identification of a focused series of oxime derivatives, originally designed as estrogen receptor (ER) ligands, which were structurally optimized in order to direct their activity towards GLUT1 and to minimize their binding to the ERs, leading to the production of efficient and selective inhibitors of glucose uptake in cancer cells. Oximes 68-73 estrogen receptor 1 Homo sapiens 110-127 29218520-4 2018 This process started with the identification of a focused series of oxime derivatives, originally designed as estrogen receptor (ER) ligands, which were structurally optimized in order to direct their activity towards GLUT1 and to minimize their binding to the ERs, leading to the production of efficient and selective inhibitors of glucose uptake in cancer cells. Oximes 68-73 estrogen receptor 1 Homo sapiens 129-131 29218520-4 2018 This process started with the identification of a focused series of oxime derivatives, originally designed as estrogen receptor (ER) ligands, which were structurally optimized in order to direct their activity towards GLUT1 and to minimize their binding to the ERs, leading to the production of efficient and selective inhibitors of glucose uptake in cancer cells. Oximes 68-73 solute carrier family 2 member 1 Homo sapiens 218-223 28722512-5 2018 In silico the molecular interactions between AChE and oximes were examined and binding energies were assessed. Oximes 54-60 acetylcholinesterase (Cartwright blood group) Homo sapiens 45-49 28722512-7 2018 In vitro the intrinsic ability of the oximes to inhibit AChE (IC50) and their reactivation potency (R50) when used in paraoxon inhibited human RBC-AChE was determined. Oximes 38-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 56-60 29091431-1 2017 Recently, a new class of reactivators of chemical warfare agent inhibited acetylcholinesterase (AChE) with promising in vitro potential was developed by the covalent linkage of an oxime nucleophile and a peripheral site ligand. Oximes 180-185 acetylcholinesterase Rattus norvegicus 74-94 29091431-1 2017 Recently, a new class of reactivators of chemical warfare agent inhibited acetylcholinesterase (AChE) with promising in vitro potential was developed by the covalent linkage of an oxime nucleophile and a peripheral site ligand. Oximes 180-185 acetylcholinesterase Rattus norvegicus 96-100 31723659-4 2017 Additionally, acetylcholinesterase aging, which is the loss of an alkyl side chain that prevents reactivation by oximes, is very rapid so that the effective reactivation by oximes is thwarted. Oximes 113-119 acetylcholinesterase (Cartwright blood group) Homo sapiens 14-34 31723659-4 2017 Additionally, acetylcholinesterase aging, which is the loss of an alkyl side chain that prevents reactivation by oximes, is very rapid so that the effective reactivation by oximes is thwarted. Oximes 173-179 acetylcholinesterase (Cartwright blood group) Homo sapiens 14-34 28738249-0 2017 New 1,3,4-oxadiazole/oxime hybrids: Design, synthesis, anti-inflammatory, COX inhibitory activities and ulcerogenic liability. Oximes 21-26 cytochrome c oxidase subunit 8A Homo sapiens 74-77 28738249-1 2017 A series of new 1,3,4-oxadiazole/oxime hybrids were synthesized and designed as potent COX inhibitors. Oximes 33-38 cytochrome c oxidase subunit 8A Homo sapiens 87-90 29291440-7 2018 Oxime and particularly oxime ether formation strongly increased their inhibitory activity on the efflux of rhodamine 123 by P-glycoprotein (P-gp), while the new ecdysteroid lactam did not interfere with the efflux function. Oximes 0-5 ATP binding cassette subfamily B member 1 Homo sapiens 124-138 29291440-7 2018 Oxime and particularly oxime ether formation strongly increased their inhibitory activity on the efflux of rhodamine 123 by P-glycoprotein (P-gp), while the new ecdysteroid lactam did not interfere with the efflux function. Oximes 0-5 ATP binding cassette subfamily B member 1 Homo sapiens 140-144 29291440-7 2018 Oxime and particularly oxime ether formation strongly increased their inhibitory activity on the efflux of rhodamine 123 by P-glycoprotein (P-gp), while the new ecdysteroid lactam did not interfere with the efflux function. Oximes 23-28 ATP binding cassette subfamily B member 1 Homo sapiens 124-138 29291440-7 2018 Oxime and particularly oxime ether formation strongly increased their inhibitory activity on the efflux of rhodamine 123 by P-glycoprotein (P-gp), while the new ecdysteroid lactam did not interfere with the efflux function. Oximes 23-28 ATP binding cassette subfamily B member 1 Homo sapiens 140-144 28722512-7 2018 In vitro the intrinsic ability of the oximes to inhibit AChE (IC50) and their reactivation potency (R50) when used in paraoxon inhibited human RBC-AChE was determined. Oximes 38-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 147-151 29046224-0 2017 Reprint of: Impact of the corrin framework of vitamin B12 on the electrochemical carbon-skeleton rearrangement in comparison to an imine/oxime planar ligand; tuning selectivity in 1,2-migration of a functional group by controlling electrolysis potential. Oximes 137-142 NADH:ubiquinone oxidoreductase subunit B3 Homo sapiens 54-57 28639122-7 2017 RESULTS: F-18-labeled PSMA inhibitors were synthesized in 32-69 % radiochemical yields using (1) acylation reaction at the primary amino group of the lysine residue with [18F]SFB and (2) oxime formation with 4-[18F]fluorobenzaldehyde and [18F]FDG using the respective aminooxy-functionalized lysine residue. Oximes 187-192 folate hydrolase 1 Homo sapiens 22-26 28440951-8 2017 5- or 5"-Bromo- or phenyl-substituted (but not in combination) inhibitors, having a H-bonded oxime weakly acidic group of a small volume, are optimal candidates for binding hGSTM1-1. Oximes 93-98 glutathione S-transferase mu 1 Homo sapiens 173-181 28795808-3 2017 In this paper, we describe how the unique features of SNO-OCTs can be employed to modify an oxime-bearing styrene copolymer and introduce an array of polar functionalities into the polymer. Oximes 92-97 strawberry notch homolog 1 Homo sapiens 54-57 28542985-6 2017 Oximes poorly reactivate AChE inhibited by phosphoramidates. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 25-29 28805227-5 2017 The resonance effect dominates the electronic effects on the BDEs of oximes, and electron-donating conjugation increases the BDE. Oximes 69-75 homeobox D13 Homo sapiens 61-64 28646405-0 2017 Revealing the importance of linkers in K-series oxime reactivators for tabun-inhibited AChE using quantum chemical, docking and SMD studies. Oximes 48-53 acetylcholinesterase (Cartwright blood group) Homo sapiens 87-91 28693885-4 2017 The present study utilized a macaque (Ma) model to demonstrate the efficacy of a novel zwitterionic and centrally acting oxime RS194B to reactivate sarin- and paraoxon-inhibited macaque AChE and butyrylcholinesterase (BChE) in vitro and to further assess the capacity of RS194B to effect a reversal of clinical symptoms following sarin inhalation in vivo. Oximes 121-126 butyrylcholinesterase Homo sapiens 195-216 28693885-4 2017 The present study utilized a macaque (Ma) model to demonstrate the efficacy of a novel zwitterionic and centrally acting oxime RS194B to reactivate sarin- and paraoxon-inhibited macaque AChE and butyrylcholinesterase (BChE) in vitro and to further assess the capacity of RS194B to effect a reversal of clinical symptoms following sarin inhalation in vivo. Oximes 121-126 butyrylcholinesterase Homo sapiens 218-222 29062551-2 2017 Oximes, especially pralidoxime (2-PAM), are widely used as antidotes to treat OP poisoning. Oximes 0-6 peptidylglycine alpha-amidating monooxygenase Homo sapiens 34-37 28474886-5 2017 "Click SAgA" (cSAgAPLP:LABL) uses hydrolytically stable covalent conjugation chemistry (Copper-catalyzed Azide-Alkyne Cycloaddition (CuAAC)) rather than a hydrolyzable oxime bond to attach PLP and LABL to HA. Oximes 168-173 proteolipid protein 1 Homo sapiens 19-22 28696367-3 2017 The reactivating efficacy of a newly developed oxime K305 is lower compared to the reactivating efficacy of the oxime K203 and trimedoxime while the ability of the oxime K307 to reactivate tabun-inhibited acetylcholinesterase (AChE) in the brain roughly corresponds to the reactivating efficacy of the oxime K203 and it is slightly lower compared to trimedoxime. Oximes 47-52 acetylcholinesterase Rattus norvegicus 205-225 28696367-3 2017 The reactivating efficacy of a newly developed oxime K305 is lower compared to the reactivating efficacy of the oxime K203 and trimedoxime while the ability of the oxime K307 to reactivate tabun-inhibited acetylcholinesterase (AChE) in the brain roughly corresponds to the reactivating efficacy of the oxime K203 and it is slightly lower compared to trimedoxime. Oximes 47-52 acetylcholinesterase Rattus norvegicus 227-231 29201079-0 2017 Docking Studies, Synthesis, and In-vitro Evaluation of Novel Oximes Based on Nitrones as Reactivators of Inhibited Acetylcholinesterase. Oximes 61-67 acetylcholinesterase (Cartwright blood group) Homo sapiens 115-135 28737687-4 2017 As the results showed, the tested oximes were more efficient in the reactivation of BChE and they reactivated enzyme activity to up to 70% with reactivation rates similar to known pyridinium oximes used as antidotes in medical practice today. Oximes 34-40 butyrylcholinesterase Homo sapiens 84-88 28737687-5 2017 Furthermore, the oximes showed selectivity towards binding to the BChE active site and the determined enzyme-oxime dissociation constants supported work on the future development of inhibitors in other targeted studies (e.g., in treatment of neurodegenerative disease). Oximes 17-23 butyrylcholinesterase Homo sapiens 66-70 28737687-5 2017 Furthermore, the oximes showed selectivity towards binding to the BChE active site and the determined enzyme-oxime dissociation constants supported work on the future development of inhibitors in other targeted studies (e.g., in treatment of neurodegenerative disease). Oximes 17-22 butyrylcholinesterase Homo sapiens 66-70 28696367-1 2017 The ability of two newly developed oximes (K305, K307) to protect tabun-poisoned rats from tabun-induced inhibition of brain acetylcholinesterase, acute neurotoxic signs and symptoms and brain damage was compared with that of the oxime K203 and trimedoxime. Oximes 35-41 acetylcholinesterase Rattus norvegicus 125-145 28696367-1 2017 The ability of two newly developed oximes (K305, K307) to protect tabun-poisoned rats from tabun-induced inhibition of brain acetylcholinesterase, acute neurotoxic signs and symptoms and brain damage was compared with that of the oxime K203 and trimedoxime. Oximes 35-40 acetylcholinesterase Rattus norvegicus 125-145 27358236-2 2017 One current approach is directed toward synthesizing oximes with high affinity and reactivatability toward butyrylcholinesterase (BChE) in plasma to generate an effective pseudocatalytic scavenger. Oximes 53-59 butyrylcholinesterase Homo sapiens 107-128 28412361-5 2017 INCB14943 binds to heme iron in IDO1 protein through the oxime nitrogen. Oximes 57-62 indoleamine 2,3-dioxygenase 1 Homo sapiens 32-36 28412361-7 2017 Comparing with the other reported inhibitors, the oxime nitrogen and halogen bond interaction are identified as the unique features of INCB14943 among the IDO1 inhibitors. Oximes 50-55 indoleamine 2,3-dioxygenase 1 Homo sapiens 155-159 27125569-1 2017 Butyryl cholinesterase (BChE) has been seen as a key enzyme in the search for new strategies in the treatment of poisoning by organophosphates (OPs), since human BChE (HssBChE), complexed with the appropriate oxime, can be a suitable scavenger and deactivator for OPs in the blood stream. Oximes 209-214 butyrylcholinesterase Homo sapiens 0-22 27125569-1 2017 Butyryl cholinesterase (BChE) has been seen as a key enzyme in the search for new strategies in the treatment of poisoning by organophosphates (OPs), since human BChE (HssBChE), complexed with the appropriate oxime, can be a suitable scavenger and deactivator for OPs in the blood stream. Oximes 209-214 butyrylcholinesterase Homo sapiens 24-28 27125569-1 2017 Butyryl cholinesterase (BChE) has been seen as a key enzyme in the search for new strategies in the treatment of poisoning by organophosphates (OPs), since human BChE (HssBChE), complexed with the appropriate oxime, can be a suitable scavenger and deactivator for OPs in the blood stream. Oximes 209-214 butyrylcholinesterase Homo sapiens 162-166 27125569-0 2017 Mechanistic studies of new oximes reactivators of human butyryl cholinesterase inhibited by cyclosarin and sarin. Oximes 27-33 butyrylcholinesterase Homo sapiens 56-78 28097769-6 2017 The location of this oxime with the PLP, which forms in place of the native internal aldimine linkage of PLP of the native KAT-I, is away from the position of the native internal aldimine, with the free Lys247 substantially retaining the orientation of the native structure. Oximes 21-26 pyridoxal phosphatase Homo sapiens 36-39 28097769-6 2017 The location of this oxime with the PLP, which forms in place of the native internal aldimine linkage of PLP of the native KAT-I, is away from the position of the native internal aldimine, with the free Lys247 substantially retaining the orientation of the native structure. Oximes 21-26 pyridoxal phosphatase Homo sapiens 105-108 28097769-6 2017 The location of this oxime with the PLP, which forms in place of the native internal aldimine linkage of PLP of the native KAT-I, is away from the position of the native internal aldimine, with the free Lys247 substantially retaining the orientation of the native structure. Oximes 21-26 kynurenine aminotransferase 1 Homo sapiens 123-128 31294152-5 2017 Oximes are compounds that reactivate Acetylcholinesterase (AChE), a regulatory enzyme responsible for the transmission of nerve impulses, which is one of the molecular targets most vulnerable to neurotoxic agents. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 37-57 31294152-5 2017 Oximes are compounds that reactivate Acetylcholinesterase (AChE), a regulatory enzyme responsible for the transmission of nerve impulses, which is one of the molecular targets most vulnerable to neurotoxic agents. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 59-63 27358236-2 2017 One current approach is directed toward synthesizing oximes with high affinity and reactivatability toward butyrylcholinesterase (BChE) in plasma to generate an effective pseudocatalytic scavenger. Oximes 53-59 butyrylcholinesterase Homo sapiens 130-134 27358236-3 2017 An interim solution could be the administration of external AChE or BChE from blood products to augment pseudocatalytic scavenging with slower but clinically approved oximes to decrease nerve agent concentrations in the body. Oximes 167-173 acetylcholinesterase (Cartwright blood group) Homo sapiens 60-64 27358236-3 2017 An interim solution could be the administration of external AChE or BChE from blood products to augment pseudocatalytic scavenging with slower but clinically approved oximes to decrease nerve agent concentrations in the body. Oximes 167-173 butyrylcholinesterase Homo sapiens 68-72 28165084-0 2017 Unbinding of fluorinated oxime drug from the AChE gorge in polarizable water: a well-tempered metadynamics study. Oximes 25-30 acetylcholinesterase (Cartwright blood group) Homo sapiens 45-49 28119957-2 2017 The resulting Ni/ACOX catalyst is highly active and chemoselective for hydrogenation of nitroarenes to produce functionalized anilines and oximes. Oximes 139-145 acyl-CoA oxidase 1 Homo sapiens 17-21 27908452-9 2017 This study concludes that NO3- formation during ozonation of DON is induced by an oxygen-transfer to nitrogen forming hydroxylamine and oxime, while NH4+ formation is induced by electron-transfer reactions involving C-centered radicals and imine intermediates. Oximes 136-141 NBL1, DAN family BMP antagonist Homo sapiens 26-29 28124920-0 2017 Biomimetic Synthesis of Insulin Enabled by Oxime Ligation and Traceless "C-Peptide" Chemical Excision. Oximes 43-48 insulin Homo sapiens 24-31 26612005-0 2016 Docking and molecular dynamics studies of peripheral site ligand-oximes as reactivators of sarin-inhibited human acetylcholinesterase. Oximes 65-71 acetylcholinesterase (Cartwright blood group) Homo sapiens 113-133 28596833-7 2017 The oxime M41 accounted for only 0.62% of the total plasma radioactivity and was detected only at early time points. Oximes 4-9 DSCAM antisense RNA 1 Homo sapiens 10-13 27582056-9 2016 Among further modifications of known oximes, the main attention has been paid to dual binding site ligands of AChE as the current mainstream strategy. Oximes 37-43 acetylcholinesterase (Cartwright blood group) Homo sapiens 110-114 26612005-1 2016 In the present work, we performed docking and molecular dynamics simulations studies on two groups of long-tailored oximes designed as peripheral site binders of acetylcholinesterase (AChE) and potential penetrators on the blood brain barrier. Oximes 116-122 acetylcholinesterase (Cartwright blood group) Homo sapiens 184-188 26612005-1 2016 In the present work, we performed docking and molecular dynamics simulations studies on two groups of long-tailored oximes designed as peripheral site binders of acetylcholinesterase (AChE) and potential penetrators on the blood brain barrier. Oximes 116-122 acetylcholinesterase (Cartwright blood group) Homo sapiens 162-182 26899146-13 2016 In particular, association of cholinesterase mutants (not susceptible to age after phosphylation) with fast-reactivating oximes leads to pseudocatalytic bioscavengers. Oximes 121-127 butyrylcholinesterase Homo sapiens 30-44 27062893-0 2016 Probing the activity of a non-oxime reactivator for acetylcholinesterase inhibited by organophosphorus nerve agents. Oximes 30-35 acetylcholinesterase (Cartwright blood group) Homo sapiens 52-72 27062893-2 2016 2PAM reactivates nerve agent-inhibited AChE via direct nucleophilic attack by the oxime moiety on the phosphorus center of the bound nerve agent. Oximes 82-87 acetylcholinesterase (Cartwright blood group) Homo sapiens 39-43 27125761-2 2016 The need for an effective treatment of OP poisoning resulted in the implementation of a combination therapy with the muscarinic receptor antagonist atropine and an oxime for the reactivation of OP-inhibited acetylcholinesterase (AChE). Oximes 164-169 acetylcholinesterase (Cartwright blood group) Homo sapiens 229-233 27125761-6 2016 Multiple in vitro and in vivo studies investigated the potential of oximes to reactivate OP-inhibited AChE and to reverse OP-induced cholinergic signs. Oximes 68-74 acetylcholinesterase (Cartwright blood group) Homo sapiens 102-106 27129421-1 2016 The antidotal treatment of organophosphates (OP) nerve agents (NA) poisoning is based on anticholinergics (e.g. atropine) combined with oxime reactivators (e.g. 2PAM) of acetylcholinesterase (AChE). Oximes 136-141 acetylcholinesterase Rattus norvegicus 170-190 27238725-1 2016 Within this study, we designed and synthesized four new oxime compounds of the N-substituted 2-hydroxyiminoacetamide structure and evaluated their interactions with acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Oximes 56-61 acetylcholinesterase (Cartwright blood group) Homo sapiens 165-185 27238725-1 2016 Within this study, we designed and synthesized four new oxime compounds of the N-substituted 2-hydroxyiminoacetamide structure and evaluated their interactions with acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Oximes 56-61 acetylcholinesterase (Cartwright blood group) Homo sapiens 187-191 27238725-1 2016 Within this study, we designed and synthesized four new oxime compounds of the N-substituted 2-hydroxyiminoacetamide structure and evaluated their interactions with acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Oximes 56-61 butyrylcholinesterase Homo sapiens 197-218 27238725-1 2016 Within this study, we designed and synthesized four new oxime compounds of the N-substituted 2-hydroxyiminoacetamide structure and evaluated their interactions with acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Oximes 56-61 butyrylcholinesterase Homo sapiens 220-224 27387540-5 2016 A number of these novel oximes have shown the ability to decrease the level of ChE inhibition in the brains of rats treated with a high sublethal dosage of either a sarin surrogate (nitrophenyl isopropyl methylphosphonate, NIMP) or the VX surrogate NEMP. Oximes 24-30 butyrylcholinesterase Rattus norvegicus 79-82 27387540-8 2016 Therefore these novel oximes have demonstrated an ability to reactivate inhibited ChE in brain preparations from two species and in vivo data support their ability to enter the brain and provide a therapeutic action. Oximes 22-28 butyrylcholinesterase Rattus norvegicus 82-85 27785869-5 2016 To address this issue, we report the synthesis of a covalent RANTES-PF4 heterodimer (termed OPRAH) by total chemical synthesis and oxime ligation, with an acceleration of the final ligation step driven by PPIs between RANTES and PF4. Oximes 131-136 C-C motif chemokine ligand 5 Homo sapiens 61-67 27785869-5 2016 To address this issue, we report the synthesis of a covalent RANTES-PF4 heterodimer (termed OPRAH) by total chemical synthesis and oxime ligation, with an acceleration of the final ligation step driven by PPIs between RANTES and PF4. Oximes 131-136 platelet factor 4 Homo sapiens 68-71 27693733-5 2016 As the results have shown, the tested oximes were in general more efficient in the reactivation of OP-inhibited BChE than AChE. Oximes 38-44 butyrylcholinesterase Homo sapiens 112-116 27693733-7 2016 The cholinesterases displayed a binding affinity for these derivatives in a mumolar range no matter the substituent on their rings which was in accordance with the molecular modelling results showing a similar binding pattern for all oximes within the active site of both AChE and BChE. Oximes 234-240 acetylcholinesterase (Cartwright blood group) Homo sapiens 272-276 27693733-7 2016 The cholinesterases displayed a binding affinity for these derivatives in a mumolar range no matter the substituent on their rings which was in accordance with the molecular modelling results showing a similar binding pattern for all oximes within the active site of both AChE and BChE. Oximes 234-240 butyrylcholinesterase Homo sapiens 281-285 27581755-0 2016 Discovery of Chromeno[4,3-c]pyrazol-4(2H)-one Containing Carbonyl or Oxime Derivatives as Potential, Selective Inhibitors PI3Kalpha. Oximes 69-74 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha Homo sapiens 122-131 27371941-2 2016 Catalytically inactive OP-AChE conjugates formed between the active-center serine and phosphorus of OPs can, in principle, be reactivated by nucleophilic oxime antidotes. Oximes 154-159 acetylcholinesterase (Cartwright blood group) Homo sapiens 26-30 27654152-0 2016 A comprehensive evaluation of novel oximes in creation of butyrylcholinesterase-based nerve agent bioscavengers. Oximes 36-42 butyrylcholinesterase Homo sapiens 58-79 27654152-2 2016 An additional improvement in medical countermeasures would be to use oximes that could reactivate BChE as well to upgrade bioscavenging from stoichiometric to oxime-assisted catalytic. Oximes 69-75 butyrylcholinesterase Homo sapiens 98-102 27654152-2 2016 An additional improvement in medical countermeasures would be to use oximes that could reactivate BChE as well to upgrade bioscavenging from stoichiometric to oxime-assisted catalytic. Oximes 69-74 butyrylcholinesterase Homo sapiens 98-102 27654152-5 2016 A comprehensive analysis was performed for the most promising oximes defining kinetic parameters of reactivation as well as interactions with uninhibited BChE. Oximes 62-68 butyrylcholinesterase Homo sapiens 154-158 27654152-9 2016 The obtained protection in VX poisoning outlines its potential in development oxime-assisted OP-bioscavenging with BChE. Oximes 78-83 butyrylcholinesterase Homo sapiens 115-119 27624074-0 2016 Application of oxime-diversification to optimize ligand interactions within a cryptic pocket of the polo-like kinase 1 polo-box domain. Oximes 15-20 polo like kinase 1 Homo sapiens 100-118 27494215-0 2016 Biological Testing of Organophosphorus-Inactivated Acetylcholinesterase Oxime Reactivators Identified via Virtual Screening. Oximes 72-77 acetylcholinesterase (Cartwright blood group) Homo sapiens 51-71 27494215-4 2016 In order to find new starting points for the development of oxime-containing therapeutic reactivators and to increase our base of knowledge, we have employed a combination of computational and experimental procedures to identify additional compounds with the real or potential ability to reactivate AChE while augmenting and complementing current knowledge. Oximes 60-65 acetylcholinesterase (Cartwright blood group) Homo sapiens 299-303 27460171-4 2016 Molecular docking and dynamics simulation revealed that (i) hydrogen atom of the oxime group interacts with Asp99 of HDAC1 through a water bridged hydrogen bond and (ii) a hydroxyl group is optimal attached on the para-position of benzene, interacting with Glu203 at the entrance to the active site tunnel. Oximes 81-86 histone deacetylase 1 Homo sapiens 117-122 28327676-9 2016 Oximes reactivate cholinesterase enzymes and help to overcome even the nicotinic effects of OP poisoning. Oximes 0-6 butyrylcholinesterase Homo sapiens 18-32 27191504-4 2016 We have solved structures of human acetylcholinesterase in different states in complex with the organophosphate insecticide, paraoxon, and oximes. Oximes 139-145 acetylcholinesterase (Cartwright blood group) Homo sapiens 35-55 27191504-8 2016 Ternary structures of paraoxon-inhibited human acetylcholinesterase in complex with the oximes HI6 and 2-PAM reveals relatively poor positioning for reactivation. Oximes 88-94 acetylcholinesterase (Cartwright blood group) Homo sapiens 47-67 27212630-4 2016 Modification of C-6 of 11-nortetrodotoxin-6,6-diol to form an oxime derivative decreased the activity to 1/22. Oximes 62-67 complement component 6 Mus musculus 16-19 27450532-6 2016 In comparison to 2-PAM and obidoxime, oxime 4a and 4b exhibited enhanced reactivation efficacy toward sarin inhibited hAChE while oxime 4c showed far greater reactivation efficacy toward VX inhibited hAChE. Oximes 38-43 acetylcholinesterase (Cartwright blood group) Homo sapiens 118-123 27371941-3 2016 Antidote efficacy is limited by the structural diversity of OP-AChE conjugates resulting from differences in the structure of the conjugated OP, the different active-center volumes they occupy when conjugated to the active-center serine of AChE, and the distinct chemical characteristics of both OPs and oximes documented in numerous X-ray structures of OP-conjugated AChEs. Oximes 304-310 acetylcholinesterase (Cartwright blood group) Homo sapiens 63-67 27371941-4 2016 Efforts to improve oxime reactivation efficacy by AChE structure-based enhancement of oxime structure have yielded only limited success. Oximes 19-24 acetylcholinesterase (Cartwright blood group) Homo sapiens 50-54 27371941-4 2016 Efforts to improve oxime reactivation efficacy by AChE structure-based enhancement of oxime structure have yielded only limited success. Oximes 86-91 acetylcholinesterase (Cartwright blood group) Homo sapiens 50-54 27371941-5 2016 We outline here the potential limitations of available AChE X-ray structures that preclude an accurate prediction of oxime structures, which are necessary for association in the OP-AChE gorge and nucleophilic attack of the OP-conjugated phosphorus. Oximes 117-122 acetylcholinesterase (Cartwright blood group) Homo sapiens 55-59 27371941-5 2016 We outline here the potential limitations of available AChE X-ray structures that preclude an accurate prediction of oxime structures, which are necessary for association in the OP-AChE gorge and nucleophilic attack of the OP-conjugated phosphorus. Oximes 117-122 acetylcholinesterase (Cartwright blood group) Homo sapiens 181-185 27177985-0 2016 Therapeutic and reactivating efficacy of oximes K027 and K203 against a direct acetylcholinesterase inhibitor. Oximes 41-47 acetylcholinesterase Rattus norvegicus 79-99 27396356-1 2016 BACKGROUND: Current therapies for organophosphate poisoning involve administration of oximes, such as pralidoxime (2-PAM), that reactivate the enzyme acetylcholinesterase. Oximes 86-92 peptidylglycine alpha-amidating monooxygenase Canis lupus familiaris 117-120 27396356-1 2016 BACKGROUND: Current therapies for organophosphate poisoning involve administration of oximes, such as pralidoxime (2-PAM), that reactivate the enzyme acetylcholinesterase. Oximes 86-92 acetylcholinesterase Canis lupus familiaris 150-170 27177985-1 2016 As oxime-based structures are the only causal antidotes to organophosphate (OP)-inhibited acetylcholinesterase (AChE), the majority of studies on these have been directed towards their synthesis and testing. Oximes 3-8 acetylcholinesterase Rattus norvegicus 90-110 27177985-1 2016 As oxime-based structures are the only causal antidotes to organophosphate (OP)-inhibited acetylcholinesterase (AChE), the majority of studies on these have been directed towards their synthesis and testing. Oximes 3-8 acetylcholinesterase Rattus norvegicus 112-116 27131125-5 2016 While both periodate oxidation and aniline-catalyzed oxime ligation (PAL) and galactose oxidase and aniline-catalyzed oxime ligation (GAL) can be used to monitor neuraminidase activity toward glycans in microtiter plates, only GAL accurately measured neuraminidase activity toward glycans displayed on a commercial glass slide microarray. Oximes 118-123 neuraminidase 1 Homo sapiens 162-175 26930003-3 2016 SZV-1287 is a new 3-(4,5-diphenyl-1,3-oxazol-2-yl)propanal oxime SSAO inhibitor, its chemical structure is similar to other oxime derivatives described as TRPA1 antagonists. Oximes 59-64 amine oxidase, copper containing 3 Rattus norvegicus 65-69 27371941-0 2016 Limitations in current acetylcholinesterase structure-based design of oxime antidotes for organophosphate poisoning. Oximes 70-75 acetylcholinesterase (Cartwright blood group) Homo sapiens 23-43 26930003-10 2016 This is the first evidence that our novel oxime compound SZV-1287 originally developed as a SSAO inhibitor has a potent dual antagonistic action on TRPA1 and TRPV1 ion channels on primary sensory neurons. Oximes 42-47 amine oxidase, copper containing 3 Rattus norvegicus 92-96 26930003-10 2016 This is the first evidence that our novel oxime compound SZV-1287 originally developed as a SSAO inhibitor has a potent dual antagonistic action on TRPA1 and TRPV1 ion channels on primary sensory neurons. Oximes 42-47 transient receptor potential cation channel, subfamily A, member 1 Rattus norvegicus 148-153 26930003-10 2016 This is the first evidence that our novel oxime compound SZV-1287 originally developed as a SSAO inhibitor has a potent dual antagonistic action on TRPA1 and TRPV1 ion channels on primary sensory neurons. Oximes 42-47 transient receptor potential cation channel, subfamily V, member 1 Rattus norvegicus 158-163 27327269-6 2016 For postaging treatment, realkylation of aged AChE by appropriate alkylators may pave the way for oxime treatment by neutralizing the oxyanion at the active site of aged AChE. Oximes 98-103 acetylcholinesterase (Cartwright blood group) Homo sapiens 46-50 27327269-6 2016 For postaging treatment, realkylation of aged AChE by appropriate alkylators may pave the way for oxime treatment by neutralizing the oxyanion at the active site of aged AChE. Oximes 98-103 acetylcholinesterase (Cartwright blood group) Homo sapiens 170-174 27153507-0 2016 Novel brain-penetrating oximes for reactivation of cholinesterase inhibited by sarin and VX surrogates. Oximes 24-30 butyrylcholinesterase Rattus norvegicus 51-65 26879641-2 2016 We have examined the structural features of the tabun-conjugated AChE complex with an oxime reactivator, Ortho-7, to provide a strategy for designing new and efficient reactivators. Oximes 86-91 acetylcholinesterase (Cartwright blood group) Homo sapiens 65-69 27153507-1 2016 Current oxime reactivators for organophosphate-inhibited cholinesterase (ChE) do not effectively cross the blood-brain barrier and therefore cannot restore brain ChE activity in vivo. Oximes 8-13 butyrylcholinesterase Rattus norvegicus 57-71 27153507-1 2016 Current oxime reactivators for organophosphate-inhibited cholinesterase (ChE) do not effectively cross the blood-brain barrier and therefore cannot restore brain ChE activity in vivo. Oximes 8-13 butyrylcholinesterase Rattus norvegicus 73-76 27153507-4 2016 In addition, treatment of rats with these novel oximes is associated with attenuation of seizure-like behavior compared to rats treated with 2-PAM, providing additional evidence that the oximes penetrate the blood-brain barrier. Oximes 187-193 peptidylglycine alpha-amidating monooxygenase Rattus norvegicus 143-146 27101948-0 2016 Oxime-mediated in vitro reactivation kinetic analysis of organophosphates-inhibited human and electric eel acetylcholinesterase. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 107-127 27101948-9 2016 Studies stipulated that butene-linked oximes consisting of different functional moieties are good reactivators and found to have better efficacy to reactivate nerve agent-inhibited human AChE in comparison to eel AChE. Oximes 38-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 187-191 27101948-9 2016 Studies stipulated that butene-linked oximes consisting of different functional moieties are good reactivators and found to have better efficacy to reactivate nerve agent-inhibited human AChE in comparison to eel AChE. Oximes 38-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 213-217 27042207-6 2016 Several oximes are found to be hyperglycemic, anti-neoplastic, anti-inflammatory, anti-leishmanial and VEGFR-2 kinase inhibitors. Oximes 8-14 kinase insert domain receptor Homo sapiens 103-110 27010345-6 2016 Oxime analog 7o displayed the most potent EGFR TK inhibitory activity with an IC50 of 0.07 muM, which was analogous to the positive control. Oximes 0-5 epidermal growth factor receptor Homo sapiens 42-46 27000635-2 2016 The main treatment for organophosphorus (OP) compound poisoning in clinics is to restore the activity of acetylcholinesterase (AChE) through oxime-induced reactivation of the phosphorylated OP-AChE adduct. Oximes 141-146 acetylcholinesterase (Cartwright blood group) Homo sapiens 105-125 27000635-2 2016 The main treatment for organophosphorus (OP) compound poisoning in clinics is to restore the activity of acetylcholinesterase (AChE) through oxime-induced reactivation of the phosphorylated OP-AChE adduct. Oximes 141-146 acetylcholinesterase (Cartwright blood group) Homo sapiens 127-131 27000635-2 2016 The main treatment for organophosphorus (OP) compound poisoning in clinics is to restore the activity of acetylcholinesterase (AChE) through oxime-induced reactivation of the phosphorylated OP-AChE adduct. Oximes 141-146 acetylcholinesterase (Cartwright blood group) Homo sapiens 193-197 26809136-4 2016 The ortho-hydroxylbenzaldoximes were chosen as reactivation ligands of AChE to prevent the secondary poisoning of AChE, and simple aromatic groups were used as peripheral site ligands of AChE, which were linked to the oximes in a similar way as that found in the reactivator HI-6. Oximes 25-31 acetylcholinesterase (Cartwright blood group) Homo sapiens 71-75 26851641-1 2016 Standard therapy of poisoning by organophosphorus compounds (OP) is a combined administration of an anti-muscarinic drug (e.g. atropine) and an oxime as reactivator of inhibited acetylcholinesterase (AChE). Oximes 144-149 acetylcholinesterase (Cartwright blood group) Homo sapiens 178-198 26851641-1 2016 Standard therapy of poisoning by organophosphorus compounds (OP) is a combined administration of an anti-muscarinic drug (e.g. atropine) and an oxime as reactivator of inhibited acetylcholinesterase (AChE). Oximes 144-149 acetylcholinesterase (Cartwright blood group) Homo sapiens 200-204 27153754-0 2016 Reactivation of nerve agent-inhibited human acetylcholinesterase by obidoxime, HI-6 and obidoxime+HI-6: Kinetic in vitro study with simulated nerve agent toxicokinetics and oxime pharmacokinetics. Oximes 72-77 acetylcholinesterase (Cartwright blood group) Homo sapiens 44-64 27153754-3 2016 To investigate the ability of obidoxime, HI-6 and the combination of both oximes to reactivate inhibited human AChE in the presence of sarin, cyclosarin or tabun we adopted a dynamic in vitro model with real-time and continuous determination of AChE activity to simulate inhalation nerve agent exposure and intramuscular oxime administration. Oximes 74-80 acetylcholinesterase (Cartwright blood group) Homo sapiens 111-115 27153754-5 2016 The oxime-induced reactivation of inhibited human AChE in the presence of nerve agents is markedly impaired and the combination of obidoxime and HI-6 had no additive effect but could broaden the spectrum. Oximes 4-9 acetylcholinesterase (Cartwright blood group) Homo sapiens 50-54 25743373-2 2016 Inhibited AChE can be reactivated by cleavage of the Ser-phosphorus bond either spontaneously or through a reaction with nucleophilic agents, such as oximes. Oximes 150-156 acetylcholinesterase (Cartwright blood group) Homo sapiens 10-14 25743373-5 2016 Here, our goal was to study oxime reactivation and aging reactions of human AChE inhibited by mipafox or a sarin analog (Flu-MPs, fluorescent methylphosphonate). Oximes 28-33 acetylcholinesterase (Cartwright blood group) Homo sapiens 76-80 26519930-0 2015 Novel oxime-bearing coumarin derivatives act as potent Nrf2/ARE activators in vitro and in mouse model. Oximes 6-11 nuclear factor, erythroid derived 2, like 2 Mus musculus 55-59 28959540-4 2016 Currently approved antidotes against OPs include the peripheral anticholinergic drug atropine and an oxime that reactivates the inhibited cholinesterase. Oximes 101-106 butyrylcholinesterase Homo sapiens 138-152 26368669-1 2015 Tabun-inhibited acetylcholinesterase (AChE) is rather resistant towards reactivation by oximes in vitro while in vivo experiments showed some protection of animals poisoned by this chemical warfare nerve agent after treatment with an oxime and atropine. Oximes 88-94 acetylcholinesterase (Cartwright blood group) Homo sapiens 16-36 26368669-1 2015 Tabun-inhibited acetylcholinesterase (AChE) is rather resistant towards reactivation by oximes in vitro while in vivo experiments showed some protection of animals poisoned by this chemical warfare nerve agent after treatment with an oxime and atropine. Oximes 88-94 acetylcholinesterase (Cartwright blood group) Homo sapiens 38-42 26368669-1 2015 Tabun-inhibited acetylcholinesterase (AChE) is rather resistant towards reactivation by oximes in vitro while in vivo experiments showed some protection of animals poisoned by this chemical warfare nerve agent after treatment with an oxime and atropine. Oximes 88-93 acetylcholinesterase (Cartwright blood group) Homo sapiens 16-36 26368669-1 2015 Tabun-inhibited acetylcholinesterase (AChE) is rather resistant towards reactivation by oximes in vitro while in vivo experiments showed some protection of animals poisoned by this chemical warfare nerve agent after treatment with an oxime and atropine. Oximes 88-93 acetylcholinesterase (Cartwright blood group) Homo sapiens 38-42 26368669-2 2015 In addition, AChE inhibited by close tabun analogues, N,N-diethyltabun and N,N-di-n-propyltabun was completely resistant towards reactivation by oximes. Oximes 145-151 acetylcholinesterase (Cartwright blood group) Homo sapiens 13-17 26368669-3 2015 In order to get more insight into potential mechanisms of this oxime resistance experiments with these toxic agents and the oximes obidoxime, 2-PAM, MMB-4 and HI-6 were performed utilizing a dynamic model with real-time determination of AChE activity. Oximes 63-68 peptidylglycine alpha-amidating monooxygenase Homo sapiens 144-147 26368669-3 2015 In order to get more insight into potential mechanisms of this oxime resistance experiments with these toxic agents and the oximes obidoxime, 2-PAM, MMB-4 and HI-6 were performed utilizing a dynamic model with real-time determination of AChE activity. Oximes 63-68 acetylcholinesterase (Cartwright blood group) Homo sapiens 237-241 26368669-8 2015 These data give further support to the assumption that an interaction of tabun with residues in the active site gorge of AChE prevents effective reactivation by oximes, a mechanism which may also be the reason for the total oxime resistance of N,N-diethyl- and N,N-di-n-propyltabun-inhibited human AChE. Oximes 161-167 acetylcholinesterase (Cartwright blood group) Homo sapiens 121-125 26368669-8 2015 These data give further support to the assumption that an interaction of tabun with residues in the active site gorge of AChE prevents effective reactivation by oximes, a mechanism which may also be the reason for the total oxime resistance of N,N-diethyl- and N,N-di-n-propyltabun-inhibited human AChE. Oximes 161-167 acetylcholinesterase (Cartwright blood group) Homo sapiens 298-302 26368669-8 2015 These data give further support to the assumption that an interaction of tabun with residues in the active site gorge of AChE prevents effective reactivation by oximes, a mechanism which may also be the reason for the total oxime resistance of N,N-diethyl- and N,N-di-n-propyltabun-inhibited human AChE. Oximes 161-166 acetylcholinesterase (Cartwright blood group) Homo sapiens 121-125 26368669-8 2015 These data give further support to the assumption that an interaction of tabun with residues in the active site gorge of AChE prevents effective reactivation by oximes, a mechanism which may also be the reason for the total oxime resistance of N,N-diethyl- and N,N-di-n-propyltabun-inhibited human AChE. Oximes 161-166 acetylcholinesterase (Cartwright blood group) Homo sapiens 298-302 26210933-1 2016 The limited effectiveness of the established oximes obidoxime and pralidoxime resulted in ongoing research on novel oximes for the reactivation of acetylcholinesterase (AChE) inhibited by organophosphorus compounds (OP). Oximes 45-51 acetylcholinesterase (Cartwright blood group) Homo sapiens 169-173 26210933-1 2016 The limited effectiveness of the established oximes obidoxime and pralidoxime resulted in ongoing research on novel oximes for the reactivation of acetylcholinesterase (AChE) inhibited by organophosphorus compounds (OP). Oximes 116-122 acetylcholinesterase (Cartwright blood group) Homo sapiens 147-167 26210933-1 2016 The limited effectiveness of the established oximes obidoxime and pralidoxime resulted in ongoing research on novel oximes for the reactivation of acetylcholinesterase (AChE) inhibited by organophosphorus compounds (OP). Oximes 116-122 acetylcholinesterase (Cartwright blood group) Homo sapiens 169-173 26210933-4 2016 Several oximes with superior reactivating potency towards selective OP-AChE conjugates were identified but none of the tested oximes can be considered as a broad spectrum reactivator. Oximes 8-14 acetylcholinesterase (Cartwright blood group) Homo sapiens 71-75 26747974-2 2016 Both oximes are very potent reactivators of organophosphate-inhibited AChE. Oximes 5-11 acetylcholinesterase (Cartwright blood group) Homo sapiens 70-74 26705700-5 2016 Brain cholinesterase inhibition was slightly less in novel oxime treated rats compared to 2-PAM in the 24h survivors. Oximes 59-64 butyrylcholinesterase Rattus norvegicus 6-20 26519930-1 2015 We have designed and synthesized certain novel oxime- and amide-bearing coumarin derivatives as nuclear factor erythroid 2 p45-related factor 2 (Nrf2) activators. Oximes 47-52 nuclear factor, erythroid derived 2, like 2 Mus musculus 145-149 26519930-7 2015 These results suggested that novel oxime-bearing coumarin 17a is able to activate Nrf2/ARE pathway in vivo and are therefore seen as a promising candidate for further investigation. Oximes 35-40 nuclear factor, erythroid derived 2, like 2 Mus musculus 82-86 26468911-0 2015 Protein-Drug Interactions with Effective Polarization in Polarizable Water: Oxime Unbinding from AChE Gorge. Oximes 76-81 acetylcholinesterase (Cartwright blood group) Homo sapiens 97-101 25945727-5 2015 An aminooxy-modified LXR agonist was conjugated to anti-CD11a IgG through a stable, cathepsin B cleavable oxime linkage to afford a chemically defined ADC. Oximes 106-111 integrin subunit alpha L Homo sapiens 56-61 25945727-5 2015 An aminooxy-modified LXR agonist was conjugated to anti-CD11a IgG through a stable, cathepsin B cleavable oxime linkage to afford a chemically defined ADC. Oximes 106-111 cathepsin B Homo sapiens 84-95 26468911-2 2015 We present oxime (HI-6) unbinding from the active site gorge of AChE, known to be strongly influenced by intermolecular cation-pi, hydrogen bridge (HB) and water bridge (WB) interactions and by molecular simulations with effective polarization in polarizable mean-field model of TIP3P water. Oximes 11-16 acetylcholinesterase (Cartwright blood group) Homo sapiens 64-68 25407587-0 2015 Molecular modeling and in vitro reactivation study between the oxime BI-6 and acetylcholinesterase inhibited by different nerve agents. Oximes 63-68 acetylcholinesterase (Cartwright blood group) Homo sapiens 69-98 26594472-3 2015 Further, the O atom of the benzo-furan ring is syn to the N atom of the oxime group. Oximes 72-77 synemin Homo sapiens 47-50 25963916-0 2015 Binding of Anticell Adhesive Oxime-Crosslinked PEG Hydrogels to Cardiac Tissues. Oximes 29-34 progestagen associated endometrial protein Homo sapiens 47-50 26070418-7 2015 However, the synthesized oximes showed marginal reactivation efficacies in case of tabun inhibited hAChE. Oximes 25-31 acetylcholinesterase (Cartwright blood group) Homo sapiens 99-104 25907366-0 2015 Discovery of oxime-bearing naphthalene derivatives as a novel structural type of Nrf2 activators. Oximes 13-18 NFE2 like bZIP transcription factor 2 Homo sapiens 81-85 25907366-5 2015 In the present study, certain oxime-bearing naphthalene derivatives were synthesized and evaluated for their Nrf2 activation and anti-proliferative activities. Oximes 30-35 NFE2 like bZIP transcription factor 2 Homo sapiens 109-113 25963916-2 2015 A fast gelling oxime-crosslinked PEG hydrogel with tunable gelation time, degradation, and mechanical properties is presented. Oximes 15-20 progestagen associated endometrial protein Homo sapiens 33-36 25784649-2 2015 We recently synthesized the sodium salt of IQ-1S (11H-indeno[1,2-b]quinoxalin-11-one oxime) and demonstrated that it is a high-affinity JNK inhibitor and inhibits murine delayed-type hypersensitivity. Oximes 85-90 mitogen-activated protein kinase 8 Mus musculus 136-139 25835984-2 2015 Oxime antidotes commonly used to reactivate organophosphate inhibited AChE are ineffective against soman, while the efficacy of the recommended nerve agent bioscavenger butyrylcholinesterase is limited by strictly stoichiometric scavenging. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 70-74 25753941-0 2015 Rh(III)-catalyzed oxime ether-directed heteroarylation of arene through oxidative C-H/C-H cross-coupling. Oximes 18-23 churchill domain containing 1 Homo sapiens 82-89 25701203-2 2015 Here we evaluated the zebrafish as a potential pharmacological model for screening novel oxime antidotes to organophosphate (OP)-inhibited acetylcholinesterase (AChE). Oximes 89-94 acetylcholinesterase Danio rerio 161-165 25701203-5 2015 However, differences between the Kox and k2 constants suggest that zebrafish AChE associates more tightly with oximes, but has a slower maximal reactivation rate than human AChE. Oximes 111-117 acetylcholinesterase Danio rerio 77-81 24912784-5 2015 Human plasma was incubated with OP and the reactivation of inhibited BChE was tested with multiple oxime concentrations followed by nonlinear regression analysis for the determination of reactivity, affinity and overall reactivation constants. Oximes 99-104 butyrylcholinesterase Homo sapiens 69-73 24912784-6 2015 The generated data indicate that the tested oximes have a low-to-negligible reactivating potency with paraoxon- and tabun-inhibited human BChE. Oximes 44-50 butyrylcholinesterase Homo sapiens 138-142 25451328-1 2015 In this study, we employed site-directed mutagenesis to understand the role of amino acids in the gorge in oxime-induced reactivation of nerve agent-inhibited human (Hu) acetylcholinesterase (AChE). Oximes 107-112 acetylcholinesterase (Cartwright blood group) Homo sapiens 192-196 24912784-7 2015 Several oximes showed a moderate-to-high potency with cyclosarin-inhibited BChE. Oximes 8-14 butyrylcholinesterase Homo sapiens 75-79 24912784-9 2015 In the end, novel structures of oxime and non-oxime reactivators are urgently needed for the development of human BChE into an effective pseudo-catalytic scavenger. Oximes 32-37 butyrylcholinesterase Homo sapiens 114-118 24912784-9 2015 In the end, novel structures of oxime and non-oxime reactivators are urgently needed for the development of human BChE into an effective pseudo-catalytic scavenger. Oximes 46-51 butyrylcholinesterase Homo sapiens 114-118 25522658-0 2015 Effect of reversible ligands on oxime-induced reactivation of sarin- and cyclosarin-inhibited human acetylcholinesterase. Oximes 32-37 acetylcholinesterase (Cartwright blood group) Homo sapiens 100-120 25894563-1 2015 The ability of two novel bispyridinium oximes K727 and K733 and currently available oximes (HI-6, obidoxime) to reactivate sarin-inhibited acetylcholinesterase and to reduce acute toxicity of sarin was evaluated. Oximes 39-45 acetylcholinesterase Rattus norvegicus 139-159 25522658-4 2015 Hereby, oxime-induced reactivation of OP-inhibited non-human AChE was reported to be accelerated by different AChE-ligands. Oximes 8-13 acetylcholinesterase (Cartwright blood group) Homo sapiens 61-65 25522658-4 2015 Hereby, oxime-induced reactivation of OP-inhibited non-human AChE was reported to be accelerated by different AChE-ligands. Oximes 8-13 acetylcholinesterase (Cartwright blood group) Homo sapiens 110-114 25522658-5 2015 To investigate this concept with AChE from human source, the inhibitory potency, binding properties and the potential enhancement of oxime-induced reactivation of OP-inhibited AChE by structurally different AChE-ligands was assessed. Oximes 133-138 acetylcholinesterase (Cartwright blood group) Homo sapiens 33-37 25522658-5 2015 To investigate this concept with AChE from human source, the inhibitory potency, binding properties and the potential enhancement of oxime-induced reactivation of OP-inhibited AChE by structurally different AChE-ligands was assessed. Oximes 133-138 acetylcholinesterase (Cartwright blood group) Homo sapiens 176-180 25522658-5 2015 To investigate this concept with AChE from human source, the inhibitory potency, binding properties and the potential enhancement of oxime-induced reactivation of OP-inhibited AChE by structurally different AChE-ligands was assessed. Oximes 133-138 acetylcholinesterase (Cartwright blood group) Homo sapiens 176-180 25522658-6 2015 Several ligands competed with the oxime for the AChE binding-site impairing reactivation of OP-inhibited AChE whereas a markedly accelerated reactivation of sarin-inhibited enzyme by obidoxime was recorded in the presence of edrophonium, galanthamine and donepezil. Oximes 34-39 acetylcholinesterase (Cartwright blood group) Homo sapiens 48-52 25522658-6 2015 Several ligands competed with the oxime for the AChE binding-site impairing reactivation of OP-inhibited AChE whereas a markedly accelerated reactivation of sarin-inhibited enzyme by obidoxime was recorded in the presence of edrophonium, galanthamine and donepezil. Oximes 34-39 acetylcholinesterase (Cartwright blood group) Homo sapiens 105-109 25450746-0 2015 Adaptation of a dynamic in vitro model with real-time determination of butyrylcholinesterase activity in the presence of cyclosarin and an oxime. Oximes 141-146 butyrylcholinesterase Homo sapiens 72-93 25369775-0 2015 Generation and screening of oxime libraries addressing the neuronal GABA transporter GAT1. Oximes 28-33 solute carrier family 6 member 1 Homo sapiens 85-89 25461321-1 2015 Utilizing our previously reported in silico pharmacophore model for reactivation efficacy of oximes, we present here a discovery of twelve new non-oxime reactivators of diisopropylfluorophosphate (DFP)-inhibited acetylcholinesterase (AChE) obtained through virtual screening of an in-house compound database. Oximes 93-99 acetylcholinesterase Rattus norvegicus 234-238 25461321-1 2015 Utilizing our previously reported in silico pharmacophore model for reactivation efficacy of oximes, we present here a discovery of twelve new non-oxime reactivators of diisopropylfluorophosphate (DFP)-inhibited acetylcholinesterase (AChE) obtained through virtual screening of an in-house compound database. Oximes 93-98 acetylcholinesterase Rattus norvegicus 234-238 25461323-2 2015 A series of novel VEGFR-2 inhibitors containing oxime as hinge binding fragment were described. Oximes 48-53 kinase insert domain receptor Homo sapiens 18-25 25461323-4 2015 The oxime group was firstly introduced to interact with hinge region of VEGFR-2. Oximes 4-9 kinase insert domain receptor Homo sapiens 72-79 25373357-0 2015 Relationships between the antidotal efficacy and structure, PK/PD parameters and bio-relevant molecular descriptors of AChE reactivating oximes: inclusion and integration to biopharmaceutical classification systems. Oximes 137-143 acetylcholinesterase (Cartwright blood group) Homo sapiens 119-123 25497132-0 2015 Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor alpha/gamma ligand LT175. Oximes 71-77 peroxisome proliferator activated receptor alpha Homo sapiens 96-144 25373357-1 2015 INTRODUCTION: The therapeutic outcome of oximes used as reactivators of phosphorylated human acetylcholinesterase (AChE) is influenced, among other factors, by their biological distribution, their in vivo ability to achieve the nucleophilic attack and their affinity for the anionic center of the intact/inhibited AChE. Oximes 41-47 acetylcholinesterase (Cartwright blood group) Homo sapiens 93-113 25373357-1 2015 INTRODUCTION: The therapeutic outcome of oximes used as reactivators of phosphorylated human acetylcholinesterase (AChE) is influenced, among other factors, by their biological distribution, their in vivo ability to achieve the nucleophilic attack and their affinity for the anionic center of the intact/inhibited AChE. Oximes 41-47 acetylcholinesterase (Cartwright blood group) Homo sapiens 115-119 25373357-1 2015 INTRODUCTION: The therapeutic outcome of oximes used as reactivators of phosphorylated human acetylcholinesterase (AChE) is influenced, among other factors, by their biological distribution, their in vivo ability to achieve the nucleophilic attack and their affinity for the anionic center of the intact/inhibited AChE. Oximes 41-47 acetylcholinesterase (Cartwright blood group) Homo sapiens 314-318 25373357-5 2015 EXPERT OPINION: The structural differences of the organophosphorus compounds (OP) and the available oximes reactivators of OP-inhibited AChE generate distinct toxicokinetic or PK profiles. Oximes 100-106 acetylcholinesterase (Cartwright blood group) Homo sapiens 136-140 25351635-0 2015 Oxime bond-linked daunorubicin-GnRH-III bioconjugates exert antitumor activity in castration-resistant prostate cancer cells via the type I GnRH receptor. Oximes 0-5 gonadotropin releasing hormone receptor Homo sapiens 133-153 25894563-6 2015 On the other hand, the oxime HI-6 was found to be the most efficient reactivator of sarin-inhibited acetylcholinesterase. Oximes 23-28 acetylcholinesterase Rattus norvegicus 100-120 24805972-0 2015 Oxime-dipeptides as anticholinesterase, reactivator of phosphonylated-serine of AChE catalytic triad: probing the mechanistic insight by MM-GBSA, dynamics simulations and DFT analysis. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 80-84 25859175-5 2015 There are also known triterpenes with two carbonyl groups, e.g. at C-3 and C-11 positions, which differ in reactivity: among them only C-3 group can be transformed into oxime. Oximes 169-174 complement C3 Homo sapiens 67-70 25845909-1 2015 Oxime K203 seems to be the most promising oxime in case of reactivation of tabun-inhibited acetylcholinesterase (AChE). Oximes 42-47 acetylcholinesterase (Cartwright blood group) Homo sapiens 113-117 25859175-5 2015 There are also known triterpenes with two carbonyl groups, e.g. at C-3 and C-11 positions, which differ in reactivity: among them only C-3 group can be transformed into oxime. Oximes 169-174 RNA polymerase III subunit K Homo sapiens 75-79 25859175-5 2015 There are also known triterpenes with two carbonyl groups, e.g. at C-3 and C-11 positions, which differ in reactivity: among them only C-3 group can be transformed into oxime. Oximes 169-174 complement C3 Homo sapiens 135-138 25304213-8 2015 However, in the presence of eight novel oximes, PON1-mediated degradation of both surrogates occurs. Oximes 40-46 paraoxonase 1 Homo sapiens 48-52 25479380-1 2014 For three random splits, one-variable models of oximes reactivation of sarin inhibited acetylcholinesterase (logarithm of the AChE reactivation percentage by oximes with concentration of 0.001 M) have been calculated with CORAL software. Oximes 48-54 acetylcholinesterase (Cartwright blood group) Homo sapiens 126-130 25240274-6 2014 This effect was not observed when incubating highly diluted AChE with oximes. Oximes 70-76 acetylcholinesterase (Cartwright blood group) Homo sapiens 60-64 25190468-1 2014 The search of proficient oximes as reactivators of irreversibly inhibited-AChE by organophosphate poisoning necessitates an appropriate assessment of their physicochemical properties and reactivation kinetics. Oximes 25-31 acetylcholinesterase (Cartwright blood group) Homo sapiens 74-78 25218671-0 2014 Quantum chemical and steered molecular dynamics studies for one pot solution to reactivate aged acetylcholinesterase with alkylator oxime. Oximes 132-137 acetylcholinesterase (Cartwright blood group) Homo sapiens 96-116 25218671-1 2014 Dimethyl(pyridin-2-yl)sulfonium based oxime has been designed to reverse the aging process of organophosphorus inhibited AChE and to reactivate the aged-AChE adduct. Oximes 38-43 acetylcholinesterase (Cartwright blood group) Homo sapiens 121-125 25218671-1 2014 Dimethyl(pyridin-2-yl)sulfonium based oxime has been designed to reverse the aging process of organophosphorus inhibited AChE and to reactivate the aged-AChE adduct. Oximes 38-43 acetylcholinesterase (Cartwright blood group) Homo sapiens 153-157 25218671-5 2014 The free enzyme can be liberated from the inhibited acetylcholinesterase with the sulfonium compound decorated with an oxime group to avoid the administration of oxime drugs separately. Oximes 119-124 acetylcholinesterase (Cartwright blood group) Homo sapiens 52-72 25218671-5 2014 The free enzyme can be liberated from the inhibited acetylcholinesterase with the sulfonium compound decorated with an oxime group to avoid the administration of oxime drugs separately. Oximes 162-167 acetylcholinesterase (Cartwright blood group) Homo sapiens 52-72 25218671-12 2014 The computational study suggests that the newly designed oxime is a potential candidate to reactivate the aged-AChE adduct. Oximes 57-62 acetylcholinesterase (Cartwright blood group) Homo sapiens 111-115 25346249-8 2014 Shift of DFP induced brain AChE IC50 curves to right was observed at 0.20 LD50 treatment dose of oximes with respect to 2-PAM. Oximes 97-103 acetylcholinesterase Mus musculus 27-31 25190468-4 2014 Further the tested oximes were screened through in vitro reactivation kinetics against paraoxon-inhibited AChE. Oximes 19-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 106-110 25045021-0 2014 The mitochondrial amidoxime reducing component (mARC): involvement in metabolic reduction of N-oxides, oximes and N-hydroxyamidinohydrazones. Oximes 103-109 activity regulated cytoskeletal-associated protein Mus musculus 48-52 25045021-2 2014 In this study, we tested the involvement of mARC in the reduction of N-oxides (amitriptyline-N-oxide, nicotinamide-N-oxide), oximes ((E)-/(Z)-2,4,6-trimethylacetophenonoxime) and a N-hydroxyamidinohydrazone (guanoxabenz). Oximes 125-131 activity regulated cytoskeletal-associated protein Mus musculus 44-48 25045021-6 2014 However, differences in the reduction of oximes and N-oxides between the two isoforms, namely mARC1 and mARC2, were detectable; N-oxides are exclusively reduced by mARC1. Oximes 41-47 mitochondrial amidoxime reducing component 2 Mus musculus 94-99 25045021-6 2014 However, differences in the reduction of oximes and N-oxides between the two isoforms, namely mARC1 and mARC2, were detectable; N-oxides are exclusively reduced by mARC1. Oximes 41-47 mitochondrial amidoxime reducing component 2 Mus musculus 104-109 25045021-6 2014 However, differences in the reduction of oximes and N-oxides between the two isoforms, namely mARC1 and mARC2, were detectable; N-oxides are exclusively reduced by mARC1. Oximes 41-47 mitochondrial amidoxime reducing component 2 Mus musculus 164-169 24136594-9 2014 Prophylactic administration of an oxime (such as K-27) in case of imminent OPC exposure may be a viable option. Oximes 34-39 keratin 27 Rattus norvegicus 49-53 25016257-5 2014 (1) The 1H-NMR signals at ~5.5, 4-8, 7.4-10.2, and 12.22-12.37 ppm were attributed to the chemical shifts of active protons on carbons adjacent to R-OH, RAr-OH, oximes, and -COOH, respectively. Oximes 161-167 RAB40B, member RAS oncogene family Homo sapiens 153-156 24964273-3 2014 Tabun is one of the highly toxic organophosphorus (OP) compounds and is resistant to many oxime drugs formulated for the reactivation of AChE. Oximes 90-95 acetylcholinesterase (Cartwright blood group) Homo sapiens 137-141 24902036-0 2014 Ketoxime coupling of p-acetylphenylalanine at neutral pH for site-directed spin labeling of human sulfite oxidase. Oximes 0-8 sulfite oxidase Homo sapiens 98-113 24902036-1 2014 Site-directed spin labeling of the unnatural amino acid p-acetylphenylalanine (p-AcPhe) using oxime based coupling chemistry is successfully applied to investigate human sulfite oxidase (hSO), a protein containing an essential cysteine residue, which impedes the use of thiol based coupling chemistry. Oximes 94-99 sulfite oxidase Homo sapiens 170-185 24549829-0 2014 Unbinding free energy of acetylcholinesterase bound oxime drugs along the gorge pathway from metadynamics-umbrella sampling investigation. Oximes 52-57 acetylcholinesterase (Cartwright blood group) Homo sapiens 25-45 25006785-10 2014 We observed the involvement of BKCa channels in Oxime S1-induced relaxation in mesenteric artery rings. Oximes 48-53 potassium calcium-activated channel subfamily M alpha 1 Rattus norvegicus 31-35 23962483-0 2013 Investigation of kinetic interactions between approved oximes and human acetylcholinesterase inhibited by pesticide carbamates. Oximes 55-61 acetylcholinesterase (Cartwright blood group) Homo sapiens 72-92 24129980-5 2014 This is confirmed using HEK-293 cells transfected to express human HDC and the aminooxy analog of histidine, 4(5)-aminooxymethylimidazole (O-IMHA, IC50 2 x 10(-7) M) capable to form a PLP-inhibitor complex (oxime) in the enzyme active center. Oximes 209-214 histidine decarboxylase Homo sapiens 67-70 24129980-6 2014 Taking advantage of the availability of the human HDC X-ray structure, we have also determined the potential interactions that could stabilize this oxime in the active site of mammalian HDC. Oximes 148-153 histidine decarboxylase Homo sapiens 50-53 24129980-6 2014 Taking advantage of the availability of the human HDC X-ray structure, we have also determined the potential interactions that could stabilize this oxime in the active site of mammalian HDC. Oximes 148-153 histidine decarboxylase Homo sapiens 186-189 24345352-1 2014 Reactivation of organophosphate (OP) inhibited acetylcholinesterase (AChE) by oximes is inadequate against various OP nerve agents known till date owing to their diverse structural features. Oximes 78-84 acetylcholinesterase (Cartwright blood group) Homo sapiens 69-73 24345352-3 2014 The efficacy of oxime reactivators is estimated through different in vitro and in vivo models using AChE from various sources against structurally different OPs. Oximes 16-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 100-104 24345352-7 2014 The enhanced reactivation efficacy of oximes may be attributed to the optimal length of xylene linker which facilitates appropriate positioning of carbamoyl function to the peripheral anionic site (PAS) and extending the oxime moiety to the active site of AChE. Oximes 38-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 256-260 24345352-7 2014 The enhanced reactivation efficacy of oximes may be attributed to the optimal length of xylene linker which facilitates appropriate positioning of carbamoyl function to the peripheral anionic site (PAS) and extending the oxime moiety to the active site of AChE. Oximes 38-43 acetylcholinesterase (Cartwright blood group) Homo sapiens 256-260 24057572-1 2014 Great efforts have been undertaken in the last decades to develop new oximes to reactivate acetylcholinesterase inhibited by organophosphorus compounds (OP). Oximes 70-76 acetylcholinesterase (Cartwright blood group) Homo sapiens 91-111 24283935-1 2014 A novel oxime grafting scheme was utilized to conjugate an ICAM-1 ligand (LABL), a cellular antigen ovalbumin (OVA), or both peptides simultaneously to hyaluronic acid (HA). Oximes 8-13 intercellular adhesion molecule 1 Homo sapiens 59-65 24599312-3 2014 Moreover, these oximes also exhibit a good ability to reactivate VX-, tabun- and paraoxon-inhibited human AChE. Oximes 16-22 acetylcholinesterase (Cartwright blood group) Homo sapiens 106-110 24658567-1 2014 A new series of oxime ethers 4a-z was designed and synthesized to test the blocking activity against beta1 and beta2-adrenergic receptors. Oximes 16-21 potassium calcium-activated channel subfamily M regulatory beta subunit 1 Homo sapiens 101-106 24658567-1 2014 A new series of oxime ethers 4a-z was designed and synthesized to test the blocking activity against beta1 and beta2-adrenergic receptors. Oximes 16-21 potassium calcium-activated channel subfamily M regulatory beta subunit 2 Homo sapiens 111-116 24258240-0 2014 Oxime-type acetylcholinesterase reactivators in pregnancy: an overview. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 11-31 24295433-1 2014 The potency of two newly developed oximes (K361 and K378) to reactivate tabun-inhibited cholinesterase and to reduce acute toxicity of tabun was compared with the oxime K203 and trimedoxime using in vivo methods. Oximes 35-41 butyrylcholinesterase Rattus norvegicus 88-102 24295433-1 2014 The potency of two newly developed oximes (K361 and K378) to reactivate tabun-inhibited cholinesterase and to reduce acute toxicity of tabun was compared with the oxime K203 and trimedoxime using in vivo methods. Oximes 35-40 butyrylcholinesterase Rattus norvegicus 88-102 24295433-3 2014 In the brain, the potency of both newly developed oximes to reactivate tabun-inhibited cholinesterase was negligible. Oximes 50-56 butyrylcholinesterase Rattus norvegicus 87-101 24443939-0 2014 Exploring the physicochemical properties of oxime-reactivation therapeutics for cyclosarin, sarin, tabun, and VX inactivated acetylcholinesterase. Oximes 44-49 acetylcholinesterase (Cartwright blood group) Homo sapiens 125-145 24443939-2 2014 The reactivation of OP-inactivated AChE is dependent on the OP conjugate, and commonly a specific oxime is better at reactivating a specific OP conjugate than several diverse OP conjugates. Oximes 98-103 acetylcholinesterase (Cartwright blood group) Homo sapiens 35-39 24443939-8 2014 The reactivation of AChE inactivated with either cyclosarin or tabun requires the oxime therapeutic to possess an overall polar-positive surface area. Oximes 82-87 acetylcholinesterase (Cartwright blood group) Homo sapiens 20-24 24443939-9 2014 Oxime therapeutics for the reactivation of sarin-inactivated AChE are conformationally dependent while oxime reverse therapeutics for VX require a compact region with a highly hydrophilic region and two positively charged pyridine rings. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 61-65 24344993-5 2014 In this work, we evaluated the affinity and reactivity of oximes with activity already reported against AChE inhibited by the OP chemical warfare agent ciclosarin, with MmAChE and HsAChE active sites inhibited by the CB pesticide carbofuran. Oximes 58-64 acetylcholinesterase (Cartwright blood group) Homo sapiens 104-108 24200808-1 2013 An analysis of the main pharmacophoric features present in the still limited number of inhibitors of glucose transporter GLUT1 led to the identification of new oxime-based inhibitors, which proved to be able to efficiently hinder glucose uptake and cell growth in H1299 lung cancer cells. Oximes 160-165 solute carrier family 2 member 1 Homo sapiens 121-126 23962483-4 2013 Therefore, we performed an in vitro kinetic study to investigate the effect of clinically used oximes on carbamoylation and decarbamoylation of human AChE. Oximes 95-101 acetylcholinesterase (Cartwright blood group) Homo sapiens 150-154 24312449-7 2013 The calculated activation barriers support the superiority of neutral oximes for the activation of tabun-inhibited AChE compared to charged oximes. Oximes 70-76 acetylcholinesterase (Cartwright blood group) Homo sapiens 115-119 24312449-9 2013 Docking studies revealed that the poor binding affinity of simple neutral oxime drugs such as 3-hydroxy-2-pyridinealdoxime inside the active-site gorge of AChE was significantly augmented with the addition of neutral peripheral units compared to conventional charged peripheral sites. Oximes 74-79 acetylcholinesterase (Cartwright blood group) Homo sapiens 155-159 24161674-5 2013 Substitution of 5 amino acid residues in combination with the use of an oxime linker for dimerization increased the solubility and chemical stability of the dimeric CXCL14(51-77). Oximes 72-77 C-X-C motif chemokine ligand 14 Homo sapiens 165-171 24157926-2 2013 Standard treatment by administration of atropine and oximes, e.g., obidoxime or pralidoxime, focuses on antagonism of mAChRs and reactivation of AChE, whereas nicotinic malfunction is not directly treated. Oximes 53-59 acetylcholinesterase (Cartwright blood group) Homo sapiens 145-149 24054643-6 2013 An oxime peak identifier (OPI) of the carbohydrate analytes, based on the combination of an internal standard and the corresponding syn/anti peak ratios, increased the reliability of the identification of reducing carbohydrates. Oximes 3-8 synemin Homo sapiens 132-135 23735753-9 2013 On the other hand pralidoxime, an oxime, reactivating acetylcholinesterase (AChE) after organophosphate poisoning, induced population spike recovery after DFP exposure in the presence of bradykinin and Lys-des-Arg(9)-bradykinin. Oximes 24-29 acetylcholinesterase (Cartwright blood group) Homo sapiens 76-80 23735753-9 2013 On the other hand pralidoxime, an oxime, reactivating acetylcholinesterase (AChE) after organophosphate poisoning, induced population spike recovery after DFP exposure in the presence of bradykinin and Lys-des-Arg(9)-bradykinin. Oximes 24-29 kininogen 1 Homo sapiens 187-197 23735753-9 2013 On the other hand pralidoxime, an oxime, reactivating acetylcholinesterase (AChE) after organophosphate poisoning, induced population spike recovery after DFP exposure in the presence of bradykinin and Lys-des-Arg(9)-bradykinin. Oximes 24-29 kininogen 1 Homo sapiens 217-227 23789829-0 2013 In silico pharmacophore modeling on known pyridinium oxime reactivators of cyclosarin (GF) inhibited AChE to Aid discovery of potential, more efficacious novel non-oxime reactivators. Oximes 53-58 acetylcholinesterase (Cartwright blood group) Homo sapiens 101-105 23789829-0 2013 In silico pharmacophore modeling on known pyridinium oxime reactivators of cyclosarin (GF) inhibited AChE to Aid discovery of potential, more efficacious novel non-oxime reactivators. Oximes 53-58 activation induced cytidine deaminase Homo sapiens 109-112 23789829-3 2013 The model was generated from published experimental percentage reactivation data on oximes as changes of AChE/BuChE activities in the whole blood after cyclosarin intoxication and administration. Oximes 84-90 acetylcholinesterase (Cartwright blood group) Homo sapiens 105-109 23789829-6 2013 Furthermore, from virtual screening of two commercial databases, Maybridge and ChemNavigator using map-fitting of the model led us to identify two new non-oxime compounds showing reactivation efficacy within 10-fold range of 2-PAM for DFP-inhibited AChE. Oximes 155-160 acetylcholinesterase (Cartwright blood group) Homo sapiens 249-253 23680647-0 2013 Kinetic analysis of inhibition of glucoamylase and active site mutants via chemoselective oxime immobilization of acarbose on SPR chip surfaces. Oximes 90-95 sepiapterin reductase Homo sapiens 126-129 23631694-11 2013 Oxidation of the sialic acid side chains of Tf generated aldehyde functionalized protein that was reacted with aminooxy terminated poly(HPMA), which resulted in protein-polymer bioconjugates carrying oxime linkages. Oximes 200-205 transferrin Homo sapiens 44-46 23959117-0 2013 Oximes: inhibitors of human recombinant acetylcholinesterase. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 40-60 23959117-3 2013 Standard care involves the use of anticonvulsants (e.g., diazepam), parasympatolytics (e.g., atropine) and oximes that restore AChE activity. Oximes 107-113 acetylcholinesterase (Cartwright blood group) Homo sapiens 127-131 23959117-4 2013 However, oximes also bind to the active site of AChE, simultaneously acting as reversible inhibitors. Oximes 9-15 acetylcholinesterase (Cartwright blood group) Homo sapiens 48-52 23959117-5 2013 The goal of the present study is to determine how oxime structure influences the inhibition of human recombinant AChE (hrAChE). Oximes 50-55 acetylcholinesterase (Cartwright blood group) Homo sapiens 113-117 22960624-0 2013 Centrally acting oximes in reactivation of tabun-phosphoramidated AChE. Oximes 17-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 66-70 22827894-0 2013 Structural requirements for effective oximes--evaluation of kinetic in vitro data with phosphylated human AChE and structurally different oximes. Oximes 38-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 106-110 22827894-1 2013 Treatment of poisoning by various organophosphorus (OP) nerve agents with established acetylcholinesterase (AChE) reactivators (oximes) is insufficient. Oximes 128-134 acetylcholinesterase (Cartwright blood group) Homo sapiens 86-106 22827894-1 2013 Treatment of poisoning by various organophosphorus (OP) nerve agents with established acetylcholinesterase (AChE) reactivators (oximes) is insufficient. Oximes 128-134 acetylcholinesterase (Cartwright blood group) Homo sapiens 108-112 22827894-4 2013 The crucial mechanism of action of oximes is the reactivation of phosphylated AChE. Oximes 35-41 acetylcholinesterase (Cartwright blood group) Homo sapiens 78-82 22827894-6 2013 It was tempting to evaluate the reactivation kinetics of a series of oximes with various OP inhibitors performed under identical experimental conditions in order to get insight into structural requirements for adequate affinity and reactivity towards inhibited AChE. Oximes 69-75 acetylcholinesterase (Cartwright blood group) Homo sapiens 261-265 22827894-7 2013 The determination of reactivation rate constants with bispyridinium oximes having different linkers, bearing oxime group(s) at different positions and having in part additional substituents revealed that (a) the reactivating potency was dependent on the position of the oxime groups and of additional substituents, (b) small modifications of the oxime structure had an in part marked effect on the kinetic properties and (c) no single oxime had an adequate reactivating potency with AChE inhibited by structurally different OP. Oximes 68-73 acetylcholinesterase (Cartwright blood group) Homo sapiens 483-487 22982773-0 2013 A common mechanism for resistance to oxime reactivation of acetylcholinesterase inhibited by organophosphorus compounds. Oximes 37-42 acetylcholinesterase (Cartwright blood group) Homo sapiens 59-79 22982773-1 2013 Administration of oxime therapy is currently the standard approach used to reverse the acute toxicity of organophosphorus (OP) compounds, which is usually attributed to OP inhibition of acetylcholinesterase (AChE). Oximes 18-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 186-206 22982773-1 2013 Administration of oxime therapy is currently the standard approach used to reverse the acute toxicity of organophosphorus (OP) compounds, which is usually attributed to OP inhibition of acetylcholinesterase (AChE). Oximes 18-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 208-212 22982773-2 2013 Rate constants for reactivation of OP-inhibited AChE by even the best oximes, such as HI-6 and obidoxime, can vary >100-fold between OP-AChE conjugates that are easily reactivated and those that are difficult to reactivate. Oximes 70-76 acetylcholinesterase (Cartwright blood group) Homo sapiens 48-52 22982773-2 2013 Rate constants for reactivation of OP-inhibited AChE by even the best oximes, such as HI-6 and obidoxime, can vary >100-fold between OP-AChE conjugates that are easily reactivated and those that are difficult to reactivate. Oximes 70-76 acetylcholinesterase (Cartwright blood group) Homo sapiens 139-143 22982773-3 2013 To gain a better understanding of this oxime specificity problem for future design of improved reactivators, we conducted a QSAR analysis for oxime reactivation of AChE inhibited by OP agents and their analogues. Oximes 39-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 164-168 22982773-3 2013 To gain a better understanding of this oxime specificity problem for future design of improved reactivators, we conducted a QSAR analysis for oxime reactivation of AChE inhibited by OP agents and their analogues. Oximes 142-147 acetylcholinesterase (Cartwright blood group) Homo sapiens 164-168 22982773-4 2013 Our objective was to identify common mechanism(s) among OP-AChE conjugates of phosphates, phosphonates and phosphoramidates that result in resistance to oxime reactivation. Oximes 153-158 acetylcholinesterase (Cartwright blood group) Homo sapiens 59-63 22982773-5 2013 Our evaluation of oxime reactivation of AChE inhibited by a sarin analogue, O-methyl isopropylphosphonofluoridate, or a cyclosarin analogue, O-methyl cyclohexylphosphonofluoridate, indicated that AChE inhibited by these analogues was at least 70-fold more difficult to reactivate than AChE inhibited by sarin or cyclosarin. Oximes 18-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 40-44 22982773-5 2013 Our evaluation of oxime reactivation of AChE inhibited by a sarin analogue, O-methyl isopropylphosphonofluoridate, or a cyclosarin analogue, O-methyl cyclohexylphosphonofluoridate, indicated that AChE inhibited by these analogues was at least 70-fold more difficult to reactivate than AChE inhibited by sarin or cyclosarin. Oximes 18-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 196-200 22982773-5 2013 Our evaluation of oxime reactivation of AChE inhibited by a sarin analogue, O-methyl isopropylphosphonofluoridate, or a cyclosarin analogue, O-methyl cyclohexylphosphonofluoridate, indicated that AChE inhibited by these analogues was at least 70-fold more difficult to reactivate than AChE inhibited by sarin or cyclosarin. Oximes 18-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 196-200 23047024-1 2013 Organophosphorus compounds (OPs) and oximes may interfere with other molecules than AChE in the living systems, affecting in this way various cellular processes and underlying mechanisms. Oximes 37-43 acetylcholinesterase (Cartwright blood group) Homo sapiens 84-88 23073172-1 2013 We are evaluating a facilitative transport strategy to move oximes across the blood brain barrier (BBB) to reactivate inhibited brain acetylcholinesterase (AChE). Oximes 60-66 acetylcholinesterase (Cartwright blood group) Homo sapiens 156-160 23422169-7 2013 Previous work has shown the success of oxime-based sensors in the selective detection of AChE inhibitors and this work highlights the ability of an AChE-inspired biomimetic sensor to accurately predict the toxicity (LD50 and LC50) for a range of AChE inhibitors. Oximes 39-44 acetylcholinesterase Rattus norvegicus 89-93 23422169-7 2013 Previous work has shown the success of oxime-based sensors in the selective detection of AChE inhibitors and this work highlights the ability of an AChE-inspired biomimetic sensor to accurately predict the toxicity (LD50 and LC50) for a range of AChE inhibitors. Oximes 39-44 acetylcholinesterase Rattus norvegicus 148-152 23422169-7 2013 Previous work has shown the success of oxime-based sensors in the selective detection of AChE inhibitors and this work highlights the ability of an AChE-inspired biomimetic sensor to accurately predict the toxicity (LD50 and LC50) for a range of AChE inhibitors. Oximes 39-44 acetylcholinesterase Rattus norvegicus 148-152 23314320-2 2013 The current U.S. military and civilian oxime countermeasure, 2-[(hydroxyimino)methyl]-1-methylpyridin-1-ium chloride (2-PAM), is under consideration for replacement with a more effective acetylcholinesterase reactivator, 1,1"-methylenebis{4-hydroxyiminomethyl}pyridinium dimethanesulfonate (MMB-4). Oximes 39-44 peptidylglycine alpha-amidating monooxygenase Homo sapiens 120-123 23534424-1 2013 BACKGROUND: Extreme efforts are made for the structural diversification of oximes used as AChE reactivators. Oximes 75-81 acetylcholinesterase (Cartwright blood group) Homo sapiens 90-94 23073172-5 2013 Here we report the reactivation parameters for VX- and GB-inhibited human (Hu) AChE of the best SOx (13c) and our findings that the kinetics are similar to those of the parent oxime. Oximes 176-181 acetylcholinesterase (Cartwright blood group) Homo sapiens 79-83 23111374-4 2013 In this study, a series of seven new uncharged oximes reactivators have been synthesized and their in vitro ability to reactivate VX and tabun-inhibited human acetylcholinesterase (hAChE) has been evaluated. Oximes 47-53 acetylcholinesterase (Cartwright blood group) Homo sapiens 159-179 23111374-4 2013 In this study, a series of seven new uncharged oximes reactivators have been synthesized and their in vitro ability to reactivate VX and tabun-inhibited human acetylcholinesterase (hAChE) has been evaluated. Oximes 47-53 acetylcholinesterase (Cartwright blood group) Homo sapiens 181-186 23123249-0 2013 Testing of novel brain-penetrating oxime reactivators of acetylcholinesterase inhibited by nerve agent surrogates. Oximes 35-40 acetylcholinesterase Rattus norvegicus 57-77 23123249-1 2013 A critical need for combating the effects of organophosphate (OP) anticholinesterases, such as nerve agents, is the current lack of an effective oxime reactivator which can penetrate the blood-brain barrier (BBB), and therefore reactivate inhibited acetylcholinesterase (AChE) in the brain. Oximes 145-150 acetylcholinesterase Rattus norvegicus 249-269 23123249-1 2013 A critical need for combating the effects of organophosphate (OP) anticholinesterases, such as nerve agents, is the current lack of an effective oxime reactivator which can penetrate the blood-brain barrier (BBB), and therefore reactivate inhibited acetylcholinesterase (AChE) in the brain. Oximes 145-150 acetylcholinesterase Rattus norvegicus 271-275 23123249-4 2013 The oximes demonstrated a range of 14-76% reactivation of rat brain AChE in vitro. Oximes 4-10 acetylcholinesterase Rattus norvegicus 68-72 23123249-5 2013 An in vivo testing paradigm was developed in which the novel oxime was administered at the time of maximal brain AChE inhibition (about 80%) (1h) elicited by nitrophenyl isopropyl methylphosphonate (NIMP; sarin surrogate). Oximes 61-66 acetylcholinesterase Rattus norvegicus 113-117 23123249-6 2013 This paradigm, with delayed administration of oxime to a time when brain AChE was starting to recover, was designed to minimize reactivation/reinhibition of peripheral AChE during the reactivation period which would decrease the availability of the surrogate for entry into the brain; this paradigm will allow proof of concept of BBB penetrability. Oximes 46-51 acetylcholinesterase Rattus norvegicus 168-172 23220589-6 2013 The aim of the present study was to evaluate the efficacy of some ChE reactivators against OPC intoxication (tabun, paraoxon and dichlorvos) in in vitro experiments and to compare their activity to that known for some currently used oximes (obidoxime, HI-6, 2-PAM). Oximes 233-239 butyrylcholinesterase Rattus norvegicus 66-69 22960624-4 2013 The oxime RS150D [N-((1-(3-(2-((hydroxyimino)methyl)-1H-imidazol-1-yl)propyl)-1H-1,2,3-triazol-4-yl)methyl)benzamide] was highlighted as the most promising reactivator of the tabun-hAChE conjugate. Oximes 4-9 acetylcholinesterase (Cartwright blood group) Homo sapiens 181-186 22975155-1 2013 A library of more than 200 novel uncharged oxime reactivators was used to select and refine lead reactivators of human acetylcholinesterase (hAChE) covalently conjugated with sarin, cyclosarin, VX, paraoxon and tabun. Oximes 43-48 acetylcholinesterase (Cartwright blood group) Homo sapiens 141-146 23339663-8 2013 X-ray crystallography and mass spectrometry show the formation of an aged end product formed in both AChE and BChE that cannot be reactivated by current oxime-based therapeutics. Oximes 153-158 acetylcholinesterase (Cartwright blood group) Homo sapiens 101-105 23339663-8 2013 X-ray crystallography and mass spectrometry show the formation of an aged end product formed in both AChE and BChE that cannot be reactivated by current oxime-based therapeutics. Oximes 153-158 butyrylcholinesterase Homo sapiens 110-114 22901042-2 2013 The study determining percentage of reactivation of tabun-inhibited diaphragm and brain acetylcholinesterase in poisoned rats showed that the reactivating efficacy of all newly developed oximes is comparable with K203 but lower than the reactivating potency of trimedoxime in diaphragm. Oximes 187-193 acetylcholinesterase Rattus norvegicus 88-108 23085985-6 2013 The Ag2 ion is coordinated to the N61 oxime nitrogens, a monodentate and a (O,O)-bridging nitrato/perchlorato or two monodentate O-trifluoromethylsulfonato anions. Oximes 38-43 anterior gradient 2, protein disulphide isomerase family member Homo sapiens 4-7 23184734-2 2013 We found that the HDAC potency and isoform selectivity provided by the oxime unit of psammaplin A could be reproduced by using carefully chosen heterocyclic frameworks. Oximes 71-76 histone deacetylase 9 Homo sapiens 18-22 23410111-2 2013 Although oxime nucleophiles can reactivate the AChE-phosphyl adduct, the adduct undergoes a reaction called aging. Oximes 9-14 acetylcholinesterase (Cartwright blood group) Homo sapiens 47-51 22561105-0 2012 Kinetic interactions of a homologous series of bispyridinium monooximes (HGG oximes) with native and phosphonylated human acetylcholinesterase. Oximes 65-71 acetylcholinesterase (Cartwright blood group) Homo sapiens 122-142 23002990-2 2012 Treatment of O-arylmethyl alkynyl oxime ethers with 5 mol % of Cu(OTf)(2) in chlorobenzene at reflux gave 4-arylmethylisoxazoles in good to excellent yields via the sequential intramolecular addition of the oxime moiety to the alkyne with subsequent 1,3-migration of the arylmethyl group. Oximes 34-39 POU class 2 homeobox 2 Homo sapiens 63-72 23461011-0 2013 [Studying kinetics of oxime-induced reactivation of malathion-inhibited cholinesterase]. Oximes 22-27 butyrylcholinesterase Homo sapiens 72-86 23461011-1 2013 The kinetics of oxime-induced reactivation of malathion-inhibited cholinesterase has been experimentally studied in vitro. Oximes 16-21 butyrylcholinesterase Homo sapiens 66-80 23176543-1 2013 INTRODUCTION: The more or less systematic studies on the specific activity of oximes as reactivators of acetylcholinesterase (AChE) inhibited by organophosphorus (OP) compounds provide a panoramic image of their pharmacological and toxicological profiles. Oximes 78-84 acetylcholinesterase (Cartwright blood group) Homo sapiens 104-124 23176543-1 2013 INTRODUCTION: The more or less systematic studies on the specific activity of oximes as reactivators of acetylcholinesterase (AChE) inhibited by organophosphorus (OP) compounds provide a panoramic image of their pharmacological and toxicological profiles. Oximes 78-84 acetylcholinesterase (Cartwright blood group) Homo sapiens 126-130 23176543-5 2013 The non-homogenous distribution of oximes versus OP in tissues was considered and correlated with the highly variable AChE reactivation at both peripheral and central levels. Oximes 35-41 acetylcholinesterase (Cartwright blood group) Homo sapiens 118-122 22703537-11 2012 In conclusion, our work demonstrated that the newly synthesised oximes were able to reactivate not only human erythrocyte AChE but also human plasma BChE, which could represent an advantage in the treatment of OP compounds poisoning. Oximes 64-70 acetylcholinesterase (Cartwright blood group) Homo sapiens 122-126 22703537-11 2012 In conclusion, our work demonstrated that the newly synthesised oximes were able to reactivate not only human erythrocyte AChE but also human plasma BChE, which could represent an advantage in the treatment of OP compounds poisoning. Oximes 64-70 butyrylcholinesterase Homo sapiens 149-153 23047286-4 2012 The incorporation of oxime ethers on the carbonyl portion of the benzoyl group can bring the PPARalpha/gamma potency ratio equal to or slightly greater than one, as is the case for compounds 20 c and 21 a. Oximes 21-26 peroxisome proliferator activated receptor alpha Mus musculus 93-102 23136681-13 2004 synthesized two conjugates, [(18)F]-5 and [(18)F]-8, by conjugating [(18)F]FDG with folate and methotrexate (MTX), respectively, using the readily available oxime-reactive [(18)F]FDG building block (1). Oximes 157-162 metaxin 1 Homo sapiens 109-112 22437842-1 2012 The reactivation of organophosphorus compound (OP)-inhibited acetylcholinesterase (AChE) by oximes is inadequate in case of different OP nerve agents. Oximes 92-98 acetylcholinesterase (Cartwright blood group) Homo sapiens 61-81 22437842-1 2012 The reactivation of organophosphorus compound (OP)-inhibited acetylcholinesterase (AChE) by oximes is inadequate in case of different OP nerve agents. Oximes 92-98 acetylcholinesterase (Cartwright blood group) Homo sapiens 83-87 22437842-4 2012 In part, marked differences in affinity and reactivity of the investigated oximes toward OP-inhibited human AChE were recorded. Oximes 75-81 acetylcholinesterase (Cartwright blood group) Homo sapiens 108-112 22561105-1 2012 Inhibition of acetylcholinesterase (AChE) is the main toxic mechanism of organophosphorus compounds (OP) and reactivation of OP-inhibited AChE by oximes is a mainstay of antidotal treatment. Oximes 146-152 acetylcholinesterase (Cartwright blood group) Homo sapiens 36-40 22561105-1 2012 Inhibition of acetylcholinesterase (AChE) is the main toxic mechanism of organophosphorus compounds (OP) and reactivation of OP-inhibited AChE by oximes is a mainstay of antidotal treatment. Oximes 146-152 acetylcholinesterase (Cartwright blood group) Homo sapiens 138-142 22649796-2 2012 However, numerous in vitro and in vivo studies demonstrated a limited ability of these oximes to reactivate acetylcholinesterase (AChE) inhibited by different OP pesticides and nerve agents. Oximes 87-93 acetylcholinesterase (Cartwright blood group) Homo sapiens 108-128 22649796-2 2012 However, numerous in vitro and in vivo studies demonstrated a limited ability of these oximes to reactivate acetylcholinesterase (AChE) inhibited by different OP pesticides and nerve agents. Oximes 87-93 acetylcholinesterase (Cartwright blood group) Homo sapiens 130-134 22649796-3 2012 New oximes were mostly tested for their therapeutic efficacy by using different animal models and for their reactivating potency with AChE from different species. Oximes 4-10 acetylcholinesterase (Cartwright blood group) Homo sapiens 134-138 22649796-5 2012 Now, we found it tempting to determine the reactivation kinetics of a series of bispyridinium oximes bearing one or two oxime groups at different positions and having an oxybismethylene or a trimethylene linker under identical conditions with human AChE inhibited by structurally different OP. Oximes 94-99 acetylcholinesterase (Cartwright blood group) Homo sapiens 249-253 22649796-7 2012 Hence, these and previous data emphasize the necessity for thorough kinetic investigations of OP-oxime-AChE interactions and underline the difficulty to develop a broad spectrum oxime reactivator which is efficient against structurally different OP inhibitors. Oximes 97-102 acetylcholinesterase (Cartwright blood group) Homo sapiens 103-107 22343626-2 2012 Starting with the initial lead oxime RS41A identified in our earlier study and extending to the azepine analog RS194B, reactivation rates for OP-hAChE conjugates formed by sarin, cyclosarin, VX, paraoxon, and tabun are enhanced severalfold in vitro. Oximes 31-36 acetylcholinesterase (Cartwright blood group) Homo sapiens 145-150 23115436-6 2012 Following decontamination, depending on the severity of intoxication the administration of atropine to counteract muscarinic over-stimulation, and an oxime to reactivate acetyl cholinesterase are indicated. Oximes 150-155 butyrylcholinesterase Homo sapiens 177-191 22292814-0 2012 Identification of high affinity polo-like kinase 1 (Plk1) polo-box domain binding peptides using oxime-based diversification. Oximes 97-102 polo like kinase 1 Homo sapiens 32-50 22292814-0 2012 Identification of high affinity polo-like kinase 1 (Plk1) polo-box domain binding peptides using oxime-based diversification. Oximes 97-102 polo like kinase 1 Homo sapiens 52-56 22292814-1 2012 In an effort to develop improved binding antagonists of the polo-like kinase 1 (Plk1) polo-box domain (PBD), we optimized interactions of the known high affinity 5-mer peptide PLHSpT using oxime-based post solid-phase peptide diversification of the N-terminal Pro residue. Oximes 189-194 polo like kinase 1 Homo sapiens 60-78 22292814-1 2012 In an effort to develop improved binding antagonists of the polo-like kinase 1 (Plk1) polo-box domain (PBD), we optimized interactions of the known high affinity 5-mer peptide PLHSpT using oxime-based post solid-phase peptide diversification of the N-terminal Pro residue. Oximes 189-194 polo like kinase 1 Homo sapiens 80-84 22343626-6 2012 The enhanced intrinsic reactivity against the OP-AChE target combined with favorable pharmacokinetic properties resulted in great improvement of antidotal properties of RS194B compared with RS41A and the standard peripherally active oxime, 2-pyridinealdoxime methiodide. Oximes 233-238 acetylcholinesterase Mus musculus 49-53 22385173-7 2012 Analysis of solvation free energy indicates high solute polarization and dispersion energies of the oximes to be particularly critical for the tabun- inhibited mouse AChE, whereas lower values of these properties favor reactivation against other OP agents, such as soman, sarin and cyclosarin. Oximes 100-106 acetylcholinesterase Mus musculus 166-170 22230262-0 2012 Comparative kinetics of organophosphates and oximes with erythrocyte, muscle and brain acetylcholinesterase. Oximes 45-51 acetylcholinesterase (Cartwright blood group) Homo sapiens 87-107 22230262-1 2012 There is an ongoing debate whether oximes can effectively counteract the effects of organophosphorus compounds (OP) on brain acetylcholinesterase (AChE) activity and whether there are differences in the kinetic properties of brain and erythrocyte AChE. Oximes 35-41 acetylcholinesterase (Cartwright blood group) Homo sapiens 125-145 22230262-1 2012 There is an ongoing debate whether oximes can effectively counteract the effects of organophosphorus compounds (OP) on brain acetylcholinesterase (AChE) activity and whether there are differences in the kinetic properties of brain and erythrocyte AChE. Oximes 35-41 acetylcholinesterase (Cartwright blood group) Homo sapiens 147-151 22230262-7 2012 These data support the view that AChE from different tissue has similar kinetic properties and that brain AChE is comparably susceptible toward reactivation by oximes. Oximes 160-166 acetylcholinesterase (Cartwright blood group) Homo sapiens 106-110 22160885-5 2012 Plasma cholinesterase activity was higher in animals receiving enzyme and oxime before the organophosphates than in the oxime-only pretreated groups. Oximes 74-79 butyrylcholinesterase Homo sapiens 7-21 22160885-5 2012 Plasma cholinesterase activity was higher in animals receiving enzyme and oxime before the organophosphates than in the oxime-only pretreated groups. Oximes 120-125 butyrylcholinesterase Homo sapiens 7-21 21998030-2 2012 Being the key target of OP toxicity, AChE may serve as a valuable tool for diagnosis of OP exposure as well as for the investigation of the kinetics of interactions between OP and oximes. Oximes 180-186 acetylcholinesterase (Cartwright blood group) Homo sapiens 37-41 22125290-1 2012 OBJECTIVES: Oximes such as pralidoxime (2-PAM) are essential antidotes for life-threatening organophosphate poisoning. Oximes 12-18 peptidylglycine alpha-amidating monooxygenase Homo sapiens 42-45 22309910-1 2012 We earlier reported an in silico pharmacophore model for reactivation of oximes to tabun-inhibited AChE. Oximes 73-79 acetylcholinesterase (Cartwright blood group) Homo sapiens 99-103 22309910-2 2012 Since DFP (diisopropylfluorophosphate) like tabun is a G-agent simulator, we utilized the model as a rational strategy to discover non-oxime reactivators of DFP-inhibited AChE in this study. Oximes 135-140 acetylcholinesterase (Cartwright blood group) Homo sapiens 171-175 22309910-4 2012 The procedure led us to identify several potent non-oxime compounds that reactivate DFP-inhibited AChE. Oximes 52-57 acetylcholinesterase (Cartwright blood group) Homo sapiens 98-102 22447833-1 2012 Oxime HI-6 is an efficient reactivator of the acetylcholinesterase inhibited by organophosphorous nerve agents. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 46-66 22731788-1 2012 We have applied a theoretical methodology, previously developed to evaluate the association and kinetic reactivation constants of oximes, comparing theoretical data obtained for human acetylcholinesterase (HsAChE) with in vitro results from Mus musculus AChE (MmAChE) previously reported in the literature. Oximes 130-136 acetylcholinesterase (Cartwright blood group) Homo sapiens 184-204 22280363-5 2012 SAR around our focused library revealed a number of features, most notably the oxime functionality to be important to this selectivity. Oximes 79-84 sarcosine dehydrogenase Homo sapiens 0-3 22696932-2 2012 In vivo determined percentage of reactivation of cyclosarin-inhibited blood and tissue acetylcholinesterase in poisoned rats showed that the reactivating efficacy of both combinations of oximes is slightly higher than the reactivating efficacy of the most effective individual oxime in blood, diaphragm as well as in brain. Oximes 187-193 acetylcholinesterase Rattus norvegicus 87-107 22696932-2 2012 In vivo determined percentage of reactivation of cyclosarin-inhibited blood and tissue acetylcholinesterase in poisoned rats showed that the reactivating efficacy of both combinations of oximes is slightly higher than the reactivating efficacy of the most effective individual oxime in blood, diaphragm as well as in brain. Oximes 187-192 acetylcholinesterase Rattus norvegicus 87-107 22754334-5 2012 CYP83A1 mainly metabolizes the aliphatic oximes to form aliphatic glucosinolate and CYP83B1 mostly catalyzes aromatic oximes to synthesis corresponding substrates for aromatic and indolic glucosinolates. Oximes 41-47 cytochrome P450 83A1 Brassica rapa 0-7 22754334-5 2012 CYP83A1 mainly metabolizes the aliphatic oximes to form aliphatic glucosinolate and CYP83B1 mostly catalyzes aromatic oximes to synthesis corresponding substrates for aromatic and indolic glucosinolates. Oximes 41-47 cytochrome P450, family 83, subfamily B, polypeptide 1 Arabidopsis thaliana 84-91 22731788-1 2012 We have applied a theoretical methodology, previously developed to evaluate the association and kinetic reactivation constants of oximes, comparing theoretical data obtained for human acetylcholinesterase (HsAChE) with in vitro results from Mus musculus AChE (MmAChE) previously reported in the literature. Oximes 130-136 acetylcholinesterase Mus musculus 208-212 23038000-8 2012 The activation of MPO and increase in IL-1, IL-6, TNF-alpha and IFN-gamma levels induced by CdCl(2) were also reduced by oxime. Oximes 121-126 myeloperoxidase Mus musculus 18-21 23038000-8 2012 The activation of MPO and increase in IL-1, IL-6, TNF-alpha and IFN-gamma levels induced by CdCl(2) were also reduced by oxime. Oximes 121-126 interleukin 1 complex Mus musculus 38-42 23038000-8 2012 The activation of MPO and increase in IL-1, IL-6, TNF-alpha and IFN-gamma levels induced by CdCl(2) were also reduced by oxime. Oximes 121-126 interleukin 6 Mus musculus 44-48 23038000-8 2012 The activation of MPO and increase in IL-1, IL-6, TNF-alpha and IFN-gamma levels induced by CdCl(2) were also reduced by oxime. Oximes 121-126 tumor necrosis factor Mus musculus 50-59 23038000-8 2012 The activation of MPO and increase in IL-1, IL-6, TNF-alpha and IFN-gamma levels induced by CdCl(2) were also reduced by oxime. Oximes 121-126 interferon gamma Mus musculus 64-73 23038000-9 2012 IL-10, which was reduced by cadmium, was restored by oxime administration. Oximes 53-58 interleukin 10 Mus musculus 0-5 22360668-6 2012 The review describes the evaluation of the potency of newly developed oximes (especially the oxime K203) or combinations of oximes to reactivate nerve agent-inhibited acetylcholinesterase and to counteract the acute toxicity of nerve agents in comparison with single commonly used oxime (obidoxime, trimedoxime or HI-6). Oximes 70-76 acetylcholinesterase (Cartwright blood group) Homo sapiens 167-187 22360668-6 2012 The review describes the evaluation of the potency of newly developed oximes (especially the oxime K203) or combinations of oximes to reactivate nerve agent-inhibited acetylcholinesterase and to counteract the acute toxicity of nerve agents in comparison with single commonly used oxime (obidoxime, trimedoxime or HI-6). Oximes 124-130 acetylcholinesterase (Cartwright blood group) Homo sapiens 167-187 22360668-6 2012 The review describes the evaluation of the potency of newly developed oximes (especially the oxime K203) or combinations of oximes to reactivate nerve agent-inhibited acetylcholinesterase and to counteract the acute toxicity of nerve agents in comparison with single commonly used oxime (obidoxime, trimedoxime or HI-6). Oximes 70-75 acetylcholinesterase (Cartwright blood group) Homo sapiens 167-187 22808117-0 2012 Energetics of Ortho-7 (oxime drug) translocation through the active-site gorge of tabun conjugated acetylcholinesterase. Oximes 23-28 acetylcholinesterase (Cartwright blood group) Homo sapiens 99-119 22808117-1 2012 Oxime drugs translocate through the 20 A active-site gorge of acetylcholinesterase in order to liberate the enzyme from organophosphorus compounds" (such as tabun) conjugation. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 62-82 22052741-5 2011 By incorporating artificial amino acids that carry an azide (Aha) or an alkyne (Plk) in their side chains, into ubiquitin (Ub) and PCNA, respectively, we were able to link the two proteins site-specifically by the Cu(I) -catalyzed azide-alkyne cycloaddition. Oximes 61-64 proliferating cell nuclear antigen Homo sapiens 131-135 21989207-3 2011 Pro-2-PAM (1-methyl-1,6-dihydropyridine-2-carbaldoxime), a pro-drug of 2-PAM, due to higher hydrophobicity, penetrates the BBB better but must be oxidized to 2-PAM, the active form of the oxime to reactivate CNS AChE in order to abrogate seizures. Oximes 49-54 peptidyl-glycine alpha-amidating monooxygenase Cavia porcellus 6-9 21989207-3 2011 Pro-2-PAM (1-methyl-1,6-dihydropyridine-2-carbaldoxime), a pro-drug of 2-PAM, due to higher hydrophobicity, penetrates the BBB better but must be oxidized to 2-PAM, the active form of the oxime to reactivate CNS AChE in order to abrogate seizures. Oximes 49-54 peptidyl-glycine alpha-amidating monooxygenase Cavia porcellus 73-76 21989207-3 2011 Pro-2-PAM (1-methyl-1,6-dihydropyridine-2-carbaldoxime), a pro-drug of 2-PAM, due to higher hydrophobicity, penetrates the BBB better but must be oxidized to 2-PAM, the active form of the oxime to reactivate CNS AChE in order to abrogate seizures. Oximes 49-54 peptidyl-glycine alpha-amidating monooxygenase Cavia porcellus 73-76 21989207-3 2011 Pro-2-PAM (1-methyl-1,6-dihydropyridine-2-carbaldoxime), a pro-drug of 2-PAM, due to higher hydrophobicity, penetrates the BBB better but must be oxidized to 2-PAM, the active form of the oxime to reactivate CNS AChE in order to abrogate seizures. Oximes 49-54 acetylcholinesterase Cavia porcellus 212-216 21799476-6 2011 Standard treatment involves the administration of intravenous atropine and an oxime to counteract acetylcholinesterase inhibition at the synapse, but the usefulness of oximes is still debated. Oximes 78-83 acetylcholinesterase (Cartwright blood group) Homo sapiens 98-118 21930118-1 2011 Treatment of poisoning by highly toxic organophosphorus compounds (OP) with atropine and an acetylcholinesterase (AChE) reactivator (oxime) is of limited effectiveness in case of different nerve agents and pesticides. Oximes 133-138 acetylcholinesterase (Cartwright blood group) Homo sapiens 92-112 21723318-11 2011 This indicates that peripheral and central AChE activities are not necessarily correlated after the treatment of OP compounds and/or oximes, which should be taken into account in the diagnosis and management of OP-exposed humans. Oximes 133-139 acetylcholinesterase (Cartwright blood group) Homo sapiens 43-47 21983245-0 2011 Potential of two new oximes in reactivate human acetylcholinesterase and butyrylcholinesterase inhibited by organophosphate compounds: an in vitro study. Oximes 21-27 acetylcholinesterase (Cartwright blood group) Homo sapiens 48-68 21983245-0 2011 Potential of two new oximes in reactivate human acetylcholinesterase and butyrylcholinesterase inhibited by organophosphate compounds: an in vitro study. Oximes 21-27 butyrylcholinesterase Homo sapiens 73-94 21983245-2 2011 Oximes are compounds generally used to reverse the ChE inhibition caused by OP agents. Oximes 0-6 butyrylcholinesterase Homo sapiens 51-54 21983245-3 2011 In this study, we compared the in vitro reactivation potency of two new oximes (oxime 1: butane-2,3-dionethiosemicarbazone; oxime 2: 3-(phenylhydrazono) butan-2-one) against the inhibition on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities induced by chlorpyrifos, diazinon and malathion. Oximes 72-77 acetylcholinesterase (Cartwright blood group) Homo sapiens 192-212 21983245-3 2011 In this study, we compared the in vitro reactivation potency of two new oximes (oxime 1: butane-2,3-dionethiosemicarbazone; oxime 2: 3-(phenylhydrazono) butan-2-one) against the inhibition on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities induced by chlorpyrifos, diazinon and malathion. Oximes 72-77 acetylcholinesterase (Cartwright blood group) Homo sapiens 214-218 21983245-3 2011 In this study, we compared the in vitro reactivation potency of two new oximes (oxime 1: butane-2,3-dionethiosemicarbazone; oxime 2: 3-(phenylhydrazono) butan-2-one) against the inhibition on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities induced by chlorpyrifos, diazinon and malathion. Oximes 72-77 butyrylcholinesterase Homo sapiens 224-245 21983245-3 2011 In this study, we compared the in vitro reactivation potency of two new oximes (oxime 1: butane-2,3-dionethiosemicarbazone; oxime 2: 3-(phenylhydrazono) butan-2-one) against the inhibition on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities induced by chlorpyrifos, diazinon and malathion. Oximes 72-77 butyrylcholinesterase Homo sapiens 247-251 21983245-8 2011 However, both newly developed oximes achieved similar reactivations rates that pralidoxime for chlorpyrifos and diazinon-inhibited AChE. Oximes 30-36 acetylcholinesterase (Cartwright blood group) Homo sapiens 131-135 21983245-10 2011 We conclude that both newly developed oximes seem to be promising reactivators of OP-inhibited AChE. Oximes 38-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 95-99 21930118-1 2011 Treatment of poisoning by highly toxic organophosphorus compounds (OP) with atropine and an acetylcholinesterase (AChE) reactivator (oxime) is of limited effectiveness in case of different nerve agents and pesticides. Oximes 133-138 acetylcholinesterase (Cartwright blood group) Homo sapiens 114-118 21504785-0 2011 Peripheral site ligand conjugation to a non-quaternary oxime enhances reactivation of nerve agent-inhibited human acetylcholinesterase. Oximes 55-60 acetylcholinesterase (Cartwright blood group) Homo sapiens 114-134 21504785-2 2011 Conversely, non-ionic oxime reactivators often suffer from a lack of reactivating potency due to a low affinity for the active site of AChE. Oximes 22-27 acetylcholinesterase (Cartwright blood group) Homo sapiens 135-139 21726608-1 2011 The standard treatment of intoxication with organophosphorus (OP) compounds includes the administration of oximes acting as acetylcholinesterase (AChE) reactivating antidotes. Oximes 107-113 acetylcholinesterase (Cartwright blood group) Homo sapiens 124-144 21730071-5 2011 Here, we characterize 10 human (h) AChE mutants that, when coupled with an oxime, give rise to catalytic reactivation and aging resistance of the soman conjugate. Oximes 75-80 acetylcholinesterase (Cartwright blood group) Homo sapiens 35-39 21726608-1 2011 The standard treatment of intoxication with organophosphorus (OP) compounds includes the administration of oximes acting as acetylcholinesterase (AChE) reactivating antidotes. Oximes 107-113 acetylcholinesterase (Cartwright blood group) Homo sapiens 146-150 21726608-7 2011 In vitro testing of the nanoparticulate oxime formulations in primary porcine brain capillary endothelial cells (pBCEC) demonstrated an up to two times higher reactivation of OP-inhibited AChE than the free oximes. Oximes 40-45 acetylcholinesterase (Cartwright blood group) Homo sapiens 188-192 21803135-2 2011 To achieve this goal, oximes are administered for reactivation of inhibited acetylcholinesterase (AChE). Oximes 22-28 acetylcholinesterase (Cartwright blood group) Homo sapiens 76-96 21803135-2 2011 To achieve this goal, oximes are administered for reactivation of inhibited acetylcholinesterase (AChE). Oximes 22-28 acetylcholinesterase (Cartwright blood group) Homo sapiens 98-102 21641693-3 2011 In addition, oxime Ih displayed cytotoxicity against KB cells with an IC(50) value of 0.17 muM which is about 10 times stronger than the ellipticine. Oximes 13-18 latexin Homo sapiens 91-94 21730071-0 2011 Oxime-assisted acetylcholinesterase catalytic scavengers of organophosphates that resist aging. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 15-35 21671403-0 2011 Oxime-based click chemistry in the development of 3-isoxazolecarboxylic acid containing inhibitors of Yersinia pestis protein tyrosine phosphatase, YopH. Oximes 0-5 YopH Yersinia pestis 148-152 21605992-2 2011 Oximes are used as potential reactivators of OP-inhibited AChE due to their alpha-effect nucleophilic reactivity. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 58-62 21524678-1 2011 The oximes pralidoxime (2-PAM), its dimethanesulphonate salt derivative P2S, and obidoxime (toxogonin) are currently licensed and fielded for the treatment of chemical warfare (CW) organophosphorous (OP) nerve agent poisoning. Oximes 4-10 peptidylglycine alpha-amidating monooxygenase Homo sapiens 26-29 21600273-3 2011 An explanation for limited penetration might be that oximes are substrates for the active P-glycoprotein (Pgp) efflux transporter located in the BBB. Oximes 53-59 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 90-104 21600273-3 2011 An explanation for limited penetration might be that oximes are substrates for the active P-glycoprotein (Pgp) efflux transporter located in the BBB. Oximes 53-59 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 106-109 21688786-2 2011 The reactions proceeded with both of anti- and syn-isomers of oximes with a wide scope of substituents. Oximes 62-68 synemin Homo sapiens 47-50 21530621-3 2011 Although successful treatment of OP poisoning can be obtained through decontamination and/or oxime reactivation of agent-inhibited cholinesterase, medical countermeasures that increase the therapeutic window for these measures would be of benefit. Oximes 93-98 cholinesterase Sus scrofa 131-145 21574642-5 2011 First, we identified an optimized oxime conjugation strategy under which complex dendrimers can be fully decorated not only with model peptides, but also with recombinant proteins (insulin was taken as an example). Oximes 34-39 insulin Homo sapiens 181-188 21493754-10 2011 Protein expression of ACHE nonsynonymous variant D134H (SNP6) is impaired: this variant shows compromised stability and altered rates of organophosphate inhibition and oxime-assisted reactivation. Oximes 168-173 acetylcholinesterase (Cartwright blood group) Homo sapiens 22-26 21464125-4 2011 Reactivation capacities of novel oximes are rank ordered by their relative reactivation rate constants at 0.67 mm compared with 2-pyridinealdoxime methiodide for reactivation of four organophosphate (sarin, cyclosarin, VX, and paraoxon) conjugates of human acetylcholinesterase (hAChE). Oximes 33-39 acetylcholinesterase (Cartwright blood group) Homo sapiens 279-284 21464125-6 2011 The 10 best reactivating oximes, predominantly hydroxyimino acetamide derivatives (for hAChE) and imidazole-containing aldoximes (for hBChE) also exhibited reasonable activity in the reactivation of tabun conjugates. Oximes 25-31 acetylcholinesterase (Cartwright blood group) Homo sapiens 87-92 21464125-6 2011 The 10 best reactivating oximes, predominantly hydroxyimino acetamide derivatives (for hAChE) and imidazole-containing aldoximes (for hBChE) also exhibited reasonable activity in the reactivation of tabun conjugates. Oximes 25-31 butyrylcholinesterase Homo sapiens 134-139 21195145-4 2011 Oxime-type AChE reactivators pralidoxime, obidoxime, trimedoxime, methoxime and HI-6 were tested for their potential to affect the activity of monoamine oxidase of type A (MAO-A) and type B (MAO-B) in crude mitochondrial fraction of pig brains. Oximes 0-5 acetylcholinesterase (Yt blood group) Sus scrofa 11-15 21417297-6 2011 These somehow contradictory results were finally rationalized by a computational assisted SAR, which gave us the chance to understand how the oxime derivatives interact with the catalytic site and justify the observed activity profile. Oximes 142-147 sarcosine dehydrogenase Homo sapiens 90-93 21367426-3 2011 Results confirmed that (i) the TMS oxime-ether derivatives of the keto steroids provide from 1.40 times (gestodene) up to 4.25 times (norethisterone) higher responses compared to their TMS-ether ones, and (ii) the distribution of syn/anti oximes is characteristic to the ketosteroid species examined. Oximes 35-40 synemin Homo sapiens 230-233 20807085-1 2011 The standard treatment of poisoning by organophosphorus compounds (OP) includes the reversible muscarine receptor antagonist atropine and oximes for the reactivation of OP-inhibited acetylcholinesterase (AChE). Oximes 138-144 acetylcholinesterase (Cartwright blood group) Homo sapiens 204-208 20807085-4 2011 These constants can be used to calculate reactivation velocities and oxime concentrations necessary for the reactivation of a desired fraction of inhibited AChE. Oximes 69-74 acetylcholinesterase (Cartwright blood group) Homo sapiens 156-160 20807085-7 2011 Hereby, it has to be taken into account that an increase of affinity to OP-inhibited AChE is generally accompanied by an increased affinity to native AChE and subsequent reduction in oxime tolerance. Oximes 183-188 acetylcholinesterase (Cartwright blood group) Homo sapiens 85-89 20807085-8 2011 Hence, future developments of more effective oximes should consider kinetic demands by attempting to achieve a certain level of reactivity and affinity, preferentially towards OP-inhibited AChE. Oximes 45-51 acetylcholinesterase (Cartwright blood group) Homo sapiens 189-193 21402092-2 2011 However, successful oxime treatment in soman poisoning is limited due to rapid aging of phosphylated acetylcholinesterase (AChE). Oximes 20-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 101-121 21402092-2 2011 However, successful oxime treatment in soman poisoning is limited due to rapid aging of phosphylated acetylcholinesterase (AChE). Oximes 20-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 123-127 21195145-4 2011 Oxime-type AChE reactivators pralidoxime, obidoxime, trimedoxime, methoxime and HI-6 were tested for their potential to affect the activity of monoamine oxidase of type A (MAO-A) and type B (MAO-B) in crude mitochondrial fraction of pig brains. Oximes 0-5 monoamine oxidase A Sus scrofa 143-170 21251822-0 2011 Non-oxime inhibitors of B-Raf(V600E) kinase. Oximes 4-9 Braf transforming gene Mus musculus 24-29 21328273-2 2011 Standard treatment involves administration of intravenous atropine and oxime to reactivate inhibited acetylcholinesterase. Oximes 71-76 acetylcholinesterase (Cartwright blood group) Homo sapiens 101-121 21080696-0 2010 Enantioselective conjugate addition of oximes to trisubstituted beta-nitroacrylates: an organocatalytic approach to beta(2,2)-amino acid derivatives. Oximes 39-45 potassium calcium-activated channel subfamily M regulatory beta subunit 2 Homo sapiens 116-124 20569082-3 2011 The reactivation efficacy of the oximes was estimated on the rats exposed to tabun, atropine and a reactivator of AChE. Oximes 33-39 acetylcholinesterase Rattus norvegicus 114-118 20688148-3 2011 The oxime 3c exhibited 45% regeneration of inhibited hAChE, in comparison to 34% and 24% regeneration by 2-PAM and obidoxime, respectively, at a concentration of 10(-3) M within 10 min. Oximes 4-9 acetylcholinesterase (Cartwright blood group) Homo sapiens 53-58 20688148-6 2011 This method involving the in vitro reactivation of inhibited hAChE may be useful for the screening of new oximes as reactivators. Oximes 106-112 acetylcholinesterase (Cartwright blood group) Homo sapiens 61-66 21195611-2 2011 A novel series of oxime containing benzyl-1,3-dioxane-r-2-carboxylic acid derivatives (6a-k) were designed as selective PPARalpha agonists, through bioisosteric modification in the lipophilic tail region of PPARalpha/gamma dual agonist. Oximes 18-23 peroxisome proliferator activated receptor alpha Homo sapiens 120-129 21195611-2 2011 A novel series of oxime containing benzyl-1,3-dioxane-r-2-carboxylic acid derivatives (6a-k) were designed as selective PPARalpha agonists, through bioisosteric modification in the lipophilic tail region of PPARalpha/gamma dual agonist. Oximes 18-23 peroxisome proliferator activated receptor alpha Homo sapiens 207-216 21195611-6 2011 Together, these results confirm discovery of novel series of oxime based selective PPARalpha agonists for the safe and effective treatment of various metabolic disorders. Oximes 61-66 peroxisome proliferator activated receptor alpha Homo sapiens 83-92 21215640-0 2011 Effect of structurally constrained oxime-ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists. Oximes 35-40 peroxisome proliferator activated receptor alpha Homo sapiens 57-61 21215640-0 2011 Effect of structurally constrained oxime-ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists. Oximes 35-40 peroxisome proliferator activated receptor alpha Homo sapiens 125-129 21215640-5 2011 These results support our hypothesis that the introduction of structurally constrained oxime-ether linker between lipophilic tail and acidic head plays an important role in modulating subtype selectivity and subsequently led to the discovery of potent PPAR-pan agonists. Oximes 87-92 peroxisome proliferator activated receptor alpha Homo sapiens 252-256 21712782-2 2011 Various types of oximes reactivate AChE and are commonly used as antidotes against organophosphates (pesticides, nerve agents). Oximes 17-23 acetylcholinesterase (Yt blood group) Sus scrofa 35-39 21117832-0 2011 The oxime pro-2-PAM provides minimal protection against the CNS effects of the nerve agents sarin, cyclosarin, and VX in guinea pigs. Oximes 4-9 peptidyl-glycine alpha-amidating monooxygenase Cavia porcellus 10-19 20971170-0 2011 Kinetic analysis of interactions of paraoxon and oximes with human, Rhesus monkey, swine, rabbit, rat and guinea pig acetylcholinesterase. Oximes 49-55 acetylcholinesterase Cavia porcellus 117-137 20971170-1 2011 Previous in vitro studies showed marked species differences in the reactivating efficiency of oximes between human and animal acetylcholinesterase (AChE) inhibited by organophosphorus (OP) nerve agents. Oximes 94-100 acetylcholinesterase (Cartwright blood group) Homo sapiens 126-146 20971170-1 2011 Previous in vitro studies showed marked species differences in the reactivating efficiency of oximes between human and animal acetylcholinesterase (AChE) inhibited by organophosphorus (OP) nerve agents. Oximes 94-100 acetylcholinesterase (Cartwright blood group) Homo sapiens 148-152 21112787-0 2011 Peripheral site ligand-oxime conjugates: A novel concept towards reactivation of nerve agent-inhibited human acetylcholinesterase. Oximes 23-28 acetylcholinesterase (Cartwright blood group) Homo sapiens 109-129 21954536-5 2011 Application of oxime reactivator enable return of AChE activity and full suppression of intoxication. Oximes 15-20 acetylcholinesterase Rattus norvegicus 50-54 21673941-0 2011 In vitro ability of currently available oximes to reactivate organophosphate pesticide-inhibited human acetylcholinesterase and butyrylcholinesterase. Oximes 40-46 acetylcholinesterase (Cartwright blood group) Homo sapiens 103-123 21673941-2 2011 We also tested reactivation of human butyrylcholinesterase (BChE) with the aim of finding a potent oxime, suitable to serve as a "pseudocatalytic" bioscavenger in combination with this enzyme. Oximes 99-104 butyrylcholinesterase Homo sapiens 60-64 21673941-6 2011 In the case of methamidophos-inhibited AChE, the lower oxime concentration (10(-5) M) had higher reactivation ability than the 10(-4) M concentration. Oximes 55-60 acetylcholinesterase (Cartwright blood group) Homo sapiens 39-43 21673941-7 2011 Therefore, we evaluated the reactivation ability of obidoxime in a concentration range of 10(-3)-10(-7) M. The reactivation of methamidophos-inhibited AChE with different obidoxime concentrations resulted in a bell shaped curve with maximum reactivation at 10(-5) M. In the case of BChE, no reactivator exceeded 15% reactivation ability and therefore none of the oximes can be recommended as a candidate for "pseudocatalytic" bioscavengers with BChE. Oximes 363-369 acetylcholinesterase (Cartwright blood group) Homo sapiens 151-155 21151975-4 2010 The standard treatment of OP poisoning includes a combination of a muscarinic antagonist and an AChE reactivator (oxime). Oximes 114-119 acetylcholinesterase (Cartwright blood group) Homo sapiens 96-100 20888357-8 2010 Due to the high reactivity of MMB-4 a rapid reactivation of inhibited AChE can be anticipated at adequate oxime concentrations which are substantially higher compared to HI-6. Oximes 106-111 acetylcholinesterase (Cartwright blood group) Homo sapiens 70-74 21151975-8 2010 In general, the nanoparticulate transported oximes achieved a better reactivation of OP-inhibited AChE than free oximes. Oximes 44-50 acetylcholinesterase (Cartwright blood group) Homo sapiens 98-102 21151975-8 2010 In general, the nanoparticulate transported oximes achieved a better reactivation of OP-inhibited AChE than free oximes. Oximes 113-119 acetylcholinesterase (Cartwright blood group) Homo sapiens 98-102 20510679-12 2010 Finally, these data emphasize the need to develop oximes with a higher selective affinity towards OP-inhibited hAChE in order to minimize possible side effects. Oximes 50-56 acetylcholinesterase (Cartwright blood group) Homo sapiens 111-116 20655881-2 2010 Oxime compounds used in nerve agent antidote regimen reactivate nerve agent-inhibited AChE and halt the development of this cholinergic crisis. Oximes 0-5 acetylcholinesterase Bos taurus 86-90 20655881-4 2010 To understand the mechanism for the differential activities of oximes toward AChE inhibited by diverse nerve agents in order to aid the design of new broad-spectrum AChE reactivators, we undertook site-directed mutagenesis and molecular modeling studies. Oximes 63-69 acetylcholinesterase Bos taurus 77-81 20655881-4 2010 To understand the mechanism for the differential activities of oximes toward AChE inhibited by diverse nerve agents in order to aid the design of new broad-spectrum AChE reactivators, we undertook site-directed mutagenesis and molecular modeling studies. Oximes 63-69 acetylcholinesterase Bos taurus 165-169 20688049-11 2010 Imoproxifan bound to hH(3)R and rH(3)R in E-configuration, which represents the trans-isomer of the oxime-moiety as determined in crystallization studies, and stabilized active hH(3)R-, but inactive rH(3)R-conformations. Oximes 100-105 histamine receptor H3 Homo sapiens 21-27 20635332-6 2010 It seems obvious that oximes are weakly penetrating the BBB, with minimal brain AChE reactivation (<5%) in important functional areas, such as the ponto-medullar. Oximes 22-28 acetylcholinesterase (Cartwright blood group) Homo sapiens 80-84 19883634-8 2010 Also oxime therapy in organophosphorus poisoning apparently gives perplexing results: Oximes are usually able to reactivate diethylphosphorylated AChE, but the efficiency may be occasionally markedly smaller than expected from kinetic data. Oximes 5-10 acetylcholinesterase (Cartwright blood group) Homo sapiens 146-150 19883634-8 2010 Also oxime therapy in organophosphorus poisoning apparently gives perplexing results: Oximes are usually able to reactivate diethylphosphorylated AChE, but the efficiency may be occasionally markedly smaller than expected from kinetic data. Oximes 86-92 acetylcholinesterase (Cartwright blood group) Homo sapiens 146-150 19883634-9 2010 Dimethylphosphorylated AChE is in general less amenable to oxime therapy, which largely fails in some cases of dimethoate poisoning where aging was much faster than expected from a dimethylphosphorylated enzyme. Oximes 59-64 acetylcholinesterase (Cartwright blood group) Homo sapiens 23-27 19917271-2 2010 The presently established acetylcholinesterase (AChE) reactivators (oximes), e.g. obidoxime and pralidoxime, are insufficient against a number of nerve agents and there is ongoing debate on the benefit of oxime treatment in human OP pesticide poisoning. Oximes 68-74 acetylcholinesterase (Cartwright blood group) Homo sapiens 26-46 19917271-2 2010 The presently established acetylcholinesterase (AChE) reactivators (oximes), e.g. obidoxime and pralidoxime, are insufficient against a number of nerve agents and there is ongoing debate on the benefit of oxime treatment in human OP pesticide poisoning. Oximes 68-74 acetylcholinesterase (Cartwright blood group) Homo sapiens 48-52 19917271-2 2010 The presently established acetylcholinesterase (AChE) reactivators (oximes), e.g. obidoxime and pralidoxime, are insufficient against a number of nerve agents and there is ongoing debate on the benefit of oxime treatment in human OP pesticide poisoning. Oximes 68-73 acetylcholinesterase (Cartwright blood group) Homo sapiens 26-46 19917271-2 2010 The presently established acetylcholinesterase (AChE) reactivators (oximes), e.g. obidoxime and pralidoxime, are insufficient against a number of nerve agents and there is ongoing debate on the benefit of oxime treatment in human OP pesticide poisoning. Oximes 68-73 acetylcholinesterase (Cartwright blood group) Homo sapiens 48-52 19917271-5 2010 Kinetic studies on the various interactions between erythrocyte AChE from various species, structurally different OP and different oximes provided a basis for the initial assessment of the ability of oximes to reactivate inhibited AChE. Oximes 200-206 acetylcholinesterase (Cartwright blood group) Homo sapiens 64-68 19917271-5 2010 Kinetic studies on the various interactions between erythrocyte AChE from various species, structurally different OP and different oximes provided a basis for the initial assessment of the ability of oximes to reactivate inhibited AChE. Oximes 200-206 acetylcholinesterase (Cartwright blood group) Homo sapiens 231-235 19917271-6 2010 In the present study, in vitro enzyme-kinetic and pharmacokinetic data from a minipig model of dimethoate poisoning and oxime treatment were used to calculate dynamic changes of AChE activities. Oximes 120-125 acetylcholinesterase (Cartwright blood group) Homo sapiens 178-182 20156430-10 2010 However, blood and diaphragm showed similar AChE activities in animals treated with either oxime, as both 2-PAM and pro-2-PAM are PNS active oximes. Oximes 91-96 acetylcholinesterase Cavia porcellus 44-48 20206154-2 2010 This can be improved by creating a pseudo-catalytic scavenger adding oximes as reactivators of inhibited exogenous BChE. Oximes 69-75 butyrylcholinesterase Homo sapiens 115-119 20156430-10 2010 However, blood and diaphragm showed similar AChE activities in animals treated with either oxime, as both 2-PAM and pro-2-PAM are PNS active oximes. Oximes 91-96 peptidyl-glycine alpha-amidating monooxygenase Cavia porcellus 108-111 20156430-10 2010 However, blood and diaphragm showed similar AChE activities in animals treated with either oxime, as both 2-PAM and pro-2-PAM are PNS active oximes. Oximes 91-96 peptidyl-glycine alpha-amidating monooxygenase Cavia porcellus 116-125 20156430-10 2010 However, blood and diaphragm showed similar AChE activities in animals treated with either oxime, as both 2-PAM and pro-2-PAM are PNS active oximes. Oximes 141-147 peptidyl-glycine alpha-amidating monooxygenase Cavia porcellus 116-125 20206154-3 2010 In order to improve the BChE bioscavenging function in tabun or paraoxon poisoning, we tested in vitro reactivation of phosphorylated human plasma BChE by bispyridinium oximes varying in the length and type of the linker between rings, and in the position of the oxime group on the ring. Oximes 169-174 butyrylcholinesterase Homo sapiens 147-151 20167212-4 2010 Combination of both oximes showed potentiation of their reactivation efficacy; this potentiation was expressed for peripheral AChE (blood, diaphragm) and some parts of the brain (pontomedullar area, frontal cortex); AChE in the basal ganglia was relatively resistant. Oximes 20-26 acetylcholinesterase Rattus norvegicus 126-130 20206154-4 2010 Among the tested oximes, the most potent reactivators of tabun-inhibited BChE were K117 [1,1"-(2,2"-oxybis(ethane-2,1-diyl))bis(4-hydroxyiminomethyl pyridinium) bromide] and K127 [4-carbamoyl-1-(2-(2-(4-(hydroxyiminomethyl) pyridinium-1-yl)ethoxy)ethyl)pyridinium bromide]. Oximes 17-23 butyrylcholinesterase Homo sapiens 73-77 20167212-4 2010 Combination of both oximes showed potentiation of their reactivation efficacy; this potentiation was expressed for peripheral AChE (blood, diaphragm) and some parts of the brain (pontomedullar area, frontal cortex); AChE in the basal ganglia was relatively resistant. Oximes 20-26 acetylcholinesterase Rattus norvegicus 216-220 20206154-7 2010 Using molecular mechanics, we performed docking of the oximes to tabun-inhibited BChE in order to discuss possible structural modifications of bispyridinium oximes to improve reactivation of phosphorylated BChE. Oximes 55-61 butyrylcholinesterase Homo sapiens 81-85 20206154-7 2010 Using molecular mechanics, we performed docking of the oximes to tabun-inhibited BChE in order to discuss possible structural modifications of bispyridinium oximes to improve reactivation of phosphorylated BChE. Oximes 55-61 butyrylcholinesterase Homo sapiens 206-210 20433814-5 2010 Current treatments for OP poisoning involve the administration of atropine, which blocks ACh receptors, and oximes, which reactivate AChE after inhibition. Oximes 108-114 acetylcholinesterase Cavia porcellus 133-137 20412789-0 2010 Interaction kinetics of oximes with native, phosphylated and aged human acetylcholinesterase. Oximes 24-30 acetylcholinesterase (Cartwright blood group) Homo sapiens 72-92 20433814-9 2010 Although guinea pigs historically have been used to test OP poisoning therapies, it has been found recently that guinea pig AChE is substantially more resistant to oxime-mediated reactivation than human AChE. Oximes 164-169 acetylcholinesterase Cavia porcellus 124-128 20412789-1 2010 Oximes are commonly used nucleophilic reactivators of alkyl phosphorylated and alkyl methylphosphonylated acetylcholinesterase (AChE) and butyrylcholinesterase. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 106-126 20433814-13 2010 To examine directly how these differences affect oxime-mediated reactivation of AChE after inhibition by OPs, human and guinea pig red blood cell ghosts were prepared and used as sources of AChE, and the relative capacity of several different oximes to reactivate each OP-inhibited AChE were determined. Oximes 49-54 acetylcholinesterase (Cartwright blood group) Homo sapiens 80-84 20412789-1 2010 Oximes are commonly used nucleophilic reactivators of alkyl phosphorylated and alkyl methylphosphonylated acetylcholinesterase (AChE) and butyrylcholinesterase. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 128-132 20600799-6 2010 Overall, the study reveals that the oxime 4P-2 may have therapeutic potential in the reactivation of human AChE inhibited by sarin. Oximes 36-41 acetylcholinesterase (Cartwright blood group) Homo sapiens 107-111 20412789-3 2010 In this study we determined kinetic constants for interaction of three triazole containing oximes with native human AChE, enzyme diethylphosphorylated by paraoxon, enzyme phosphonylated by VX and cyclosarin as well as enzyme aged upon phosphonylation by soman. Oximes 91-97 acetylcholinesterase (Cartwright blood group) Homo sapiens 116-120 20412789-4 2010 Stopped-flow kinetics of oxime interaction was monitored using quenching of intrinsic tryptophan fluorescence of AChE as an indicator of oxime binding. Oximes 25-30 acetylcholinesterase (Cartwright blood group) Homo sapiens 113-117 20412789-4 2010 Stopped-flow kinetics of oxime interaction was monitored using quenching of intrinsic tryptophan fluorescence of AChE as an indicator of oxime binding. Oximes 137-142 acetylcholinesterase (Cartwright blood group) Homo sapiens 113-117 20417629-1 2010 Catalytic activity of acetylcholinesterase (AChE; EC 3.1.1.7) was studied in the presence of oximes HI-6, K114, K127 and K203, and inhibition constants were determined for the reversible enzyme-inhibitor complex (K(I)). Oximes 93-99 acetylcholinesterase (Cartwright blood group) Homo sapiens 22-42 20417629-1 2010 Catalytic activity of acetylcholinesterase (AChE; EC 3.1.1.7) was studied in the presence of oximes HI-6, K114, K127 and K203, and inhibition constants were determined for the reversible enzyme-inhibitor complex (K(I)). Oximes 93-99 acetylcholinesterase (Cartwright blood group) Homo sapiens 44-48 20417629-3 2010 Molecular modelling of AChE-oxime complexes was used to determine amino acid residues of the active site involved in the interactions. Oximes 28-33 acetylcholinesterase (Cartwright blood group) Homo sapiens 23-27 20417629-6 2010 The weakest inhibitor, K127, also formed several hydrogen bonds with the active site residues, but due to its long linker it was more likely stabilized at the peripheral site (Tyr124), which could explain lower AChE affinity for this oxime. Oximes 234-239 acetylcholinesterase (Cartwright blood group) Homo sapiens 211-215 20406208-0 2010 In vitro reactivating effects of standard and newly developed oximes on malaoxon-inhibited mouse brain acetylcholinesterase. Oximes 62-68 acetylcholinesterase Mus musculus 103-123 20406208-2 2010 Human malathion poisoning has been treated with oximes (mainly pralidoxime) in an attempt to reactivate OP-inhibited acetylcholinesterase (AChE). Oximes 48-54 acetylcholinesterase Mus musculus 117-137 20406208-2 2010 Human malathion poisoning has been treated with oximes (mainly pralidoxime) in an attempt to reactivate OP-inhibited acetylcholinesterase (AChE). Oximes 48-54 acetylcholinesterase (Cartwright blood group) Homo sapiens 139-143 20406208-4 2010 In this study, we evaluated the in vitro potency of standards and newly developed oximes in reactivating malaoxon-inhibited AChE derived from mouse brain supernatants. Oximes 82-88 acetylcholinesterase Mus musculus 124-128 20623827-1 2010 The (1)H, (13)C and (15)N NMR studies have shown that the E and Z isomers of pyrrole-2-carbaldehyde oxime adopt preferable conformation with the syn orientation of the oxime group with respect to the pyrrole ring. Oximes 100-105 synemin Homo sapiens 145-148 20096273-1 2010 Oxime-induced reactivation of organophosphorus (OP) nerve agent-inhibited acetylcholinesterase (AChE) is a very important step for the treatment of nerve agent toxicity. Oximes 0-5 acetylcholinesterase Cavia porcellus 96-100 20096273-4 2010 Later these oximes were shown to rapidly reactivate GF- and VR-inhibited AChE as well. Oximes 12-18 acetylcholinesterase Cavia porcellus 73-77 20105433-5 2010 However, human AChE inhibited by certain OP is rather resistant to oxime-induced reactivation. Oximes 67-72 acetylcholinesterase (Cartwright blood group) Homo sapiens 15-19 20542100-1 2010 OBJECTIVES: Reactivation of inhibited acetylcholinesterase (AChE) with oximes is a causal therapy of intoxication with organophosphorus compounds (OPs). Oximes 71-77 acetylcholinesterase (Cartwright blood group) Homo sapiens 38-58 20542100-1 2010 OBJECTIVES: Reactivation of inhibited acetylcholinesterase (AChE) with oximes is a causal therapy of intoxication with organophosphorus compounds (OPs). Oximes 71-77 acetylcholinesterase (Cartwright blood group) Homo sapiens 60-64 20546883-5 2010 The location of groups on the pyridine ring also influences passive transport into the brain; the optimum position of the oxime group was found to be position four (para) and substitution of the oxime group on the pyridine ring by carbamoyl or amidoxime group markedly decreased penetration of AChE reactivators into the CNS. Oximes 122-127 acetylcholinesterase (Cartwright blood group) Homo sapiens 294-298 21152278-0 2010 Reactivation of human acetylcholinesterase and butyrylcholinesterase inhibited by leptophos-oxon with different oxime reactivators in vitro. Oximes 112-117 acetylcholinesterase (Cartwright blood group) Homo sapiens 22-42 21152278-0 2010 Reactivation of human acetylcholinesterase and butyrylcholinesterase inhibited by leptophos-oxon with different oxime reactivators in vitro. Oximes 112-117 butyrylcholinesterase Homo sapiens 47-68 21152278-1 2010 We have evaluated in vitro the potency of 23 oximes to reactivate human erythrocyte acetylcholinesterase (AChE) and plasma butyrylcholinesterase (BChE) inhibited by racemic leptophos-oxon (O-[4-bromo-2,5-dichlorophenyl]-O-methyl phenyl-phosphonate), a toxic metabolite of the pesticide leptophos. Oximes 45-51 acetylcholinesterase (Cartwright blood group) Homo sapiens 84-104 21152278-1 2010 We have evaluated in vitro the potency of 23 oximes to reactivate human erythrocyte acetylcholinesterase (AChE) and plasma butyrylcholinesterase (BChE) inhibited by racemic leptophos-oxon (O-[4-bromo-2,5-dichlorophenyl]-O-methyl phenyl-phosphonate), a toxic metabolite of the pesticide leptophos. Oximes 45-51 acetylcholinesterase (Cartwright blood group) Homo sapiens 106-110 21152278-3 2010 In case of leptophos-oxon inhibited AChE, the best reactivation potency was achieved with methoxime, trimedoxime, obidoxime and oxime K027. Oximes 94-99 acetylcholinesterase (Cartwright blood group) Homo sapiens 36-40 21152278-5 2010 The reactivation efficacy of tested oximes was lower in case of leptophos-oxon inhibited BChE. Oximes 36-42 butyrylcholinesterase Homo sapiens 89-93 20192902-0 2010 Oxime K027: novel low-toxic candidate for the universal reactivator of nerve agent- and pesticide-inhibited acetylcholinesterase. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 108-128 20350805-0 2010 A rapid oxime linker-based library approach to identification of bivalent inhibitors of the Yersinia pestis protein-tyrosine phosphatase, YopH. Oximes 8-13 YopH Yersinia pestis 138-142 20202777-5 2010 Oxime-type compounds used as acetylcholinesterase (AChE, E.C.3.1.1.7) reactivators have been considered for the retention study. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 29-49 20202777-5 2010 Oxime-type compounds used as acetylcholinesterase (AChE, E.C.3.1.1.7) reactivators have been considered for the retention study. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 51-55 20405932-5 2010 The presence of the syn- and anti-isomers of oxime 8 obtained from 4 were characterized by solid-state NMR and variable-temperature NMR experiments in acetone-d(6). Oximes 45-50 synemin Homo sapiens 20-23 20156534-0 2010 Comparative study of oxime-induced reactivation of erythrocyte and muscle AChE from different animal species following inhibition by sarin or paraoxon. Oximes 21-26 acetylcholinesterase (Cartwright blood group) Homo sapiens 74-78 20156534-1 2010 Standard treatment of acute poisoning by organophosphorus compounds (OP) includes administration of an antimuscarinic (e.g. atropine) and of an oxime-based reactivator of OP-inhibited acetylcholinesterase (AChE). Oximes 144-149 acetylcholinesterase (Cartwright blood group) Homo sapiens 206-210 20156534-2 2010 A recently introduced dynamically working in vitro model with real-time determination of membrane-bound AChE activity was shown to be a very versatile and promising model to investigate oxime-induced reactivation kinetics of OP-inhibited enzyme. Oximes 186-191 acetylcholinesterase (Cartwright blood group) Homo sapiens 104-108 20156534-6 2010 In addition, the basic kinetic constants of inhibition, aging, spontaneous- and oxime-induced-reactivation of erythrocyte AChE from these species were determined with a standard static model. Oximes 80-85 acetylcholinesterase (Cartwright blood group) Homo sapiens 122-126 21787634-0 2010 Reactivation of VX-inhibited AChE by novel oximes having two oxygen atoms in the linker. Oximes 43-49 acetylcholinesterase (Cartwright blood group) Homo sapiens 29-33 21787634-1 2010 Two newly developed AChE reactivators possessing two oxime groups in 4-position of the pyridinium rings with linkers CH(2)O(CH(2))(2)OCH(2) and CH(2)O(CH(2))(4)OCH(2) were tested for their potency to reactivate VX-inhibited AChE. Oximes 53-58 acetylcholinesterase (Cartwright blood group) Homo sapiens 20-24 20408892-7 2010 The ACh-induced enhancement in resistance to infection was abrogated by co-administration of an oxime which can reactivate AChE. Oximes 96-101 acetylcholinesterase Mus musculus 123-127 20929049-5 2010 Although new oximes that can reactivate both peripheral and cerebral AChE and other prophylactic agents such as human serum butyrylcholinesterase (Hu BChE), sodium bicarbonate, huperzine A (a reversible ChE inhibitor) with imidazenil (a GABAA receptor modulator) have been proved effective in animal models, systematic clinical trials in patients are warranted. Oximes 13-19 acetylcholinesterase (Cartwright blood group) Homo sapiens 69-73 20929049-5 2010 Although new oximes that can reactivate both peripheral and cerebral AChE and other prophylactic agents such as human serum butyrylcholinesterase (Hu BChE), sodium bicarbonate, huperzine A (a reversible ChE inhibitor) with imidazenil (a GABAA receptor modulator) have been proved effective in animal models, systematic clinical trials in patients are warranted. Oximes 13-19 butyrylcholinesterase Homo sapiens 124-145 20929049-5 2010 Although new oximes that can reactivate both peripheral and cerebral AChE and other prophylactic agents such as human serum butyrylcholinesterase (Hu BChE), sodium bicarbonate, huperzine A (a reversible ChE inhibitor) with imidazenil (a GABAA receptor modulator) have been proved effective in animal models, systematic clinical trials in patients are warranted. Oximes 13-19 butyrylcholinesterase Homo sapiens 150-154 20455239-3 2010 Selective oxidation of the sialic acid residues on the glycan chains of transferrin was followed by introduction of a terminal alkyne functionality through an oxime linkage. Oximes 159-164 transferrin Homo sapiens 72-83 20385200-0 2010 Muscle force and acetylcholinesterase activity in mouse hemidiaphragms exposed to paraoxon and treated by oximes in vitro. Oximes 106-112 acetylcholinesterase Mus musculus 17-37 20385200-2 2010 To alleviate peripheral respiratory failure oximes, e.g. obidoxime and pralidoxime, are used to reactivate inhibited acetylcholinesterase (AChE) with the intention to restore the disturbed neuromuscular function. Oximes 44-50 acetylcholinesterase Mus musculus 117-137 20385200-2 2010 To alleviate peripheral respiratory failure oximes, e.g. obidoxime and pralidoxime, are used to reactivate inhibited acetylcholinesterase (AChE) with the intention to restore the disturbed neuromuscular function. Oximes 44-50 acetylcholinesterase Mus musculus 139-143 20347021-3 2010 Reactivators (oximes) of inhibited AChE are a mainstay of treatment. Oximes 14-20 acetylcholinesterase (Cartwright blood group) Homo sapiens 35-39 20402532-3 2010 We demonstrate that amide coupling is efficient for producing multilayer structures on -COOH-terminated SAMs, while oxime coupling is efficient for producing multilayer structures on -CHO-terminated SAMs. Oximes 116-121 methionine adenosyltransferase 1A Homo sapiens 199-203 20350805-1 2010 A bivalent tethered approach toward YopH inhibitor development is presented that joins aldehydes with mixtures of bis-aminooxy-containing linkers using oxime coupling. Oximes 152-157 YopH Yersinia pestis 36-40 20005727-2 2010 The purpose of the present study was to evaluate new oxime compounds to reactivate acetylcholinesterase (AChE) inhibited by the OP paraoxon. Oximes 53-58 acetylcholinesterase (Cartwright blood group) Homo sapiens 83-103 19746406-2 2010 The ability of two combinations of oximes (HI-6 + obidoxime and HI-6 + K203) to reactivate tabun-inhibited acetylcholinesterase and reduce acute toxicity of tabun was compared with the reactivating and therapeutic efficacy of antidotal treatment involving single oxime (HI-6, obidoxime, K203) using in vivo methods. Oximes 35-40 acetylcholinesterase Rattus norvegicus 107-127 19746406-3 2010 Studies determining percentage of reactivation of tabun-inhibited blood and tissue acetylcholinesterase in poisoned rats showed that the reactivating efficacy of both combinations of oximes is higher than the reactivating efficacy of the most effective individual oxime in blood and diaphragm and comparable with the reactivating effects of the most effective individual oxime in brain. Oximes 183-189 acetylcholinesterase Rattus norvegicus 83-103 19746406-3 2010 Studies determining percentage of reactivation of tabun-inhibited blood and tissue acetylcholinesterase in poisoned rats showed that the reactivating efficacy of both combinations of oximes is higher than the reactivating efficacy of the most effective individual oxime in blood and diaphragm and comparable with the reactivating effects of the most effective individual oxime in brain. Oximes 183-188 acetylcholinesterase Rattus norvegicus 83-103 19746406-6 2010 Based on the obtained data, we can conclude that the antidotal treatment involving chosen combinations of oximes brings beneficial effects for the potency of antidotal treatment to reactivate tabun-inhibited acetylcholinesterase in rats and to reduce acute toxicity of tabun in mice. Oximes 106-112 acetylcholinesterase Rattus norvegicus 208-228 20004171-6 2010 OP-inhibited butyrylcholinesterase and acetylcholinesterase can be reactivated with oximes provided the OP has not aged. Oximes 84-90 butyrylcholinesterase Homo sapiens 13-34 20004171-6 2010 OP-inhibited butyrylcholinesterase and acetylcholinesterase can be reactivated with oximes provided the OP has not aged. Oximes 84-90 acetylcholinesterase (Cartwright blood group) Homo sapiens 39-59 20051531-8 2010 The addition of the neutral oxime 2,3-butanedione monoxime increases the rate of reactivation of hCE1 from sarin inhibition by more than 60-fold but has no effect on reactivation with the other agents examined. Oximes 28-33 carboxylesterase 1 Homo sapiens 97-101 20151655-2 2010 Reaction of the oxime derived from 2-(oxo-cyclopentyl)acetic acid ethyl ester with 2,3-bis(phenylsulfonyl)-1,3-butadiene gives rise to a 7-oxa-1-azanorbornane cycloadduct in high yield. Oximes 16-21 OXA1L mitochondrial inner membrane protein Homo sapiens 139-144 20140002-8 2010 Our work supports the growing body of evidence that the efficacy of the drugs is due to the differential bindings of the oximes with AChE and can aid to the rational design of oxime drugs. Oximes 121-127 acetylcholinesterase Mus musculus 133-137 20140002-8 2010 Our work supports the growing body of evidence that the efficacy of the drugs is due to the differential bindings of the oximes with AChE and can aid to the rational design of oxime drugs. Oximes 121-126 acetylcholinesterase Mus musculus 133-137 20005727-2 2010 The purpose of the present study was to evaluate new oxime compounds to reactivate acetylcholinesterase (AChE) inhibited by the OP paraoxon. Oximes 53-58 acetylcholinesterase (Cartwright blood group) Homo sapiens 105-109 20005727-7 2010 Interestingly, oximes with a heterocyclic linker inhibited AChE at higher concentration (10(-3)M), whereas their ability to reactivate was increased at lower concentrations (10(-4)M and 10(-5)M). Oximes 15-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 59-63 20028185-3 2010 Inhibited AChE can be reactivated by oximes, antidotes for OP exposure. Oximes 37-43 acetylcholinesterase (Cartwright blood group) Homo sapiens 10-14 19945872-0 2010 Oxime derivatives related to AP18: Agonists and antagonists of the TRPA1 receptor. Oximes 0-5 transient receptor potential cation channel subfamily A member 1 Homo sapiens 67-72 20028185-4 2010 However, OP intoxication caused by the nerve agent tabun (GA) is particularly resistant to oximes, which poorly reactivate GA-inhibited AChE. Oximes 91-97 acetylcholinesterase (Cartwright blood group) Homo sapiens 136-140 20028185-5 2010 In an attempt to develop a rational strategy for the discovery and design of novel reactivators with lower toxicity and increased efficacy in reactivating GA-inhibited AChE, we developed the first in silico pharmacophore model for binding affinity of GA-inhibited AChE from a set of 11 oximes. Oximes 286-292 acetylcholinesterase (Cartwright blood group) Homo sapiens 168-172 20028185-5 2010 In an attempt to develop a rational strategy for the discovery and design of novel reactivators with lower toxicity and increased efficacy in reactivating GA-inhibited AChE, we developed the first in silico pharmacophore model for binding affinity of GA-inhibited AChE from a set of 11 oximes. Oximes 286-292 acetylcholinesterase (Cartwright blood group) Homo sapiens 264-268 20028185-7 2010 Quantum chemical methods were sequentially used from semiempirical AM1 to hierarchical ab initio calculations to determine the stereoelectronic properties of nine oximes exhibiting affinity for binding to GA-inhibited AChE in vivo. Oximes 163-169 acetylcholinesterase (Cartwright blood group) Homo sapiens 218-222 20028185-10 2010 The in silico pharmacophore model of oxime affinity for binding to GA-inhibited AChE was found to require a hydrogen bond acceptor, a hydrogen bond donor at the two terminal regions, and an aromatic ring in the central region of the oximes. Oximes 37-42 acetylcholinesterase (Cartwright blood group) Homo sapiens 80-84 20345348-4 2010 It also focuses on the organophosphorus nerve agents, their properties, effects and a large part describes various possibilities in treatments, mainly traditional oxime therapies based on reactivation of AChE. Oximes 163-168 acetylcholinesterase (Cartwright blood group) Homo sapiens 204-208 20345348-5 2010 Furthermore, non-cholinesterase coupled antidotal effects of the oximes are thoroughly discussed. Oximes 65-71 butyrylcholinesterase Homo sapiens 17-31 19465093-1 2009 Oximes, including 2-pyridinealdoxime methiodide (2-PAM), are reactivators of acetylcholinesterase (AChE) inhibited by organophosphate poisoning. Oximes 0-6 peptidylglycine alpha-amidating monooxygenase Homo sapiens 51-54 20028185-10 2010 The in silico pharmacophore model of oxime affinity for binding to GA-inhibited AChE was found to require a hydrogen bond acceptor, a hydrogen bond donor at the two terminal regions, and an aromatic ring in the central region of the oximes. Oximes 233-239 acetylcholinesterase (Cartwright blood group) Homo sapiens 80-84 20028185-11 2010 The model was found to be well-correlated (R = 0.9) with experimental oxime affinity for binding to GA-inhibited AChE. Oximes 70-75 acetylcholinesterase (Cartwright blood group) Homo sapiens 113-117 20028185-13 2010 These results provided the first predictive pharmacophore model of oxime affinity for binding toward GA-inhibited AChE. Oximes 67-72 acetylcholinesterase (Cartwright blood group) Homo sapiens 114-118 20032868-0 2009 Novel bisquaternary oximes--reactivation of acetylcholinesterase and butyrylcholinesterase inhibited by paraoxon. Oximes 20-26 acetylcholinesterase (Cartwright blood group) Homo sapiens 44-64 20032868-0 2009 Novel bisquaternary oximes--reactivation of acetylcholinesterase and butyrylcholinesterase inhibited by paraoxon. Oximes 20-26 butyrylcholinesterase Homo sapiens 69-90 19761810-2 2009 Oximes, such as K027 and HLo-7, can reactivate tabun-inhibited human AChE (tabun-hAChE) whereas the activity of their close structural analogue HI-6 is notably low. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 69-73 19761810-2 2009 Oximes, such as K027 and HLo-7, can reactivate tabun-inhibited human AChE (tabun-hAChE) whereas the activity of their close structural analogue HI-6 is notably low. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 81-86 19835355-0 2009 Biomimetic synthesis of lispro insulin via a chemically synthesized "mini-proinsulin" prepared by oxime-forming ligation. Oximes 98-103 insulin Homo sapiens 31-38 19835355-0 2009 Biomimetic synthesis of lispro insulin via a chemically synthesized "mini-proinsulin" prepared by oxime-forming ligation. Oximes 98-103 insulin Homo sapiens 74-84 19835355-2 2009 We used oxime-forming chemical ligation to introduce a temporary "chemical tether" to link the N-terminal residue of the insulin A chain to the C-terminal residue of the insulin B chain; the tether enabled us to fold/form disulfides with high efficiency. Oximes 8-13 insulin Homo sapiens 121-128 19835355-2 2009 We used oxime-forming chemical ligation to introduce a temporary "chemical tether" to link the N-terminal residue of the insulin A chain to the C-terminal residue of the insulin B chain; the tether enabled us to fold/form disulfides with high efficiency. Oximes 8-13 insulin Homo sapiens 170-177 19737786-2 2009 This chemical structure affects their responsiveness to oxime-induced acetylcholinesterase (AChE) reactivation after poisoning. Oximes 56-61 acetylcholinesterase (Cartwright blood group) Homo sapiens 92-96 21578527-2 2009 One- and two-dimensional (1)H and (13)C NMR spectra, as well as IR data, are in agreement with the presence of a ketoxime group at C-23. Oximes 113-121 nucleolin Homo sapiens 131-135 21578527-6 2009 The ketoxime is stabilized with the E configuration, avoiding steric hindrance between the oxime O atom and H atom at C-23. Oximes 4-12 nucleolin Homo sapiens 118-122 19680820-1 2010 The capability of the tertiary oximes, monoisonitrosoacetone (MINA) and diacetylmonoxime (DAM), to reactivate acetylcholinesterase (AChE) inhibited by sarin (GB) in the blood, brain, and peripheral tissues of guinea pigs was compared with that of the quaternary oximes 2-PAM, HLo7, and MMB-4. Oximes 31-37 acetylcholinesterase Cavia porcellus 110-130 19680820-1 2010 The capability of the tertiary oximes, monoisonitrosoacetone (MINA) and diacetylmonoxime (DAM), to reactivate acetylcholinesterase (AChE) inhibited by sarin (GB) in the blood, brain, and peripheral tissues of guinea pigs was compared with that of the quaternary oximes 2-PAM, HLo7, and MMB-4. Oximes 31-37 acetylcholinesterase Cavia porcellus 132-136 19680820-1 2010 The capability of the tertiary oximes, monoisonitrosoacetone (MINA) and diacetylmonoxime (DAM), to reactivate acetylcholinesterase (AChE) inhibited by sarin (GB) in the blood, brain, and peripheral tissues of guinea pigs was compared with that of the quaternary oximes 2-PAM, HLo7, and MMB-4. Oximes 262-268 acetylcholinesterase Cavia porcellus 110-130 19680820-1 2010 The capability of the tertiary oximes, monoisonitrosoacetone (MINA) and diacetylmonoxime (DAM), to reactivate acetylcholinesterase (AChE) inhibited by sarin (GB) in the blood, brain, and peripheral tissues of guinea pigs was compared with that of the quaternary oximes 2-PAM, HLo7, and MMB-4. Oximes 262-268 acetylcholinesterase Cavia porcellus 132-136 19680820-13 2010 Thus, tertiary oximes reactivated AChE in the brain, improved survival, and terminated seizures following GB intoxication. Oximes 15-21 acetylcholinesterase Cavia porcellus 34-38 20402654-6 2010 Our results showed that oxime K048 reached promising reactivation activity in case of all tested AChE inhibitors, except cyclosarin, at oxime concentration 10(-3) M. At a concentration of 10(-5) M, which is more common for human use, only methylchlorpyrifos-inhibited AChE was reactivated. Oximes 24-29 acetylcholinesterase (Cartwright blood group) Homo sapiens 97-101 20402654-6 2010 Our results showed that oxime K048 reached promising reactivation activity in case of all tested AChE inhibitors, except cyclosarin, at oxime concentration 10(-3) M. At a concentration of 10(-5) M, which is more common for human use, only methylchlorpyrifos-inhibited AChE was reactivated. Oximes 24-29 acetylcholinesterase (Cartwright blood group) Homo sapiens 268-272 19572551-5 2009 The use of an oxime linkage between the polyamide and an aromatic functionality on the C-terminus resulted in a approximately 20-fold increase in the potency of polyamides targeted to the androgen response element (ARE) in LNCaP cells by measuring AR-activated PSA expression. Oximes 14-19 aminopeptidase puromycin sensitive Homo sapiens 261-264 19642642-7 2009 Furthermore, the crystal structure of the ternary complex of the aged conjugate with 2-PAM revealed that the orientation of the oxime function does not permit nucleophilic attack on the phosphorus atom, thus providing a plausible explanation for its failure to reactivate the aged soman/AChE conjugate. Oximes 128-133 peptidylglycine alpha-amidating monooxygenase Homo sapiens 87-90 19642642-7 2009 Furthermore, the crystal structure of the ternary complex of the aged conjugate with 2-PAM revealed that the orientation of the oxime function does not permit nucleophilic attack on the phosphorus atom, thus providing a plausible explanation for its failure to reactivate the aged soman/AChE conjugate. Oximes 128-133 acetylcholinesterase (Cartwright blood group) Homo sapiens 287-291 19465093-1 2009 Oximes, including 2-pyridinealdoxime methiodide (2-PAM), are reactivators of acetylcholinesterase (AChE) inhibited by organophosphate poisoning. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 77-97 19465093-1 2009 Oximes, including 2-pyridinealdoxime methiodide (2-PAM), are reactivators of acetylcholinesterase (AChE) inhibited by organophosphate poisoning. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 99-103 19338015-7 2009 The potency of oximes to reactivate brain AChE was lower due to the poor blood-brain barrier penetration of used compounds. Oximes 15-21 acetylcholinesterase Rattus norvegicus 42-46 19778238-3 2009 Oximes such as 2-PAM are used to reactivate OP-inhibited AChE so as to restore normal enzymatic function and serve as a true antidote. Oximes 0-6 acetylcholinesterase Cavia porcellus 57-61 19778238-4 2009 There are reports of non-enzymatic hydrolysis by oximes of acetylthiocholine in in vitro preparations in the widely used Ellman assay for AChE activity, which may confound the interpretation of AChE activity by producing elevated results. Oximes 49-55 acetylcholinesterase Cavia porcellus 138-142 19778238-4 2009 There are reports of non-enzymatic hydrolysis by oximes of acetylthiocholine in in vitro preparations in the widely used Ellman assay for AChE activity, which may confound the interpretation of AChE activity by producing elevated results. Oximes 49-55 acetylcholinesterase Cavia porcellus 194-198 19778238-5 2009 The purpose of this experiment was to determine if there is appreciable interference by therapeutic levels of oximes on the results of the Ellman assay in assessing AChE reactivation by oxime compounds in vivo. Oximes 110-116 acetylcholinesterase Cavia porcellus 165-169 19778238-5 2009 The purpose of this experiment was to determine if there is appreciable interference by therapeutic levels of oximes on the results of the Ellman assay in assessing AChE reactivation by oxime compounds in vivo. Oximes 110-115 acetylcholinesterase Cavia porcellus 165-169 19778238-7 2009 With appropriate dilution of samples prior to spectrophotometric assay, the Ellman assay is an acceptable method to measure in vivo oxime reactivation of inhibited AChE. Oximes 132-137 acetylcholinesterase Cavia porcellus 164-168 19778239-7 2009 These oximes exhibited differential potency in reactivating nerve agent-inhibited AChE in various peripheral tissues, but not AChE activity in the brain regions. Oximes 6-12 acetylcholinesterase Cavia porcellus 82-86 19778239-9 2009 AChE inhibited by sarin was the most and cyclosarin the least susceptible to oxime reactivation. Oximes 77-82 acetylcholinesterase Cavia porcellus 0-4 19482409-1 2009 We determine the binding mode of a macrocyclic radicicol-like oxime to yeast HSP90 by combining computer simulations and experimental measurements. Oximes 62-67 Hsp90 family chaperone HSP82 Saccharomyces cerevisiae S288C 77-82 19482409-6 2009 We find that the most likely binding mode of the oxime to yeast HSP90 is very similar to the known structure of the radicicol-HSP90 complex. Oximes 49-54 Hsp90 family chaperone HSP82 Saccharomyces cerevisiae S288C 64-69 19482409-6 2009 We find that the most likely binding mode of the oxime to yeast HSP90 is very similar to the known structure of the radicicol-HSP90 complex. Oximes 49-54 Hsp90 family chaperone HSP82 Saccharomyces cerevisiae S288C 126-131 19552519-2 2009 Studies determined percentage of reactivation of tabun-inhibited blood and tissue AChE in poisoned rats and showed that the reactivating efficacy of both newly developed oximes is comparable with the oxime HI-6 but it is significantly lower than the reactivating effects of obidoxime and trimedoxime, especially in diaphragm and brain. Oximes 170-176 acetylcholinesterase Rattus norvegicus 82-86 19603416-4 2009 The intrinsic AChE inhibitory activity of oximes, as reflected by their in vitro IC(50), is strongly correlated with their LD(50) (rat): oximes with a high IC(50) (K-27, K-48, pralidoxime and obidoxime) also show a high LD(50) and are thus relatively non-toxic, whereas oximes K-105, K-108 and K-113 have a low IC(50), a low LD(50) and are far more toxic. Oximes 42-48 acetylcholinesterase Rattus norvegicus 14-18 19603416-4 2009 The intrinsic AChE inhibitory activity of oximes, as reflected by their in vitro IC(50), is strongly correlated with their LD(50) (rat): oximes with a high IC(50) (K-27, K-48, pralidoxime and obidoxime) also show a high LD(50) and are thus relatively non-toxic, whereas oximes K-105, K-108 and K-113 have a low IC(50), a low LD(50) and are far more toxic. Oximes 42-48 keratin 27 Rattus norvegicus 164-168 19603416-4 2009 The intrinsic AChE inhibitory activity of oximes, as reflected by their in vitro IC(50), is strongly correlated with their LD(50) (rat): oximes with a high IC(50) (K-27, K-48, pralidoxime and obidoxime) also show a high LD(50) and are thus relatively non-toxic, whereas oximes K-105, K-108 and K-113 have a low IC(50), a low LD(50) and are far more toxic. Oximes 137-143 acetylcholinesterase Rattus norvegicus 14-18 19603416-4 2009 The intrinsic AChE inhibitory activity of oximes, as reflected by their in vitro IC(50), is strongly correlated with their LD(50) (rat): oximes with a high IC(50) (K-27, K-48, pralidoxime and obidoxime) also show a high LD(50) and are thus relatively non-toxic, whereas oximes K-105, K-108 and K-113 have a low IC(50), a low LD(50) and are far more toxic. Oximes 137-143 keratin 27 Rattus norvegicus 164-168 19586353-0 2009 In vitro oxime-assisted reactivation of paraoxon-inhibited human acetylcholinesterase and butyrylcholinesterase. Oximes 9-14 acetylcholinesterase (Cartwright blood group) Homo sapiens 65-111 19621084-7 2009 Crystal structures of the TTR:inhibitor complexes, in agreement with molecular docking studies, revealed that the aromatic moiety, linked to the sp(2)-hybridized oxime carbon, specifically directed the ligand in either a forward or reverse binding mode. Oximes 162-167 transthyretin Homo sapiens 26-29 19586353-3 2009 METHODS: Eighteen structurally different oxime reactivators were tested for their in vitro ability to reactivate paraoxon-inhibited human erythrocyte acetylcholinesterase and human plasma butyrylcholinesterase to find out structure-activity relationship within this set of compounds. Oximes 41-46 acetylcholinesterase (Cartwright blood group) Homo sapiens 150-170 19586353-3 2009 METHODS: Eighteen structurally different oxime reactivators were tested for their in vitro ability to reactivate paraoxon-inhibited human erythrocyte acetylcholinesterase and human plasma butyrylcholinesterase to find out structure-activity relationship within this set of compounds. Oximes 41-46 butyrylcholinesterase Homo sapiens 188-209 18950608-1 2009 Oximes are compounds generally used to reverse the acetylcholinesterase (AChE) inhibition caused by organophosphates (OPs). Oximes 0-6 acetylcholinesterase Mus musculus 51-71 19526299-2 2009 However, oximes themselves are also AChE inhibitors, albeit at higher concentrations, which is a major cause of their toxicity and may be a dose-limiting factor in oxime therapy. Oximes 9-15 acetylcholinesterase (Cartwright blood group) Homo sapiens 36-40 19526299-2 2009 However, oximes themselves are also AChE inhibitors, albeit at higher concentrations, which is a major cause of their toxicity and may be a dose-limiting factor in oxime therapy. Oximes 9-14 acetylcholinesterase (Cartwright blood group) Homo sapiens 36-40 19449818-1 2009 Oximes have been used as reactivators for organophosphorus-inhibited acetylcholinesterase (AChE). Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 91-95 19449818-4 2009 We have concluded that oximes reactivate AChE by a three-step mechanism in opposition to the four-step processes of the other modeled nucleophiles. Oximes 23-29 acetylcholinesterase (Cartwright blood group) Homo sapiens 41-45 19449818-5 2009 In addition, our model suggests that oximes react with AChE in the deprotonated form (oximate). Oximes 37-43 acetylcholinesterase (Cartwright blood group) Homo sapiens 55-59 19368529-4 2009 hBChE inhibited by phosphoramidates such as tabun displays a peculiar resistance to oxime-mediated reactivation. Oximes 84-89 butyrylcholinesterase Homo sapiens 0-5 19368529-11 2009 This study provides the structural basis to design new oximes capable of reactivating phosphoramidyl-hBChE conjugates after intoxication, notably when hBChE is used as pretreatment, or to design BChE-based catalytic bioscavengers. Oximes 55-61 butyrylcholinesterase Homo sapiens 101-106 19368529-11 2009 This study provides the structural basis to design new oximes capable of reactivating phosphoramidyl-hBChE conjugates after intoxication, notably when hBChE is used as pretreatment, or to design BChE-based catalytic bioscavengers. Oximes 55-61 butyrylcholinesterase Homo sapiens 151-156 19368529-11 2009 This study provides the structural basis to design new oximes capable of reactivating phosphoramidyl-hBChE conjugates after intoxication, notably when hBChE is used as pretreatment, or to design BChE-based catalytic bioscavengers. Oximes 55-61 butyrylcholinesterase Homo sapiens 102-106 19277015-2 2009 Here, we show that chemical conjugation of a synthetic oligosaccharide harboring mannose 6-phosphate (M6P) residues onto recombinant human acid alpha-glucosidase (rhGAA) via oxime chemistry significantly improved its affinity for the cation-independent mannose 6-phosphate receptor (CI-MPR) and subsequent uptake by muscle cells. Oximes 174-179 insulin like growth factor 2 receptor Homo sapiens 234-281 19277015-2 2009 Here, we show that chemical conjugation of a synthetic oligosaccharide harboring mannose 6-phosphate (M6P) residues onto recombinant human acid alpha-glucosidase (rhGAA) via oxime chemistry significantly improved its affinity for the cation-independent mannose 6-phosphate receptor (CI-MPR) and subsequent uptake by muscle cells. Oximes 174-179 insulin like growth factor 2 receptor Homo sapiens 283-289 19429253-1 2009 Previous kinetic studies investigating the interactions between human acetylcholinesterase (AChE), structurally different organophosphorus compounds (OP) and oximes did not reveal a conclusive structure-activity relationship of the different reactions. Oximes 158-164 acetylcholinesterase (Cartwright blood group) Homo sapiens 70-90 19429253-7 2009 Pentylsarin-inhibited AChE could be reactivated by oximes, HI 6 being more potent than obidoxime. Oximes 51-57 acetylcholinesterase (Cartwright blood group) Homo sapiens 22-26 19429253-9 2009 Unfortunately, no structure-activity relationship could be observed for the oxime-induced reactivation of inhibited AChE. Oximes 76-81 acetylcholinesterase (Cartwright blood group) Homo sapiens 116-120 19376700-6 2009 Based on the typical topology of synthetic PPAR agonists, we focused our design approach on using 4,4-dimethyl-1,2,3,4-tetrahydroquinoline as a novel cyclic scaffold with oxime and acidic head group structural variations. Oximes 171-176 peroxisome proliferator activated receptor alpha Homo sapiens 43-47 19428953-4 2009 For therapeutic monitoring of oxime treatment in OP poisoning, measurement of erythrocyte AChE is suitable because erythrocyte AChE is an easily accessible surrogate for synaptic AChE. Oximes 30-35 acetylcholinesterase (Cartwright blood group) Homo sapiens 90-94 19428953-6 2009 In contrast, determination of plasma butyrylcholinesterase (BChE) activity is in routine use for monitoring the benefit of oxime therapy. Oximes 123-128 butyrylcholinesterase Homo sapiens 37-58 19428953-6 2009 In contrast, determination of plasma butyrylcholinesterase (BChE) activity is in routine use for monitoring the benefit of oxime therapy. Oximes 123-128 butyrylcholinesterase Homo sapiens 60-64 19428953-10 2009 Furthermore, oxime-induced reactivation is too slow to accomplish a pseudo catalytic function, so that administered BChE may be merely effective as a stoichiometric scavenger. Oximes 13-18 butyrylcholinesterase Homo sapiens 116-120 19150463-5 2009 This implies that the main beneficial effect of oximes may result from reactivation of AChE activity in respiratory muscles rather than in the brain. Oximes 48-54 acetylcholinesterase (Cartwright blood group) Homo sapiens 87-91 19150463-7 2009 Albeit the concentration of oximes in the central nervous system is significantly lower than in the plasma, they do gain access into the brain and are able to reactivate inhibited local AChE. Oximes 28-34 acetylcholinesterase (Cartwright blood group) Homo sapiens 186-190 19150463-9 2009 In this review, we focus on the ability of oximes to act in the brain and protect the central nervous system from OP-induced injury, either by direct reactivation of AChE or by other pharmacological mechanisms. Oximes 43-49 acetylcholinesterase (Cartwright blood group) Homo sapiens 166-170 19428926-0 2009 Comparison of the oxime-induced reactivation of rhesus monkey, swine and guinea pig erythrocyte acetylcholinesterase following inhibition by sarin or paraoxon, using a perfusion model for the real-time determination of membrane-bound acetylcholinesterase activity. Oximes 18-23 acetylcholinesterase Cavia porcellus 96-116 19428926-0 2009 Comparison of the oxime-induced reactivation of rhesus monkey, swine and guinea pig erythrocyte acetylcholinesterase following inhibition by sarin or paraoxon, using a perfusion model for the real-time determination of membrane-bound acetylcholinesterase activity. Oximes 18-23 acetylcholinesterase Cavia porcellus 234-254 19428926-1 2009 Recently, a dynamically working in vitro model with real-time determination of membrane-bound human acetylcholinesterase (AChE) activity was shown to be a versatile model to investigate oxime-induced reactivation kinetics of organophosphate- (OP) inhibited enzyme. Oximes 186-191 acetylcholinesterase Cavia porcellus 100-120 19428926-1 2009 Recently, a dynamically working in vitro model with real-time determination of membrane-bound human acetylcholinesterase (AChE) activity was shown to be a versatile model to investigate oxime-induced reactivation kinetics of organophosphate- (OP) inhibited enzyme. Oximes 186-191 acetylcholinesterase (Cartwright blood group) Homo sapiens 122-126 19428926-7 2009 Hence, this dynamic model offers the possibility to investigate highly reproducible interactions between AChE, OP and oximes with human and animal AChE. Oximes 118-124 acetylcholinesterase (Cartwright blood group) Homo sapiens 147-151 18950608-1 2009 Oximes are compounds generally used to reverse the acetylcholinesterase (AChE) inhibition caused by organophosphates (OPs). Oximes 0-6 acetylcholinesterase Mus musculus 73-77 19544081-5 2009 A novel oxime, 1-{4-[6-amino-5-(methoxyimino-methyl)-pyrimidin-4-yloxy]-2-chloro-phenyl}-3-ethyl-urea (JNJ-38158471), was identified as a potent and selective inhibitor of VEGFR-2. Oximes 8-13 kinase insert domain protein receptor Mus musculus 172-179 18686075-7 2009 RESULTS AND DISCUSSION: In vivo determined percentage of reactivation of cyclosarin-inhibited blood and tissue acetylcholinesterase (AChE) in poisoned rats showed that the potency of both newly developed oximes (K206, K269) to reactivate cyclosarin-inhibited AChE is comparable with that of obidoxime in blood and diaphragm, but slightly higher than that of obidoxime in brain. Oximes 204-210 acetylcholinesterase Rattus norvegicus 133-137 18991751-7 2008 Correlations between the different in vitro and in vivo data available reveal that an oxime with a low in vitro AChE inhibitory activity (high IC(50)) is rather non-toxic and reduces DFP-induced mortality (low cumulative relative risk). Oximes 86-91 acetylcholinesterase Rattus norvegicus 112-116 18992260-9 2008 Moreover, oximes protected tryptophan residues of ApoB-100 in the early stage of LDL oxidation and during the subsequent propagation phase. Oximes 10-16 apolipoprotein B Homo sapiens 50-58 18608751-2 2008 Studies which determined percentage of reactivation of tabun-inhibited blood and tissue AChE in poisoned rats showed that the reactivating efficacy of both newly developed oximes is comparable with obidoxime and trimedoxime in blood but lower than the reactivating potency of trimedoxime and obidoxime in the diaphragm and brain. Oximes 172-178 acetylcholinesterase Rattus norvegicus 88-92 18608751-7 2008 Both newly developed oximes (K206, K269) are significantly more efficacious in reactivating tabun-inhibited AChE in rats and to eliminate lethal toxic effects of tabun in mice than the oxime HI-6 but their reactivating and therapeutic potency does not prevail over the effectiveness of currently available obidoxime and trimedoxime and, therefore, they are not suitable for their replacement of commonly used oximes for the treatment of acute tabun poisoning. Oximes 21-27 acetylcholinesterase Rattus norvegicus 108-112 18975951-5 2008 The inhibition of ChEs by tabun and the subsequent aging reaction are of particular interest, because tabun-ChE conjugates display an extraordinary resistance toward most current oxime reactivators. Oximes 179-184 butyrylcholinesterase Homo sapiens 18-21 18975951-6 2008 We investigated the structural basis of oxime resistance for phosphoramidated ChE conjugates by determining the crystal structures of the non-aged and aged forms of hBChE inhibited by tabun, and by updating the refinement of non-aged and aged tabun-inhibited mouse AChE (mAChE). Oximes 40-45 butyrylcholinesterase Homo sapiens 78-81 18975951-6 2008 We investigated the structural basis of oxime resistance for phosphoramidated ChE conjugates by determining the crystal structures of the non-aged and aged forms of hBChE inhibited by tabun, and by updating the refinement of non-aged and aged tabun-inhibited mouse AChE (mAChE). Oximes 40-45 butyrylcholinesterase Homo sapiens 165-170 18975951-6 2008 We investigated the structural basis of oxime resistance for phosphoramidated ChE conjugates by determining the crystal structures of the non-aged and aged forms of hBChE inhibited by tabun, and by updating the refinement of non-aged and aged tabun-inhibited mouse AChE (mAChE). Oximes 40-45 acetylcholinesterase Mus musculus 265-269 18975951-13 2008 The reported 3D data will help in the design of new oximes capable of reactivating tabun-ChE conjugates. Oximes 52-58 butyrylcholinesterase Homo sapiens 89-92 18991751-8 2008 Oximes with a high in vitro AChE reactivation potency (high tan alpha) also have a high in vitro AChE inhibitory activity (low IC(50)) and have a low LD(50) in vivo, implying high toxicity. Oximes 0-6 acetylcholinesterase Rattus norvegicus 28-32 18991751-8 2008 Oximes with a high in vitro AChE reactivation potency (high tan alpha) also have a high in vitro AChE inhibitory activity (low IC(50)) and have a low LD(50) in vivo, implying high toxicity. Oximes 0-6 acetylcholinesterase Rattus norvegicus 97-101 18991751-9 2008 Less hydrophilic oximes have strong in vitro AChE inhibitory activity, are better in vitro AChE reactivators, but are also more toxic in vivo and are associated with a high cumulative risk of death after DFP exposure in rats, implying low in vivo efficacy. Oximes 17-23 acetylcholinesterase Rattus norvegicus 45-49 18991751-9 2008 Less hydrophilic oximes have strong in vitro AChE inhibitory activity, are better in vitro AChE reactivators, but are also more toxic in vivo and are associated with a high cumulative risk of death after DFP exposure in rats, implying low in vivo efficacy. Oximes 17-23 acetylcholinesterase Rattus norvegicus 91-95 18504554-1 2008 Oximes are a class of compounds normally used to reverse the acetylcholinesterase (AChE) inhibition caused by organophosphates (OPs). Oximes 0-6 acetylcholinesterase Mus musculus 61-81 18826205-2 2008 Most of the compounds possessing an oxime ether linker were more potent PPARgamma activators than the lead PPARalpha/gamma dual agonist, tesaglitazar in vitro. Oximes 36-41 peroxisome proliferator activated receptor gamma Mus musculus 72-81 18826205-3 2008 Compound 18, one of the derivatives with an oxime ether linker, was found to selectively transactivate PPARgamma (EC 50 = 0.028 microM) over PPARalpha (EC 50 = 7.22 microM) in vitro and lower blood glucose in db/ db mice more than muraglitazar after oral treatment for 11 days. Oximes 44-49 peroxisome proliferator activated receptor gamma Mus musculus 103-112 18504554-1 2008 Oximes are a class of compounds normally used to reverse the acetylcholinesterase (AChE) inhibition caused by organophosphates (OPs). Oximes 0-6 acetylcholinesterase Mus musculus 83-87 18548743-2 2008 However, AChE inhibition by oximes themselves (as quantified by their intrinsic IC50) is the major cause of oxime toxicity and the dose-limiting factor. Oximes 28-34 acetylcholinesterase (Cartwright blood group) Homo sapiens 9-13 18548743-2 2008 However, AChE inhibition by oximes themselves (as quantified by their intrinsic IC50) is the major cause of oxime toxicity and the dose-limiting factor. Oximes 28-33 acetylcholinesterase (Cartwright blood group) Homo sapiens 9-13 18548743-5 2008 Best protection was conferred by K-27, reducing the relative risk of death (RR) to 16% of control RR (P < or = 0.05), which was statistically significantly better (P < or = 0.05) than all other tested oximes, except obidoxime, K-53 and K-75. Oximes 207-213 keratin 27 Homo sapiens 33-37 18855728-9 2008 The potency of all newly synthesized oximes to reactivate tabun-inhibited AChE is comparable with obidoxime with the exception of K074 that is significantly more efficacious in the brain. Oximes 37-43 acetylcholinesterase (Cartwright blood group) Homo sapiens 74-78 18547553-4 2008 These oximes inhibited AchE with inhibitory potency (IC(50)) ranging from 0.02 to 1.0 mM. Oximes 6-12 acetylcholinesterase (Cartwright blood group) Homo sapiens 23-27 18547553-6 2008 The protective potency (P(50)) of all oximes in human erythrocyte AChE inhibited by soman and tabun could not be determined. Oximes 38-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 66-70 18547554-1 2008 The potency of newly developed oximes (K074, K075) and commonly used oximes (obidoxime, HI-6) to reactivate nerve agent-inhibited acetylcholinesterase was evaluated in rats poisoned with soman, tabun or cyclosarin at a lethal dose corresponding to their LD(50) value. Oximes 31-37 acetylcholinesterase Rattus norvegicus 130-150 18547554-1 2008 The potency of newly developed oximes (K074, K075) and commonly used oximes (obidoxime, HI-6) to reactivate nerve agent-inhibited acetylcholinesterase was evaluated in rats poisoned with soman, tabun or cyclosarin at a lethal dose corresponding to their LD(50) value. Oximes 69-75 acetylcholinesterase Rattus norvegicus 130-150 18547554-2 2008 In vivo determined percentage of reactivation of soman-inhibited blood and brain acetylcholinesterase in poisoned rats showed that only the oxime HI-6 was able to reactivate soman-inhibited acetylcholinesterase in the peripheral (blood) as well as central (brain) compartment. Oximes 140-145 acetylcholinesterase Rattus norvegicus 81-101 18547554-2 2008 In vivo determined percentage of reactivation of soman-inhibited blood and brain acetylcholinesterase in poisoned rats showed that only the oxime HI-6 was able to reactivate soman-inhibited acetylcholinesterase in the peripheral (blood) as well as central (brain) compartment. Oximes 140-145 acetylcholinesterase Rattus norvegicus 190-210 18617161-0 2008 Potency of several oximes to reactivate human acetylcholinesterase and butyrylcholinesterase inhibited by paraoxon in vitro. Oximes 19-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 46-66 18501341-0 2008 Oximes: Reactivators of phosphorylated acetylcholinesterase and antidotes in therapy against tabun poisoning. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 39-59 18501341-1 2008 One of the therapeutic approaches to organophosphate poisoning is to reactivate AChE with site-directed nucleophiles such as oximes. Oximes 125-131 acetylcholinesterase (Cartwright blood group) Homo sapiens 80-84 18555982-2 2008 It has been demonstrated that the efficacy of an oxime primarily depends on its ability to reactivate nerve agent-inhibited acetylcholinesterase (AChE). Oximes 49-54 acetylcholinesterase (Cartwright blood group) Homo sapiens 146-150 18555982-3 2008 If the in vitro oxime reactivation of nerve agent-inhibited animal AChE is similar to that of human AChE, it is likely that the results of an in vivo animal study will reliably extrapolate to humans. Oximes 16-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 67-71 18555982-6 2008 Results indicate that oxime reactivation of all three monkey AChEs was very similar to human AChE. Oximes 22-27 acetylcholinesterase (Cartwright blood group) Homo sapiens 61-65 18565503-2 2008 The purpose of the present study was to evaluate new oxime antidotes to reactivate the inhibited AChE. Oximes 53-58 acetylcholinesterase (Cartwright blood group) Homo sapiens 97-101 18501341-3 2008 We tested oximes varying in the type of ring (pyridinium and/or imidazolium), the length and type of the linker between rings, and in the position of the oxime group on the ring to find more effective oximes to reactivate tabun-inhibited human erythrocyte AChE. Oximes 201-207 acetylcholinesterase (Cartwright blood group) Homo sapiens 256-260 18523134-7 2008 Accordingly, oxime administration to PEG-F338A-AChE-pretreated mice enabled them to withstand repeated soman exposure (5.4 and 4 LD(50)/dose), whereas same regime treatment of non-PEGylated F338A-AChE- or PEGylated WT-AChE-pretreated mice failed to protect against the second challenge, due to rapid clearance or irreversible aging of the latter enzymes. Oximes 13-18 acetylcholinesterase Mus musculus 47-51 18501341-7 2008 Since the reactivating efficacy of the oximes in vitro corresponded to their therapeutic efficacy in vivo, it seems that pharmacological effect of these oximes is indeed primarily related to the reactivation of tabun-phosphorylated AChE. Oximes 39-45 acetylcholinesterase (Cartwright blood group) Homo sapiens 232-236 18501341-7 2008 Since the reactivating efficacy of the oximes in vitro corresponded to their therapeutic efficacy in vivo, it seems that pharmacological effect of these oximes is indeed primarily related to the reactivation of tabun-phosphorylated AChE. Oximes 153-159 acetylcholinesterase (Cartwright blood group) Homo sapiens 232-236 18523134-7 2008 Accordingly, oxime administration to PEG-F338A-AChE-pretreated mice enabled them to withstand repeated soman exposure (5.4 and 4 LD(50)/dose), whereas same regime treatment of non-PEGylated F338A-AChE- or PEGylated WT-AChE-pretreated mice failed to protect against the second challenge, due to rapid clearance or irreversible aging of the latter enzymes. Oximes 13-18 acetylcholinesterase Mus musculus 196-200 18523134-7 2008 Accordingly, oxime administration to PEG-F338A-AChE-pretreated mice enabled them to withstand repeated soman exposure (5.4 and 4 LD(50)/dose), whereas same regime treatment of non-PEGylated F338A-AChE- or PEGylated WT-AChE-pretreated mice failed to protect against the second challenge, due to rapid clearance or irreversible aging of the latter enzymes. Oximes 13-18 acetylcholinesterase Mus musculus 196-200 18508103-4 2008 Analysis of in vitro reactivation was conducted with second-order rate contants (k(r2)) for oxime reactivation of agent-inhibited acetylcholinesterase (AChE) from guinea pig erythrocytes. Oximes 92-97 acetylcholinesterase Cavia porcellus 152-156 18508103-7 2008 The decrease in oxime PR and k(r2) as the volume of the agent moiety conjugated to AChE increased was consistent with a steric hindrance mechanism. Oximes 16-21 acetylcholinesterase Cavia porcellus 83-87 18655064-0 2008 SAR by oxime-containing peptide libraries: application to Tsg101 ligand optimization. Oximes 7-12 tumor susceptibility 101 Homo sapiens 58-64 18344198-1 2008 Oximes are enzyme reactivators used in treating poisoning with organophosphorus cholinesterase (AChE) inhibitors. Oximes 0-6 butyrylcholinesterase Homo sapiens 80-94 18617161-3 2008 For the recovery of inhibited AChE, derivatives from the group of pyridinium or bispyridinium aldoximes (called oximes) are used. Oximes 97-103 acetylcholinesterase (Cartwright blood group) Homo sapiens 30-34 18617161-11 2008 From the data obtained, it is clear that only two from currently available oximes (obidoxime and trimedoxime) are good reactivators of paraoxon-inhibited AChE. Oximes 75-81 acetylcholinesterase (Cartwright blood group) Homo sapiens 154-158 18481153-7 2008 CONCLUSION: Site-specific 18F-labeled Affibody against HER2 has been synthesized via chemoselective oxime formation between an aminooxy-functionalized Affibody and 18F-fluorobenzaldehyde. Oximes 100-105 erb-b2 receptor tyrosine kinase 2 Homo sapiens 55-59 18444657-2 2008 With this simple two-step procedure involving substitution with readily available TsNHOTBS and subsequent treatment with CsF, a range of oximes were prepared including the ones hardly preparable with conventional procedures. Oximes 137-143 colony stimulating factor 2 Homo sapiens 121-124 18564794-3 2008 The morbidity and mortality with organophosphate poisoning is relatively high despite the use of atropine as specific antidotal therapy and oximes to reactivate acetylcholinesterase. Oximes 140-146 acetylcholinesterase (Cartwright blood group) Homo sapiens 161-181 18344198-1 2008 Oximes are enzyme reactivators used in treating poisoning with organophosphorus cholinesterase (AChE) inhibitors. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 96-100 18344198-2 2008 The oxime dose which can be safely administered is limited by the intrinsic toxicity of the substances such as their own AChE-inhibiting tendency. Oximes 4-9 acetylcholinesterase (Cartwright blood group) Homo sapiens 121-125 18413392-4 2008 METHODS: In this study, anti-HER2 monomeric and dimeric protein scaffold molecules [Z(HER2:477) and (Z(HER2:477))(2), respectively] were radiofluorinated at a reasonable radiochemical yield (13%-18%) by use of site-specific oxime chemistry. Oximes 224-229 erb-b2 receptor tyrosine kinase 2 Homo sapiens 29-33 18281016-0 2008 Effects of oximes on rate of decarbamylation of human red blood cell AChE measured with two different methods. Oximes 11-17 acetylcholinesterase (Cartwright blood group) Homo sapiens 69-73 18304715-1 2008 The efficacy of oxime treatment in soman poisoning is limited due to rapid aging of inhibited acetylcholinesterase (AChE). Oximes 16-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 94-114 18304715-1 2008 The efficacy of oxime treatment in soman poisoning is limited due to rapid aging of inhibited acetylcholinesterase (AChE). Oximes 16-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 116-120 18281016-2 2008 The treatment options in soman poisoning are very limited due to rapid aging of the inhibited acetylcholinesterase (AChE), when the enzyme species is considered as irreversibly inhibited and resistant towards reactivation by oximes. Oximes 225-231 acetylcholinesterase (Cartwright blood group) Homo sapiens 94-114 18281016-2 2008 The treatment options in soman poisoning are very limited due to rapid aging of the inhibited acetylcholinesterase (AChE), when the enzyme species is considered as irreversibly inhibited and resistant towards reactivation by oximes. Oximes 225-231 acetylcholinesterase (Cartwright blood group) Homo sapiens 116-120 18281016-6 2008 The question whether there is a possibility of an interaction between pre-treating carbamates and oximes at AChE arises. Oximes 98-104 acetylcholinesterase (Cartwright blood group) Homo sapiens 108-112 17914843-2 2007 1H NMR and fluorescence titrations revealed that receptors 2a and 2b, incorporating suitable positioned amine and oxime moieties, are able to form strong 1:1 complexes (Ka1 approximately 10(5) M-1) with dodecyl alpha- and beta-maltoside in chloroform solutions. Oximes 114-119 glutamate ionotropic receptor kainate type subunit 4 Homo sapiens 169-172 18035420-0 2008 Temporal effects of newly developed oximes (K027, K048) on malathion-induced acetylcholinesterase inhibition and lipid peroxidation in mouse prefrontal cortex. Oximes 36-42 acetylcholinesterase Mus musculus 77-97 17918908-4 2007 The ion/molecule reaction adduct and the oxime formed via its dehydration were observed using reactive DESI; the protonated and sodiated forms of the ionized steroid were also observed both in reactive DESI and in DESI performed without the added hydroxylamine reagent. Oximes 41-46 desumoylating isopeptidase 2 Homo sapiens 103-107 17370251-2 2007 The standard treatment with atropine and acetylcholinesterase (AChE) reactivators (oximes) is considered to be ineffective with certain nerve agents due to low oxime efficacy. Oximes 83-89 acetylcholinesterase (Cartwright blood group) Homo sapiens 41-61 17370251-2 2007 The standard treatment with atropine and acetylcholinesterase (AChE) reactivators (oximes) is considered to be ineffective with certain nerve agents due to low oxime efficacy. Oximes 83-89 acetylcholinesterase (Cartwright blood group) Homo sapiens 63-67 17370251-2 2007 The standard treatment with atropine and acetylcholinesterase (AChE) reactivators (oximes) is considered to be ineffective with certain nerve agents due to low oxime efficacy. Oximes 83-88 acetylcholinesterase (Cartwright blood group) Homo sapiens 41-61 17370251-2 2007 The standard treatment with atropine and acetylcholinesterase (AChE) reactivators (oximes) is considered to be ineffective with certain nerve agents due to low oxime efficacy. Oximes 83-88 acetylcholinesterase (Cartwright blood group) Homo sapiens 63-67 17370251-4 2007 The prospective oxime HI 6 is a weak reactivator of tabun- and pesticide-inhibited AChE, while the established oxime obidoxime mainly lacks efficacy with cyclosarin-inhibited enzyme. Oximes 16-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 83-87 17964625-1 2008 To develop a new reactivator of inhibited acetylcholinesterase (AChE) that can easily penetrate the blood-brain barrier (BBB), BBB penetration of 6 known and novel pyridinealdoxime methiodide (PAM)-type oximes (alkylPAMs) with relatively high reactivation activities was examined by in vivo rat brain microdialysis with liquid chromatography-mass spectrometry (LC-MS/MS). Oximes 203-209 acetylcholinesterase Rattus norvegicus 42-62 17964625-1 2008 To develop a new reactivator of inhibited acetylcholinesterase (AChE) that can easily penetrate the blood-brain barrier (BBB), BBB penetration of 6 known and novel pyridinealdoxime methiodide (PAM)-type oximes (alkylPAMs) with relatively high reactivation activities was examined by in vivo rat brain microdialysis with liquid chromatography-mass spectrometry (LC-MS/MS). Oximes 203-209 acetylcholinesterase Rattus norvegicus 64-68 18054823-2 2008 OPs act primarily by inhibiting acetylcholinesterase (AChE), the standard treatment for which includes AChE reactivators (oximes) in combination with antimuscarinic drugs. Oximes 122-128 acetylcholinesterase (Yt blood group) Sus scrofa 32-52 18054823-2 2008 OPs act primarily by inhibiting acetylcholinesterase (AChE), the standard treatment for which includes AChE reactivators (oximes) in combination with antimuscarinic drugs. Oximes 122-128 acetylcholinesterase (Yt blood group) Sus scrofa 54-58 18054823-2 2008 OPs act primarily by inhibiting acetylcholinesterase (AChE), the standard treatment for which includes AChE reactivators (oximes) in combination with antimuscarinic drugs. Oximes 122-128 acetylcholinesterase (Yt blood group) Sus scrofa 103-107 17977518-0 2008 Comparison of the oxime-induced reactivation of erythrocyte and muscle acetylcholinesterase following inhibition by sarin or paraoxon, using a perfusion model for the real-time determination of membrane-bound acetylcholinesterase activity. Oximes 18-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 71-91 17977518-1 2008 The purpose of these experiments was to compare oxime-induced reactivation rate constants of acetylcholinesterase from different human tissue sources inhibited by organophosphorus compounds. Oximes 48-53 acetylcholinesterase (Cartwright blood group) Homo sapiens 93-113 18393843-10 2008 Oximes, by reactivating acetylcholinesterase, are important adjunct therapeutics in organophosphate poisoning. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 24-44 17869525-0 2007 New oxime reactivators connected with CH2O(CH2)nOCH2 linker and their reactivation potency for organophosphorus agents-inhibited acetylcholinesterase. Oximes 4-9 acetylcholinesterase Bos taurus 129-149 18220560-2 2007 The main drugs are anticholinergics that antagonize the effects of accumulated acetylcholine at the cholinergic synapses and cholinesterase reactivators (oximes) reactivating inhibited AChE. Oximes 154-160 butyrylcholinesterase Homo sapiens 125-139 18220560-2 2007 The main drugs are anticholinergics that antagonize the effects of accumulated acetylcholine at the cholinergic synapses and cholinesterase reactivators (oximes) reactivating inhibited AChE. Oximes 154-160 acetylcholinesterase (Cartwright blood group) Homo sapiens 185-189 18220560-9 2007 An universality of oximes able to reactivate AChE inhibited by all OP is questioned and therefore, needs of development of new oximes is underlined. Oximes 19-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 45-49 17716616-0 2007 Limitation of the Ellman method: cholinesterase activity measurement in the presence of oximes. Oximes 88-94 butyrylcholinesterase Homo sapiens 33-47 17716616-3 2007 Oximes, reactivators of inhibited cholinesterase, are nucleophiles that also react with ATCh (oximolysis), producing thiocholine and (indirectly) TNB ion. Oximes 0-6 butyrylcholinesterase Homo sapiens 34-48 17900152-1 2007 The reactivation of nerve agent-inhibited acetylcholinesterase (AChE) by oxime is the most important step in the treatment of nerve agent poisoning. Oximes 73-78 acetylcholinesterase (Cartwright blood group) Homo sapiens 64-68 17900152-4 2007 Several investigations have demonstrated that the efficacy of an oxime primarily depends on its ability to reactivate nerve agent-inhibited AChE. Oximes 65-70 acetylcholinesterase (Cartwright blood group) Homo sapiens 140-144 17900152-5 2007 If the in vitro oxime reactivation of nerve agent-inhibited animal AChE is similar to that of human AChE, it is likely that the results of an in vivo animal study will reliably extrapolate to humans. Oximes 16-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 67-71 17900152-7 2007 Reactivation kinetic studies with five mono- and bis-pyridinium oximes showed that oxime reactivation of nerve agent-inhibited human AChE in most cases was faster than guinea pig AChE. Oximes 64-69 acetylcholinesterase (Cartwright blood group) Homo sapiens 133-137 17443135-2 2007 Clinical treatment of nerve-agent poisoning is to use oxime-based antidotes to reactivate the inhibited AChE. Oximes 54-59 acetylcholinesterase (Cartwright blood group) Homo sapiens 104-108 17913691-2 2007 Therapeutic strategies are directed to antagonise overstimulation of muscarinic receptors with atropine and to reactivate inhibited AChE with oximes. Oximes 142-148 acetylcholinesterase (Cartwright blood group) Homo sapiens 132-136 17913691-11 2007 Oxime administration can be stopped when AChE is aged completely, but has to be continued as long as poison is present in the body and reactivation is possible. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 41-45 17443135-4 2007 To design improved oximes, crystal structures of a tabun-conjugated AChE in complex with different oximes are needed to guide the structural modifications of known antidotes. Oximes 19-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-72 17443135-4 2007 To design improved oximes, crystal structures of a tabun-conjugated AChE in complex with different oximes are needed to guide the structural modifications of known antidotes. Oximes 99-105 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-72 17304644-2 2007 The purpose of the study was to quantify in vivo the extent of oxime-conferred protection, using methyl-paraoxon [dimethyl p-nitrophenyl phosphate; (methyl-POX)] as a cholinesterase inhibitor. Oximes 63-68 butyrylcholinesterase Rattus norvegicus 167-181 17309042-1 2007 In the search for new oximes with higher reactivation potency and a broader spectrum, K-27 and K-48, have recently been synthesized. Oximes 22-28 keratin 27 Rattus norvegicus 86-90 17151865-4 2007 The comparison of the reaction rates of the three therapeutically used oximes (2-PAM, obidoxime, HI 6) with the respective OPC gave the highest rate for crotylsarin and cyclosarin with obidoxime and to a similar degree with HI 6, while in the case of VX the most reactive oxime was HI 6. Oximes 71-77 peptidylglycine alpha-amidating monooxygenase Homo sapiens 81-84 17151865-4 2007 The comparison of the reaction rates of the three therapeutically used oximes (2-PAM, obidoxime, HI 6) with the respective OPC gave the highest rate for crotylsarin and cyclosarin with obidoxime and to a similar degree with HI 6, while in the case of VX the most reactive oxime was HI 6. Oximes 71-76 peptidylglycine alpha-amidating monooxygenase Homo sapiens 81-84 17382909-3 2007 Reactivators (oximes) of inhibited AChE are a mainstay of treatment. Oximes 14-20 acetylcholinesterase (Cartwright blood group) Homo sapiens 35-39 17382909-4 2007 However, human AChE inhibited by certain OP, e.g. the phosphoramidates tabun and fenamiphos, is rather resistant towards reactivation by oximes while AChE inhibited by others, e.g. the phosphoramidate methamidophos is easily reactivated by oximes. Oximes 137-143 acetylcholinesterase (Cartwright blood group) Homo sapiens 15-19 17382909-4 2007 However, human AChE inhibited by certain OP, e.g. the phosphoramidates tabun and fenamiphos, is rather resistant towards reactivation by oximes while AChE inhibited by others, e.g. the phosphoramidate methamidophos is easily reactivated by oximes. Oximes 240-246 acetylcholinesterase (Cartwright blood group) Homo sapiens 15-19 17382909-6 2007 A clear structure-activity relationship of aging, spontaneous and oxime-induced reactivation kinetics could be determined with AChE inhibited by N-monoalkyl tabun analogues depending on the chain length of the N-alkyl residue. Oximes 66-71 acetylcholinesterase (Cartwright blood group) Homo sapiens 127-131 17383875-4 2007 Notably, the oxime group in position four substantially increased the ability of the novel compounds to reactivate paraoxon-inhibited AChE. Oximes 13-18 acetylcholinesterase (Cartwright blood group) Homo sapiens 134-138 17674811-1 2007 The potency of newly developed oximes (K074, K075) and commonly used oximes (obidoxime, HI-6) to reactivate nerve agent-inhibited acetylcholinesterase was evaluated in rats poisoned with tabun or cyclosarin at a lethal dose corresponding to the LD50 value. Oximes 31-37 acetylcholinesterase Rattus norvegicus 130-150 17674811-1 2007 The potency of newly developed oximes (K074, K075) and commonly used oximes (obidoxime, HI-6) to reactivate nerve agent-inhibited acetylcholinesterase was evaluated in rats poisoned with tabun or cyclosarin at a lethal dose corresponding to the LD50 value. Oximes 69-75 acetylcholinesterase Rattus norvegicus 130-150 17674811-3 2007 On the other hand, one of the newly developed oximes (K074) seems to be a significantly more efficacious reactivator of tabun-inhibited acetylcholinesterase in the central compartment (brain) than the other studied oximes. Oximes 46-52 acetylcholinesterase Rattus norvegicus 136-156 17504181-3 2007 Oximes hydrolytically cleave the organophosphates from acetylcholinesterase (AChE), restoring enzymatic function. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 55-75 17504181-3 2007 Oximes hydrolytically cleave the organophosphates from acetylcholinesterase (AChE), restoring enzymatic function. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 77-81 17504181-9 2007 An universality of oximes able to reactivate AChE inhibited by all OP is questioned and trends (molecular modelling using neural network, structure-activity relationship, combination of reactivation and anticholinergic properties in one molecule) for future research are characterized. Oximes 19-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 45-49 16904809-2 2007 OP inhibit acetylcholinesterase (AChE) and therefore standard treatment of respective poisoning includes AChE reactivators (oximes) in combination with antimuscarinic agents. Oximes 124-130 acetylcholinesterase (Cartwright blood group) Homo sapiens 105-109 17402711-2 2007 The formed AChE-OP conjugate subsequently undergoes an elimination reaction, termed aging, that results in an enzyme completely resistant to oxime-mediated reactivation by medical antidotes. Oximes 141-146 acetylcholinesterase Mus musculus 11-15 16904807-2 2007 Standard treatment with atropine and the established acetylcholinesterase (AChE) reactivators, obidoxime and pralidoxime, is considered to be ineffective with certain nerve agents due to low oxime effectiveness. Oximes 99-104 acetylcholinesterase (Cartwright blood group) Homo sapiens 53-73 16904807-2 2007 Standard treatment with atropine and the established acetylcholinesterase (AChE) reactivators, obidoxime and pralidoxime, is considered to be ineffective with certain nerve agents due to low oxime effectiveness. Oximes 99-104 acetylcholinesterase (Cartwright blood group) Homo sapiens 75-79 16904807-5 2007 Since reactivation of OP-inhibited AChE is considered to be the main mechanism of action of oximes, human erythrocyte AChE can be exploited to test the efficacy of new oximes. Oximes 92-98 acetylcholinesterase (Cartwright blood group) Homo sapiens 35-39 16904807-6 2007 Recently, a dynamic computer model was developed which allows the calculation of AChE activities at different scenarios by combining enzyme kinetics (inhibition, reactivation, aging) with OP toxicokinetics and oxime pharmacokinetics. Oximes 210-215 acetylcholinesterase (Cartwright blood group) Homo sapiens 81-85 16904807-9 2007 The model presented may serve as a tool for evaluating the impact of carbamate pretreatment on oxime-induced reactivation of inhibited AChE, for defining effective oxime concentrations and for optimizing oxime treatment. Oximes 95-100 acetylcholinesterase (Cartwright blood group) Homo sapiens 135-139 16904807-9 2007 The model presented may serve as a tool for evaluating the impact of carbamate pretreatment on oxime-induced reactivation of inhibited AChE, for defining effective oxime concentrations and for optimizing oxime treatment. Oximes 164-169 acetylcholinesterase (Cartwright blood group) Homo sapiens 135-139 16904807-9 2007 The model presented may serve as a tool for evaluating the impact of carbamate pretreatment on oxime-induced reactivation of inhibited AChE, for defining effective oxime concentrations and for optimizing oxime treatment. Oximes 164-169 acetylcholinesterase (Cartwright blood group) Homo sapiens 135-139 16904808-2 2007 Presently, standard treatment includes administration of an antimuscarinic agent (e.g. atropine) and a reactivator of inhibited AChE (oxime), but is considered to be rather ineffective with certain nerve agents due to low oxime effectiveness of the currently available oximes, obidoxime and pralidoxime. Oximes 134-139 acetylcholinesterase (Cartwright blood group) Homo sapiens 128-132 16904808-5 2007 A dynamic in vitro model, which allows the calculation of AChE activities at different scenarios was developed to facilitate the definition of effective oxime concentrations and the optimization of oxime treatment of OP poisoning of humans and may furthermore be helpful by designing animal experiments. Oximes 153-158 acetylcholinesterase (Cartwright blood group) Homo sapiens 58-62 16904808-5 2007 A dynamic in vitro model, which allows the calculation of AChE activities at different scenarios was developed to facilitate the definition of effective oxime concentrations and the optimization of oxime treatment of OP poisoning of humans and may furthermore be helpful by designing animal experiments. Oximes 198-203 acetylcholinesterase (Cartwright blood group) Homo sapiens 58-62 16904808-6 2007 The model is based on a combination of enzyme kinetics (inhibition, reactivation, aging) of AChE with OP, toxicokinetics and oxime pharmacokinetics. Oximes 125-130 acetylcholinesterase (Cartwright blood group) Homo sapiens 92-96 16904808-8 2007 Due to a low affinity of HI 6 with VR-inhibited pig AChE the oxime dose that causes maximal reactivation of VR-inhibited pig AChE is conspicuously higher compared to humans. Oximes 61-66 acetylcholinesterase Sus scrofa 52-56 16904808-8 2007 Due to a low affinity of HI 6 with VR-inhibited pig AChE the oxime dose that causes maximal reactivation of VR-inhibited pig AChE is conspicuously higher compared to humans. Oximes 61-66 acetylcholinesterase Sus scrofa 125-129 17046138-0 2007 Mutation of acetylcholinesterase to enhance oxime-assisted catalytic turnover of methylphosphonates. Oximes 44-49 acetylcholinesterase Mus musculus 12-32 17046138-1 2007 Selected mutagenesis of acetylcholinesterase (AChE; EC 3.1.1.7) may enable one to develop more effective scavenging agents in which AChE itself, in combination with an oxime, will complete a catalytic cycle of hydrolysis of the organophosphate by rapid conjugation followed by enhanced nucleophile-mediated hydrolysis of the phosphonyl enzyme conjugate. Oximes 168-173 acetylcholinesterase Mus musculus 24-44 17046138-1 2007 Selected mutagenesis of acetylcholinesterase (AChE; EC 3.1.1.7) may enable one to develop more effective scavenging agents in which AChE itself, in combination with an oxime, will complete a catalytic cycle of hydrolysis of the organophosphate by rapid conjugation followed by enhanced nucleophile-mediated hydrolysis of the phosphonyl enzyme conjugate. Oximes 168-173 acetylcholinesterase Mus musculus 46-50 17196318-2 2007 We discuss here how acetylcholinesterase (AChE), through appropriate mutations, becomes more susceptible to oxime reactivation. Oximes 108-113 acetylcholinesterase (Cartwright blood group) Homo sapiens 20-40 17196318-2 2007 We discuss here how acetylcholinesterase (AChE), through appropriate mutations, becomes more susceptible to oxime reactivation. Oximes 108-113 acetylcholinesterase (Cartwright blood group) Homo sapiens 42-46 17196318-4 2007 Accordingly, "Oxime-assisted Catalysis" by AChE provides a potential means for catalyzing the hydrolysis of organophosphates in plasma prior to their reaching the cellular target site. Oximes 14-19 acetylcholinesterase (Cartwright blood group) Homo sapiens 43-47 17010492-10 2007 This oxime concentration reactivated RBC-AChE>20% of normal in most cases of OP poisoning by diethylphosphoryl compounds within a few hours. Oximes 5-10 acetylcholinesterase (Cartwright blood group) Homo sapiens 41-45 16904809-5 2007 Recently, we studied the reactivating potency of several oximes with human AChE inhibited by structurally different OP and observed remarkable differences depending on the OP and oxime. Oximes 57-63 acetylcholinesterase (Cartwright blood group) Homo sapiens 75-79 16904809-5 2007 Recently, we studied the reactivating potency of several oximes with human AChE inhibited by structurally different OP and observed remarkable differences depending on the OP and oxime. Oximes 57-62 acetylcholinesterase (Cartwright blood group) Homo sapiens 75-79 16904809-10 2007 In contrast, no structure-activity dependence could be observed for the oxime-induced reactivation of AChE and BChE inhibited by the compounds tested. Oximes 72-77 acetylcholinesterase (Cartwright blood group) Homo sapiens 102-106 16904809-10 2007 In contrast, no structure-activity dependence could be observed for the oxime-induced reactivation of AChE and BChE inhibited by the compounds tested. Oximes 72-77 butyrylcholinesterase Homo sapiens 111-115 16904809-11 2007 In general, OP-inhibited AChE and BChE were susceptible towards reactivation by oximes. Oximes 80-86 acetylcholinesterase (Cartwright blood group) Homo sapiens 25-29 16904809-11 2007 In general, OP-inhibited AChE and BChE were susceptible towards reactivation by oximes. Oximes 80-86 butyrylcholinesterase Homo sapiens 34-38 16962227-4 2007 All oximes inhibited human AChE reversibly, and the inhibition potency increased in the following order Py-4-Br<Py-4-Cl<Py-4-CH(3)<Py-4-H<Py-4-NO(2). Oximes 4-10 acetylcholinesterase (Cartwright blood group) Homo sapiens 27-31 16962227-5 2007 Although oximes Py-4-H and Py-4-NO(2) did not show significant reactivation ability, these oximes might be of interest as pre-treatment drugs due to their high affinity for the native AChE. Oximes 91-97 acetylcholinesterase (Cartwright blood group) Homo sapiens 184-188 16962227-7 2007 The orientations of all studied oximes in the active site of human AChE have been proposed by flexible ligand docking with AutoDock 3.0. Oximes 32-38 acetylcholinesterase (Cartwright blood group) Homo sapiens 67-71 17112559-3 2007 Reactivators (oximes) of inhibited AChE are a mainstay of treatment, however, the commercially available compounds, obidoxime and pralidoxime, are considered to be rather ineffective against various nerve agents, e.g. soman and cyclosarin. Oximes 14-20 acetylcholinesterase (Cartwright blood group) Homo sapiens 35-39 17298091-0 2007 Oxime-induced reactivation of sarin-inhibited AChE: a theoretical mechanisms study. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 46-50 17298091-3 2007 The potential energy surface along the pathway of the reactivation reaction of sarin-inhibited AChE by oxime reveals that the reaction can occur quickly due to the relatively low energy barriers. Oximes 103-108 acetylcholinesterase (Cartwright blood group) Homo sapiens 95-99 17335104-1 2007 Some oxime ether-substituted aryloxypropanolamines 3-5, structurally related to the active metabolite 2 of sarpogrelate 1, were synthesized and tested for their affinities at 5-HT2A and 5-HT1A serotoninergic receptors as well as at the alpha1-adrenoceptor. Oximes 5-10 5-hydroxytryptamine receptor 2A Homo sapiens 175-181 17456837-6 2007 Oximes, as a part of antidotal therapy, ensure the recovery of phosphylated enzymes via a process denoted as reactivation of inhibited AChE. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 135-139 17456837-11 2007 An oxime HLo-7 seems to be an efficient reactivator of AChE inhibited by any of the four organophosphorus warfare agents. Oximes 3-8 acetylcholinesterase (Cartwright blood group) Homo sapiens 55-59 17456837-12 2007 According to the available literature, the oximes LuH-6 and TMB-4, although relatively toxic, are the most potent to induce reactivation of AChE inhibited by the majority of organophosphorus pesticides. Oximes 43-49 acetylcholinesterase (Cartwright blood group) Homo sapiens 140-144 17265452-0 2007 In vitro oxime reactivation of red blood cell acetylcholinesterase inhibited by methyl-paraoxon. Oximes 9-14 acetylcholinesterase (Cartwright blood group) Homo sapiens 46-66 17265452-15 2007 The ranking of reactivator potencies of the examined oximes determined with methyl-POX as an inhibitor (K-27 = K-48 > K-33 > pralidoxime > methoxime) is similar to the ranking previously reported by us using POX as an inhibitor (K-27 > or = K-48 > K-33 > methoxime = pralidoxime). Oximes 53-59 keratin 27 Homo sapiens 238-242 17112559-5 2007 Reactivation of OP-inhibited AChE is considered to be the most important reaction of oximes. Oximes 85-91 acetylcholinesterase (Cartwright blood group) Homo sapiens 29-33 17112559-6 2007 Clinical data from studies with pesticide-poisoned patients support the assumption that the various reactions between AChE, OP and oxime, i.e. inhibition, reactivation and aging, can be investigated in vitro with human AChE. Oximes 131-136 acetylcholinesterase (Cartwright blood group) Homo sapiens 219-223 18254274-0 2007 Evaluation of potency of known oximes (pralidoxime, trimedoxime, HI-6, methoxime, obidoxime) to in vitro reactivate acetylcholinesterase inhibited by pesticides (chlorpyrifos and methylchlorpyrifos) and nerve agent (Russian VX). Oximes 31-37 acetylcholinesterase (Cartwright blood group) Homo sapiens 116-136 17188490-4 2007 An X-ray co-crystal of structure 11 revealed that the oxime moiety was mimicking the C-ring of genistein, as previously predicted by SAR and docking studies. Oximes 54-59 sarcosine dehydrogenase Homo sapiens 133-136 17370870-2 2007 Concerns have been expressed over the safety and efficacy of the use of oximes such as pralidoxime (2-PAM) in patients with carbamate poisoning in general, and more so with carbaryl poisoning specifically. Oximes 72-78 peptidylglycine alpha-amidating monooxygenase Homo sapiens 102-105 17126503-0 2007 Cholinesterase pseudo-activity, oximolysis, esterolysis, thiocholine ester hydrolysis by oximes: what"s in a name? Oximes 89-95 butyrylcholinesterase Homo sapiens 0-14 16971069-7 2006 All of these oximes showed esterase-like activity, and their strengths were consistent with those of known reactivators of inhibited AChE. Oximes 13-19 acetylcholinesterase (Cartwright blood group) Homo sapiens 133-137 17265677-0 2006 Substituted monoquaternary oximes as reactivators of cyclosarin--and chlorpyrifos--inhibited acetylcholinesterase. Oximes 27-33 acetylcholinesterase Rattus norvegicus 93-113 17265677-7 2006 In case of chlorpyrifos, TO231 was the most potent AChE reactivator with an 82 % reactivation at 1.0 mmol L(-1) oxime concentration. Oximes 112-117 acetylcholinesterase Rattus norvegicus 51-55 16904331-5 2006 Further in vivo studies employing a rat carrageenan-induced paw edema model showed that the oxime compounds (17a, 18a) were more potent anti-inflammatory agents than the 5-LOX inhibitor caffeic acid, and 15-LOX inhibitor nordihydroguaiaretic acid (NDGA), but less potent than the selective COX-2 inhibitor celecoxib. Oximes 92-97 cytochrome c oxidase II, mitochondrial Rattus norvegicus 290-295 16979339-2 2006 With a 4-fluoro-2-methylindol-5-yloxy group at the 6-position and alkyl groups as the oxime side chains, many analogues showed good potency for VEGFR-2. Oximes 86-91 kinase insert domain receptor Homo sapiens 144-151 17252938-1 2006 Antidotes currently used for organophosphorus pesticide and nerve agent intoxications consist of anticholinergics (atropine mainly) and acetylcholinesterase (AChE, EC 3.1.1.7) reactivators called oximes. Oximes 196-202 acetylcholinesterase (Cartwright blood group) Homo sapiens 136-156 17252938-1 2006 Antidotes currently used for organophosphorus pesticide and nerve agent intoxications consist of anticholinergics (atropine mainly) and acetylcholinesterase (AChE, EC 3.1.1.7) reactivators called oximes. Oximes 196-202 acetylcholinesterase (Cartwright blood group) Homo sapiens 158-162 18072133-0 2006 Reactivation of sarin-inhibited pig brain acetylcholinesterase using oxime antidotes. Oximes 69-74 acetylcholinesterase (Yt blood group) Sus scrofa 42-62 18072133-2 2006 AChE reactivators (also known as oximes) are generally used for the reactivation of an inhibited enzyme. Oximes 33-39 acetylcholinesterase (Yt blood group) Sus scrofa 0-4 18072133-6 2006 However, oxime HI-6 (33%) and obidoxime (23%) seem to be the best AChE reactivators for human relevant doses (10(-4) M and lower). Oximes 9-14 acetylcholinesterase (Cartwright blood group) Homo sapiens 66-70 16982122-5 2006 In addition, since butyrylcholinesterase (BChE; EC 3.1.1.8) is considered an endogenous bioscavenger of anticholinesterase compounds and its interactions with oximes could be masked by AChE interactions, we evaluated kinetic parameters for interactions of tested oximes with native and tabun-inhibited human plasma BChE and compared them with results obtained previously for human erythrocyte acetylcholinesterase (AChE; EC 3.1.1.7). Oximes 159-165 butyrylcholinesterase Homo sapiens 42-46 16982122-5 2006 In addition, since butyrylcholinesterase (BChE; EC 3.1.1.8) is considered an endogenous bioscavenger of anticholinesterase compounds and its interactions with oximes could be masked by AChE interactions, we evaluated kinetic parameters for interactions of tested oximes with native and tabun-inhibited human plasma BChE and compared them with results obtained previously for human erythrocyte acetylcholinesterase (AChE; EC 3.1.1.7). Oximes 159-165 acetylcholinesterase (Cartwright blood group) Homo sapiens 185-189 16982122-5 2006 In addition, since butyrylcholinesterase (BChE; EC 3.1.1.8) is considered an endogenous bioscavenger of anticholinesterase compounds and its interactions with oximes could be masked by AChE interactions, we evaluated kinetic parameters for interactions of tested oximes with native and tabun-inhibited human plasma BChE and compared them with results obtained previously for human erythrocyte acetylcholinesterase (AChE; EC 3.1.1.7). Oximes 159-165 butyrylcholinesterase Homo sapiens 315-319 16982122-5 2006 In addition, since butyrylcholinesterase (BChE; EC 3.1.1.8) is considered an endogenous bioscavenger of anticholinesterase compounds and its interactions with oximes could be masked by AChE interactions, we evaluated kinetic parameters for interactions of tested oximes with native and tabun-inhibited human plasma BChE and compared them with results obtained previously for human erythrocyte acetylcholinesterase (AChE; EC 3.1.1.7). Oximes 159-165 acetylcholinesterase (Cartwright blood group) Homo sapiens 415-419 16982122-7 2006 The reactivation of tabun-inhibited BChE by oximes was very slow, and BChE binding affinity for oximes was lower than AChE"s. Oximes 44-50 butyrylcholinesterase Homo sapiens 36-40 16982122-8 2006 Therefore, BChE could scavenge tabun prior to AChE inhibition, but fast oxime-assisted reactivation of tabun-inhibited AChE or protection of AChE by oxime against inhibition with tabun would not be obstructed by interaction between BChE and oximes. Oximes 72-77 acetylcholinesterase (Cartwright blood group) Homo sapiens 119-123 16982122-8 2006 Therefore, BChE could scavenge tabun prior to AChE inhibition, but fast oxime-assisted reactivation of tabun-inhibited AChE or protection of AChE by oxime against inhibition with tabun would not be obstructed by interaction between BChE and oximes. Oximes 72-77 acetylcholinesterase (Cartwright blood group) Homo sapiens 119-123 16982122-8 2006 Therefore, BChE could scavenge tabun prior to AChE inhibition, but fast oxime-assisted reactivation of tabun-inhibited AChE or protection of AChE by oxime against inhibition with tabun would not be obstructed by interaction between BChE and oximes. Oximes 72-77 butyrylcholinesterase Homo sapiens 232-236 16919943-1 2006 A series of multi-substituted oximes were prepared and their potencies for inhibiting lipoprotein-associated phospholipase A(2) (Lp-PLA(2)) activity were evaluated in vitro. Oximes 30-36 phospholipase A2 group VII Homo sapiens 86-127 16919943-1 2006 A series of multi-substituted oximes were prepared and their potencies for inhibiting lipoprotein-associated phospholipase A(2) (Lp-PLA(2)) activity were evaluated in vitro. Oximes 30-36 phospholipase A2 group VII Homo sapiens 129-138 16690067-1 2006 A simple and reliable HPLC method for the determination of the plasma level of K-27, an oxime type antidote of use in organophosphorus poisoning is presented. Oximes 88-93 keratin 27 Rattus norvegicus 79-83 16876764-2 2006 The inhibited AChE may be reactivated by certain oximes as antidotes for clinical treatment of OP-intoxications. Oximes 49-55 acetylcholinesterase Mus musculus 14-18 16876764-3 2006 Crystal structures of the oximes HI-6, Ortho-7 and obidoxime in complex with Mus musculus acetylcholinesterase (mAChE) reveal different roles of the peripheral anionic site (PAS) in the binding of the oximes. Oximes 26-32 acetylcholinesterase Mus musculus 90-110 16876764-3 2006 Crystal structures of the oximes HI-6, Ortho-7 and obidoxime in complex with Mus musculus acetylcholinesterase (mAChE) reveal different roles of the peripheral anionic site (PAS) in the binding of the oximes. Oximes 201-207 acetylcholinesterase Mus musculus 90-110 16766478-2 2006 Both H oximes (HI-6, HLo-7) and the oxime BI-6 were found to be more efficacious reactivators of VX-inhibited acetylcholinesterase than pralidoxime and obidoxime. Oximes 7-12 acetylcholinesterase Rattus norvegicus 110-130 17194020-8 2006 Moreover, from the obtained results it could be deduced that AChE reactivators with a functional oxime group in position-2 are the most potent AChE reactivators in the case of cyclosarin intoxications. Oximes 97-102 acetylcholinesterase (Cartwright blood group) Homo sapiens 61-65 17194020-8 2006 Moreover, from the obtained results it could be deduced that AChE reactivators with a functional oxime group in position-2 are the most potent AChE reactivators in the case of cyclosarin intoxications. Oximes 97-102 acetylcholinesterase (Cartwright blood group) Homo sapiens 143-147 17194021-6 2006 Furthermore effects of two conventional oximes paralidoxime (A) and obidoxime (B) on reactivation of the inhibited hAChE were studied but low reactivity was shown by both the oximes. Oximes 40-46 acetylcholinesterase (Cartwright blood group) Homo sapiens 115-120 16952906-1 2006 The potency of newly developed asymmetric bispyridinium oximes (K027, K048) in reactivating tabun-inhibited acetylcholinesterase (AChE) and in eliminating tabun-induced acute toxic effects was compared with commonly used oximes (obidoxime, trimedoxime, the oxime HI-6) using in vivo methods. Oximes 56-62 acetylcholinesterase Rattus norvegicus 108-128 16952906-1 2006 The potency of newly developed asymmetric bispyridinium oximes (K027, K048) in reactivating tabun-inhibited acetylcholinesterase (AChE) and in eliminating tabun-induced acute toxic effects was compared with commonly used oximes (obidoxime, trimedoxime, the oxime HI-6) using in vivo methods. Oximes 56-62 acetylcholinesterase Rattus norvegicus 130-134 16952906-1 2006 The potency of newly developed asymmetric bispyridinium oximes (K027, K048) in reactivating tabun-inhibited acetylcholinesterase (AChE) and in eliminating tabun-induced acute toxic effects was compared with commonly used oximes (obidoxime, trimedoxime, the oxime HI-6) using in vivo methods. Oximes 56-61 acetylcholinesterase Rattus norvegicus 108-128 16952906-1 2006 The potency of newly developed asymmetric bispyridinium oximes (K027, K048) in reactivating tabun-inhibited acetylcholinesterase (AChE) and in eliminating tabun-induced acute toxic effects was compared with commonly used oximes (obidoxime, trimedoxime, the oxime HI-6) using in vivo methods. Oximes 56-61 acetylcholinesterase Rattus norvegicus 130-134 16952906-5 2006 In addition, our results confirm that the efficacy of oximes in reactivating tabun-inhibited AChE in blood, diaphragm, and brain correlates with the potency of oximes in protecting rats poisoned with supralethal doses of tabun. Oximes 54-60 acetylcholinesterase Rattus norvegicus 93-97 16720069-2 2006 OP inhibit acetylcholinesterase (AChE), therefore, standard treatment includes AChE reactivators (oximes) in combination with antimuscarinic agents. Oximes 98-104 acetylcholinesterase (Cartwright blood group) Homo sapiens 79-83 16720069-9 2006 The potency of the investigated oximes was remarkably lower with OP-inhibited pig AChE. Oximes 32-38 acetylcholinesterase (Yt blood group) Sus scrofa 82-86 16740352-2 2006 Presently, standard treatment of poisoning by OP includes administration of atropine as an antimuscarinic agent and of oximes, e.g. obidoxime or pralidoxime, as reactivators of OP-inhibited acetylcholinesterase (AChE), but is considered to be rather ineffective with certain nerve agents. Oximes 119-125 acetylcholinesterase (Cartwright blood group) Homo sapiens 212-216 16740352-4 2006 A computer simulation based on combination of AChE kinetic data (inhibition, reactivation, aging) with OP toxicokinetics and oxime pharmacokinetics allows the calculation of AChE activities at different scenarios and may facilitate to define effective oxime concentrations and to optimize oxime dosage in OP poisoning. Oximes 125-130 acetylcholinesterase (Cartwright blood group) Homo sapiens 174-178 16740352-4 2006 A computer simulation based on combination of AChE kinetic data (inhibition, reactivation, aging) with OP toxicokinetics and oxime pharmacokinetics allows the calculation of AChE activities at different scenarios and may facilitate to define effective oxime concentrations and to optimize oxime dosage in OP poisoning. Oximes 252-257 acetylcholinesterase (Cartwright blood group) Homo sapiens 46-50 16740352-4 2006 A computer simulation based on combination of AChE kinetic data (inhibition, reactivation, aging) with OP toxicokinetics and oxime pharmacokinetics allows the calculation of AChE activities at different scenarios and may facilitate to define effective oxime concentrations and to optimize oxime dosage in OP poisoning. Oximes 252-257 acetylcholinesterase (Cartwright blood group) Homo sapiens 174-178 16740352-4 2006 A computer simulation based on combination of AChE kinetic data (inhibition, reactivation, aging) with OP toxicokinetics and oxime pharmacokinetics allows the calculation of AChE activities at different scenarios and may facilitate to define effective oxime concentrations and to optimize oxime dosage in OP poisoning. Oximes 252-257 acetylcholinesterase (Cartwright blood group) Homo sapiens 46-50 16740352-4 2006 A computer simulation based on combination of AChE kinetic data (inhibition, reactivation, aging) with OP toxicokinetics and oxime pharmacokinetics allows the calculation of AChE activities at different scenarios and may facilitate to define effective oxime concentrations and to optimize oxime dosage in OP poisoning. Oximes 252-257 acetylcholinesterase (Cartwright blood group) Homo sapiens 174-178 16644174-2 2006 In the event of poisoning, a combination of three drugs is commonly used: an anticholinergic drug (e.g. atropine), an oxime used as cholinesterase reactivator (e.g. pralidoxime or HI-6) and an anticonvulsant (i.e. benzodiazepine). Oximes 118-123 butyrylcholinesterase Homo sapiens 132-146 16913699-7 2006 Our results suggest that the oximes provide a novel structural linker for 4-arylpiperazine-based D4 agonists, possessing leadlike quality and with potential to develop a new class of potent and selective dopamine D4 receptor agonists. Oximes 29-35 dopamine receptor D4 Rattus norvegicus 204-224 16515465-5 2006 Anticholinergic drugs block effects of accumulated neurotransmitter acetylcholine at nicotinic and muscarinic receptor sites, while oximes reactivate AChE inhibited by OPCs. Oximes 132-138 acetylcholinesterase (Cartwright blood group) Homo sapiens 150-154 16782588-3 2006 The pharmacological action of oximes is multiple: they are able to reactivate the inhibited AChE, but they affect acetylcholine release in peripheral and central cholinergic synapses, allosterically modulate the muscarinic receptors in peripheral and central synapses, and influence the nicotinic receptor-associated ion-channels. Oximes 30-36 acetylcholinesterase Mus musculus 92-96 16522109-2 2006 The one-pot sequential reaction was conducted on a surface of human carbonic anhydrase II (hCAII) based on the affinity labeling and the subsequent hydrazone/oxime exchange reaction. Oximes 158-163 carbonic anhydrase 2 Homo sapiens 68-89 16522109-2 2006 The one-pot sequential reaction was conducted on a surface of human carbonic anhydrase II (hCAII) based on the affinity labeling and the subsequent hydrazone/oxime exchange reaction. Oximes 158-163 carbonic anhydrase 2 Homo sapiens 91-96 16583462-5 2006 Based on our previous in vitro work the protection conferred by the various new oximes against inhibition by paraoxon as quantified by the IC(50) shift (nM increase in the IC(50) of the inhibitor per microM oxime present) is: 0.3 (PRX), 0.4 (methoxime; MMC-4), 1 (K-33), 1.2 (BI-6), 1.5 (K-48) and 3.7 (K-27). Oximes 80-86 keratin 27 Rattus norvegicus 303-307 16583462-5 2006 Based on our previous in vitro work the protection conferred by the various new oximes against inhibition by paraoxon as quantified by the IC(50) shift (nM increase in the IC(50) of the inhibitor per microM oxime present) is: 0.3 (PRX), 0.4 (methoxime; MMC-4), 1 (K-33), 1.2 (BI-6), 1.5 (K-48) and 3.7 (K-27). Oximes 80-85 keratin 27 Rattus norvegicus 303-307 16598855-2 2006 The inhibition enzyme-oxime dissociation constants of AChE w.t. Oximes 22-27 acetylcholinesterase Mus musculus 54-58 16598855-6 2006 A high extent of oxime-assisted reactivation of all conjugates was achieved, but rates by both oximes were up to 10 times slower for phosphorylated mutants than for AChE w.t. Oximes 17-22 acetylcholinesterase Mus musculus 165-169 16623863-3 2006 Oximes counteract acetylcholine increase, resulting from AChE inhibition. Oximes 0-6 acetylcholinesterase (Cartwright blood group) Homo sapiens 57-61 16623863-6 2006 The usefulness of oxime in the reactivation process depends on its chemical structure and on the nerve agent whereby AChE is inhibited. Oximes 18-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 117-121 16515465-7 2006 Therefore, to find new oximes able to sufficiently reactivate inhibited AChE (regardless of the type of OPCs) is still very important task for medicinal chemistry with the aim to improve the efficacy of antidotal treatment of the acute poisonings mentioned. Oximes 23-29 acetylcholinesterase (Cartwright blood group) Homo sapiens 72-76 17438836-0 2006 Reactivation potency of new group of acetylcholinesterase reactivators and their comparison with currently available oximes. Oximes 117-123 acetylcholinesterase (Cartwright blood group) Homo sapiens 37-57 16332406-4 2006 All the oximes reversibly inhibited AChE, and the enzyme-oxime dissociation constants were between 17 and 180 microM. Oximes 8-14 acetylcholinesterase Mus musculus 36-40 16332406-4 2006 All the oximes reversibly inhibited AChE, and the enzyme-oxime dissociation constants were between 17 and 180 microM. Oximes 8-13 acetylcholinesterase Mus musculus 36-40 16332406-7 2006 Soman-inhibited AChE was resistant to reactivation by 1mM oximes. Oximes 58-64 acetylcholinesterase Mus musculus 16-20 16332406-8 2006 All studied oximes protected AChE from phosphorylation with both soman and tabun. Oximes 12-18 acetylcholinesterase Mus musculus 29-33 16393932-3 2005 In this study of cyclosarin poisoning treatment, oximes of different chemical structures (obidoxime, HI-6, BI-6, and HS-6) were tested in vitro on rat brain acetylcholinesterase (enzyme source: rat brain homogenate), and afterwards, they were tested in vivo in equimolar doses, in mice and rats. Oximes 49-55 acetylcholinesterase Rattus norvegicus 157-177 17438836-6 2006 From obtained results, it can be deduced, that only reactivators with oxime group in position two are able to reactivate cyclosarin-inhibited AChE. Oximes 70-75 acetylcholinesterase (Cartwright blood group) Homo sapiens 142-146 16193529-0 2006 Five oximes (K-27, K-33, K-48, BI-6 and methoxime) in comparison with pralidoxime: in vitro reactivation of red blood cell acetylcholinesterase inhibited by paraoxon. Oximes 5-11 acetylcholinesterase (Cartwright blood group) Homo sapiens 123-143 16193529-8 2006 The purpose of the study was to quantify in vitro the extent of oxime (pralidoxime, K-27, K-33, K-48, methoxime and BI-6) conferred protection, using paraoxon as an inhibitor. Oximes 64-69 keratin 27 Homo sapiens 84-88 17192653-2 2006 Presently, a combination of an antimuscarinic agent, e.g., atropine, and an AChE reactivator, oxime, is used for the treatment of organophosphorus compound poisoning. Oximes 94-99 acetylcholinesterase Mus musculus 76-80 16038577-4 2006 Correlation of the relative conversion of the oximes with Hammett parameters shows that radical effects dominate for the meta-substituted acetophenone oximes (rho(rad)/rho(pol) = 5.4; r2 = 0.93), whereas the para-substituted oximes are influenced almost equally by radical and ionic effects (rho(rad)/rho(pol) = -1.1; r2 = 0.98). Oximes 46-52 RRAD, Ras related glycolysis inhibitor and calcium channel regulator Homo sapiens 88-91 16038577-4 2006 Correlation of the relative conversion of the oximes with Hammett parameters shows that radical effects dominate for the meta-substituted acetophenone oximes (rho(rad)/rho(pol) = 5.4; r2 = 0.93), whereas the para-substituted oximes are influenced almost equally by radical and ionic effects (rho(rad)/rho(pol) = -1.1; r2 = 0.98). Oximes 46-52 rhodopsin Homo sapiens 292-316 17288495-1 2006 The traditional therapeutic treatment of organophosphate cholinesterase inhibitor (nerve agents) poisoning consists of co-treatment with an antimuscarinic (atropine) and a reactivator of inhibited acetylcholinesterase (AChE), which contains a nucleophilic oxime function. Oximes 256-261 acetylcholinesterase (Cartwright blood group) Homo sapiens 197-217 17288495-1 2006 The traditional therapeutic treatment of organophosphate cholinesterase inhibitor (nerve agents) poisoning consists of co-treatment with an antimuscarinic (atropine) and a reactivator of inhibited acetylcholinesterase (AChE), which contains a nucleophilic oxime function. Oximes 256-261 acetylcholinesterase (Cartwright blood group) Homo sapiens 219-223 17288500-13 2006 As a result, it is important that an oxime is administered as soon after soman exposure as possible so that some reactivation of AChE occurs before all the enzyme becomes aged. Oximes 37-42 acetylcholinesterase (Cartwright blood group) Homo sapiens 129-133 16263103-7 2005 Accordingly, RBC-AChE appears to be a suitable parameter for judgment of oxime effectiveness at the neuromuscular junction, one of the most important targets for therapy where atropine is ineffective in OP-poisoning. Oximes 73-78 acetylcholinesterase (Cartwright blood group) Homo sapiens 17-21 16266695-1 2005 Standard treatment of poisoning by organophosphorus compounds (OP) includes the administration of an anti-muscarinic, e.g. atropine, and of an acetylcholinesterase (AChE) reactivator (oxime). Oximes 184-189 acetylcholinesterase (Cartwright blood group) Homo sapiens 143-163 16266695-1 2005 Standard treatment of poisoning by organophosphorus compounds (OP) includes the administration of an anti-muscarinic, e.g. atropine, and of an acetylcholinesterase (AChE) reactivator (oxime). Oximes 184-189 acetylcholinesterase (Cartwright blood group) Homo sapiens 165-169 16266695-2 2005 Two oximes, obidoxime and pralidoxime (2-PAM), are presently commercially available, yet, these compounds are considered to be of insufficient efficacy against certain nerve agents, e.g. soman and cyclosarin. Oximes 4-10 peptidylglycine alpha-amidating monooxygenase Homo sapiens 41-44 16266695-7 2005 Reactivation of inhibited AChE is considered to be the main mechanism of action of oximes. Oximes 83-89 acetylcholinesterase (Cartwright blood group) Homo sapiens 26-30 16266695-8 2005 Clinical data indicate that changes in erythrocyte AChE activity correlate to neuromuscular function indicating that interactions between AChE, inhibitor and oximes can be investigated in vitro with human erythrocyte AChE. Oximes 158-164 acetylcholinesterase (Cartwright blood group) Homo sapiens 51-55 16266695-8 2005 Clinical data indicate that changes in erythrocyte AChE activity correlate to neuromuscular function indicating that interactions between AChE, inhibitor and oximes can be investigated in vitro with human erythrocyte AChE. Oximes 158-164 acetylcholinesterase (Cartwright blood group) Homo sapiens 138-142 16266695-8 2005 Clinical data indicate that changes in erythrocyte AChE activity correlate to neuromuscular function indicating that interactions between AChE, inhibitor and oximes can be investigated in vitro with human erythrocyte AChE. Oximes 158-164 acetylcholinesterase (Cartwright blood group) Homo sapiens 138-142 16266695-9 2005 Different theoretical models were used for the evaluation of reactivating efficacy of oximes with nerve agent-inhibited human AChE and for estimating effective oxime concentrations. Oximes 86-92 acetylcholinesterase (Cartwright blood group) Homo sapiens 126-130 16266695-9 2005 Different theoretical models were used for the evaluation of reactivating efficacy of oximes with nerve agent-inhibited human AChE and for estimating effective oxime concentrations. Oximes 86-91 acetylcholinesterase (Cartwright blood group) Homo sapiens 126-130 16293236-1 2005 Current antidotes for organophosphorus compounds (OP) poisoning consist of a combination of pretreatment with carbamates (pyridostigmine bromide), to protect acetylcholinesterase (AChE) from irreversible inhibition by OP compounds, and post-exposure therapy with anti-cholinergic drugs (atropine sulfate) to counteract the effects of excess acetylcholine and oximes (e.g., 2-PAM chloride) to reactivate OP-inhibited AChE. Oximes 359-365 acetylcholinesterase (Cartwright blood group) Homo sapiens 180-184 16429518-0 2005 Comparison of ability of some oximes to reactivate sarin-inhibited brain acetylcholinesterase from different species. Oximes 30-36 acetylcholinesterase (Cartwright blood group) Homo sapiens 73-93 16429518-2 2005 The results demonstrate remarkable differences in the reactivation of inhibited brain AChE, depending on the oxime and species Oximes 109-114 acetylcholinesterase (Cartwright blood group) Homo sapiens 86-90 16429526-0 2005 Acetylcholinesterase mutants: oxime-assisted catalytic scavengers of organophosphonates. Oximes 30-35 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-20 15904945-2 2005 Standard treatment with atropine and the established acetylcholinesterase (AChE) reactivators, obidoxime and pralidoxime, is considered to be ineffective with certain nerve agents due to low oxime effectiveness. Oximes 99-104 acetylcholinesterase (Cartwright blood group) Homo sapiens 53-73 15904945-2 2005 Standard treatment with atropine and the established acetylcholinesterase (AChE) reactivators, obidoxime and pralidoxime, is considered to be ineffective with certain nerve agents due to low oxime effectiveness. Oximes 99-104 acetylcholinesterase (Cartwright blood group) Homo sapiens 75-79 15904945-5 2005 Since reactivation of OP-inhibited AChE is considered to be the main mechanism of action of oximes, human erythrocyte AChE can be exploited to test the efficacy of new oximes. Oximes 92-98 acetylcholinesterase (Cartwright blood group) Homo sapiens 35-39 15904945-6 2005 By combining enzyme kinetics (inhibition, reactivation, aging) with OP toxicokinetics and oxime pharmacokinetics a dynamic in vitro model was developed which allows the calculation of AChE activities at different scenarios. Oximes 90-95 acetylcholinesterase (Cartwright blood group) Homo sapiens 184-188 16214344-0 2006 Inhibition of O-GlcNAcase by PUGNAc is dependent upon the oxime stereochemistry. Oximes 58-63 O-GlcNAcase Homo sapiens 14-25 16214344-1 2006 The potent O-GlcNAcase inhibitor PUGNAc was synthesized and two isomers based on the E and Z stereochemistry of the oxime moiety were separated, defined, and tested for activity. Oximes 116-121 O-GlcNAcase Homo sapiens 11-22 16601802-0 2005 A comparison of the potency of trimedoxime and other currently available oximes to reactivate tabun-inhibited acetylcholinesterase and eliminate acute toxic effects of tabun. Oximes 73-79 acetylcholinesterase Rattus norvegicus 110-130 16601802-3 2005 The potency of trimedoxime and other commonly used oximes (pralidoxime, obidoxime, the oxime HI-6) to reactivate tabun-inhibited acetylcholinesterase and to eliminate tabun-induced acute effects was evaluated using in vitro and in vivo methods. Oximes 51-57 acetylcholinesterase Rattus norvegicus 129-149 16601802-3 2005 The potency of trimedoxime and other commonly used oximes (pralidoxime, obidoxime, the oxime HI-6) to reactivate tabun-inhibited acetylcholinesterase and to eliminate tabun-induced acute effects was evaluated using in vitro and in vivo methods. Oximes 21-26 acetylcholinesterase Rattus norvegicus 129-149 16259317-0 2005 A comparison of the potency of the oxime HLo-7 and currently used oximes (HI-6, pralidoxime, obidoxime) to reactivate nerve agent-inhibited rat brain acetylcholinesterase by in vitro methods. Oximes 35-40 acetylcholinesterase Rattus norvegicus 150-170 16167316-2 2005 The standard treatment with atropine and acetylcholinesterase (AChE) reactivators ("oximes") is considered to be ineffective with certain nerve agents due to low oxime efficacy. Oximes 84-90 acetylcholinesterase (Cartwright blood group) Homo sapiens 41-61 16167316-2 2005 The standard treatment with atropine and acetylcholinesterase (AChE) reactivators ("oximes") is considered to be ineffective with certain nerve agents due to low oxime efficacy. Oximes 84-90 acetylcholinesterase (Cartwright blood group) Homo sapiens 63-67 16167316-2 2005 The standard treatment with atropine and acetylcholinesterase (AChE) reactivators ("oximes") is considered to be ineffective with certain nerve agents due to low oxime efficacy. Oximes 84-89 acetylcholinesterase (Cartwright blood group) Homo sapiens 41-61 16167316-2 2005 The standard treatment with atropine and acetylcholinesterase (AChE) reactivators ("oximes") is considered to be ineffective with certain nerve agents due to low oxime efficacy. Oximes 84-89 acetylcholinesterase (Cartwright blood group) Homo sapiens 63-67 16040183-3 2005 Here, oximes as potential reactivators of inhibited AChE may be effective. Oximes 6-12 acetylcholinesterase Mus musculus 52-56 16040183-12 2005 The data show different effectiveness of the oximes investigated in reactivation of muscle AChE and recovery of NMT after inhibition by paraoxon. Oximes 45-51 acetylcholinesterase Mus musculus 91-95 16040183-13 2005 Although an increase in muscle force by the oximes was accompanied by a measurable increase in AChE activity only in the case of obidoxime, the plot of muscle force against AChE activity as well as lacking evidence for a direct effect and adaptive processes indicate that reactivation of the enzyme is the main mechanism of NMT recovery. Oximes 44-50 acetylcholinesterase Mus musculus 95-99 16040183-14 2005 In agreement, in presence of AChE inhibitory concentrations of paraoxon during reactivation a reduced effectiveness of oximes was found. Oximes 119-125 acetylcholinesterase Mus musculus 29-33 16170392-6 2005 Oxime K048 seems to be promising reactivator of tabun-inhibited AChE. Oximes 0-5 acetylcholinesterase Rattus norvegicus 64-68 16170392-8 2005 The best reactivator of sarin-inhibited AChE seems to be oxime HI-6. Oximes 57-62 acetylcholinesterase Rattus norvegicus 40-44 16119192-0 2005 In vitro reactivation of sarin-inhibited brain acetylcholinesterase from different species by various oximes. Oximes 102-108 acetylcholinesterase (Yt blood group) Sus scrofa 47-67 16119192-1 2005 In vitro as well as in vivo evaluation of the reactivating efficacy of various oximes against nerve agent-inhibited acetylcholinesterase has been usually done with the help of animal experiments. Oximes 79-85 acetylcholinesterase (Yt blood group) Sus scrofa 116-136 16119192-3 2005 Therefore, to better evaluate the efficacy of various oximes (pralidoxime, obidoxime, HI-6, K033) to reactivate brain acetylcholinesterase inhibited by sarin by in vitro methods, human, rat and pig brain acetylcholinesterase were used to calculate kinetic parameters for the reactivation. Oximes 54-60 acetylcholinesterase (Cartwright blood group) Homo sapiens 118-138 16119193-6 2005 Three newly synthesized oximes achieved similar nucleophilicity at the similar pKa according to 4-PAM, which is very promising for using these derivatives as AChE reactivators. Oximes 24-30 acetylcholinesterase (Cartwright blood group) Homo sapiens 158-162 15686348-0 2005 Site-specific polymer attachment to a CCL-5 (RANTES) analogue by oxime exchange. Oximes 65-70 C-C motif chemokine ligand 5 Homo sapiens 38-43 15686348-0 2005 Site-specific polymer attachment to a CCL-5 (RANTES) analogue by oxime exchange. Oximes 65-70 C-C motif chemokine ligand 5 Homo sapiens 45-51 15679473-8 2005 Administration of the oxime produced a significant reactivation of central and peripheral acetylcholinesterase inhibited with dichlorvos and heptenophos, with the exception of erythrocyte acetylcholinesterase inhibited by heptenophos. Oximes 22-27 acetylcholinesterase Mus musculus 90-110 15989347-3 2005 In the presence of Pd(PPh3)4, the allylic substitution of oximes with allylic carbonate afforded the linear O-allylated oxime ethers selectively without a base. Oximes 58-64 caveolin 1 Homo sapiens 22-26 15989347-3 2005 In the presence of Pd(PPh3)4, the allylic substitution of oximes with allylic carbonate afforded the linear O-allylated oxime ethers selectively without a base. Oximes 58-63 caveolin 1 Homo sapiens 22-26 16021679-1 2005 The potency of currently used oximes to reactivate sarin-inhibited acetylcholinesterase (AChE) in various parts of pig brain and whole pig brain was evaluated using in vitro methods. Oximes 30-36 acetylcholinesterase Sus scrofa 89-93 16021679-3 2005 At concentrations (10(-4) M) corresponding to recommended doses in vivo, the oxime HI-6 seems to be a more efficacious reactivator of sarin-inhibited AChE in whole pig brain as well as in cerebral hemispheres and cerebellum compared with the other oximes studied. Oximes 77-82 acetylcholinesterase Sus scrofa 150-154 16025528-3 2005 All oximes are able to reactivate sarin-inhibited AChE. Oximes 4-10 acetylcholinesterase Rattus norvegicus 50-54 15901095-1 2005 The potency of newly developed and currently used oximes to reactivate sarin-inhibited acetylcholinesterase was evaluated using in vitro methods. Oximes 50-56 acetylcholinesterase Rattus norvegicus 87-107 15901095-4 2005 Although the ability of newly developed oximes to reactivate sarin-inhibited acetylcholinesterase does not reach the reactivating potency of the oxime HI-6, the oxime K033 seems to be a more efficacious reactivator of sarin-inhibited acetylcholinesterase than other currently available oximes (pralidoxime, obidoxime) at concentrations (10(-5)-10(-4)M) corresponding to recommended doses in vivo. Oximes 40-46 acetylcholinesterase Rattus norvegicus 77-97 15901095-4 2005 Although the ability of newly developed oximes to reactivate sarin-inhibited acetylcholinesterase does not reach the reactivating potency of the oxime HI-6, the oxime K033 seems to be a more efficacious reactivator of sarin-inhibited acetylcholinesterase than other currently available oximes (pralidoxime, obidoxime) at concentrations (10(-5)-10(-4)M) corresponding to recommended doses in vivo. Oximes 40-45 acetylcholinesterase Rattus norvegicus 77-97 15781395-2 2005 The oxime containing penam sulfones strongly inhibited the Escherichia coli TEM-1 and Klebsiella pneumoniae cefotaximase (CTX-1) enzymes, but moderately inhibited the Pseudomonas aeruginosa 46012 cephalosporinase; while the 2beta-substituted-hydrazone derivatives were generally less active against these enzymes. Oximes 4-9 hypothetical protein Escherichia coli 76-81 15859286-4 2005 Upon treatment of [ReV(NPh)Cl3(PPh3)2] with L1OH in solution, the neutral azoimine complex [ReV(NPh)Cl3(L1H)], 3, resulted due to the spontaneous transfer of the oxime oxygen atom to a PPh3 ligand, which is eliminated as OPPh3. Oximes 162-167 protein phosphatase 4 catalytic subunit Homo sapiens 31-35 15859286-5 2005 In contrast, the oxime of 2-acetylpyridine (L2OH, 4) did not undergo oxygen atom transfer and simply afforded the imine-oxime complex [ReV(NC6H4Y)Cl2(PPh3)(L2O)], 5, upon reacting with [ReV(NC6H4Y)Cl3(PPh3)2] (Y = H, Me, Cl). Oximes 17-22 protein phosphatase 4 catalytic subunit Homo sapiens 150-154 15859286-5 2005 In contrast, the oxime of 2-acetylpyridine (L2OH, 4) did not undergo oxygen atom transfer and simply afforded the imine-oxime complex [ReV(NC6H4Y)Cl2(PPh3)(L2O)], 5, upon reacting with [ReV(NC6H4Y)Cl3(PPh3)2] (Y = H, Me, Cl). Oximes 17-22 protein phosphatase 4 catalytic subunit Homo sapiens 201-205 15654704-2 2005 Standard treatment involves administration of intravenous atropine and oxime to counter acetylcholinesterase inhibition at the synapse. Oximes 71-76 acetylcholinesterase (Cartwright blood group) Homo sapiens 88-108 16259317-1 2005 (1) The efficacy of the oxime HLo7 and currently used oximes (pralidoxime, obidoxime, HI-6) to reactivate acetylcholinesterase inhibited by various nerve agents (sarin, tabun, cyclosarin, VX) was tested by in vitro methods. Oximes 24-29 acetylcholinesterase Rattus norvegicus 106-126 16259317-1 2005 (1) The efficacy of the oxime HLo7 and currently used oximes (pralidoxime, obidoxime, HI-6) to reactivate acetylcholinesterase inhibited by various nerve agents (sarin, tabun, cyclosarin, VX) was tested by in vitro methods. Oximes 54-60 acetylcholinesterase Rattus norvegicus 106-126 16259317-4 2005 In the case of cyclosarin, the oxime HI-6 was only found to be able to sufficiently reactivate cyclosarin-inhibited acetylcholinesterase in vitro. Oximes 31-36 acetylcholinesterase Rattus norvegicus 116-136 16259317-0 2005 A comparison of the potency of the oxime HLo-7 and currently used oximes (HI-6, pralidoxime, obidoxime) to reactivate nerve agent-inhibited rat brain acetylcholinesterase by in vitro methods. Oximes 66-72 acetylcholinesterase Rattus norvegicus 150-170 15532020-0 2004 Synthesis of branched oxime-linked peptide mimetics of the MUC1 containing a universal T-helper epitope. Oximes 22-27 mucin 1, cell surface associated Homo sapiens 59-63 15498514-0 2004 Kinetic analysis of interactions between human acetylcholinesterase, structurally different organophosphorus compounds and oximes. Oximes 123-129 acetylcholinesterase (Cartwright blood group) Homo sapiens 47-67 15498514-3 2004 Reactivators (oximes) of inhibited AChE are a mainstay of treatment, however, the commercially available compounds, obidoxime and pralidoxime, are considered to be rather ineffective against various nerve agents. Oximes 14-20 acetylcholinesterase (Cartwright blood group) Homo sapiens 35-39 15498514-5 2004 However, the various interactions between AChE, OP and oximes can be investigated with human AChE which enables the direct assessment of oxime potency, thus excluding species differences. Oximes 55-61 acetylcholinesterase (Cartwright blood group) Homo sapiens 93-97 15498514-5 2004 However, the various interactions between AChE, OP and oximes can be investigated with human AChE which enables the direct assessment of oxime potency, thus excluding species differences. Oximes 55-60 acetylcholinesterase (Cartwright blood group) Homo sapiens 93-97 15498514-7 2004 The inhibitory potency of OPs, reactivating potency of oximes and spontaneous reactivation and aging were strongly affected by the structural characteristics of the OPs and of the phosphyl-AChE-complex. Oximes 55-61 acetylcholinesterase (Cartwright blood group) Homo sapiens 189-193 15498514-9 2004 AChE inhibited by various phosphoramidates was mostly resistant towards reactivation by oximes while phosphonylated AChE was easily reactivated. Oximes 88-94 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-4 15386544-2 2004 In the case of the latter compounds, oximation is accompanied by epimerization at C-5 to avoid the A(1,3)-strain between the oxime OH group and the 5e-aryl ring of the initially formed oxime resulting in 2e,3e,5a,6e-tetraarylpiperidin-4-one oximes. Oximes 125-130 complement C5 Homo sapiens 82-85 15386544-2 2004 In the case of the latter compounds, oximation is accompanied by epimerization at C-5 to avoid the A(1,3)-strain between the oxime OH group and the 5e-aryl ring of the initially formed oxime resulting in 2e,3e,5a,6e-tetraarylpiperidin-4-one oximes. Oximes 185-190 complement C5 Homo sapiens 82-85 15386544-2 2004 In the case of the latter compounds, oximation is accompanied by epimerization at C-5 to avoid the A(1,3)-strain between the oxime OH group and the 5e-aryl ring of the initially formed oxime resulting in 2e,3e,5a,6e-tetraarylpiperidin-4-one oximes. Oximes 241-247 complement C5 Homo sapiens 82-85 15379785-0 2004 Specification of the structure of oximes able to reactivate tabun-inhibited acetylcholinesterase. Oximes 34-40 acetylcholinesterase (Cartwright blood group) Homo sapiens 76-96 15514903-4 2004 Current treatments of patients poisoned with organophosphorus compounds include atropine (in order to protect muscarinic receptors), oximes (in order to accelerate the reactivation of the inhibited acetylcholinesterase) and benzodiazepines (in order to avoid convulsions). Oximes 133-139 acetylcholinesterase (Cartwright blood group) Homo sapiens 198-218 15544060-2 2004 The new oxime K033 was found to be a more efficacious reactivator of sarin or cyclosarin-inhibited acetylcholinesterase than pralidoxime and obidoxime but it did not reach the efficacy of oxime HI-6 in the case of the inhibition of acetylcholinesterase by sarin or cyclosarin. Oximes 8-13 acetylcholinesterase (Cartwright blood group) Homo sapiens 99-119 15544060-2 2004 The new oxime K033 was found to be a more efficacious reactivator of sarin or cyclosarin-inhibited acetylcholinesterase than pralidoxime and obidoxime but it did not reach the efficacy of oxime HI-6 in the case of the inhibition of acetylcholinesterase by sarin or cyclosarin. Oximes 8-13 acetylcholinesterase (Cartwright blood group) Homo sapiens 232-252 15481984-7 2004 The electron density of derivative 28 bound to chicken PARP-1 revealed that the oxime makes a tight hydrogen bond with the catalytic gamma-carboxylate of glutamic acid (Glu) 988 in accordance with our original designs and models. Oximes 80-85 poly(ADP-ribose) polymerase 1 Gallus gallus 55-61 15379785-1 2004 The efficacy of various oximes to reactivate acetylcholinesterase phosphorylated by tabun (O-ethyl-N,N-dimethyl phosphoramidocyanidate) was tested by in vitro and in vivo methods. Oximes 24-30 acetylcholinesterase (Cartwright blood group) Homo sapiens 45-65 15095579-1 2004 The ability of the oxime HS-6 [1-(4-hydroxyiminomethylpyridinium)-3-(4-carbamoylpyridinium)-2-oxa-propane dichloride] to reactive in vitro the enzyme acetylcholinesterase inhibited by the nerve agent sarin [O-isopropylmethylfluorophosphonate] was evaluated. Oximes 19-24 acetylcholinesterase (Cartwright blood group) Homo sapiens 150-170 15173065-3 2004 EXPERIMENTAL DESIGN: (18)F-labeled glucose (Gluc-S-) and cellobiose (Cel-S-) derivatives of aminooxy-functionalized TOCA were synthesized via oxime formation with 4-[(18)F]fluorobenzaldehyde ([(18)F]FBOA-peptides). Oximes 142-147 glucosidase, beta, acid Mus musculus 44-48 15068300-0 2004 Synthesis of a new oxime and its application to the construction of a highly selective and sensitive Co(II) PVC-based membrane sensor. Oximes 19-24 mitochondrially encoded cytochrome c oxidase II Homo sapiens 101-106 14985944-1 2004 The reactivation of organophosphate (OP)-inhibited acetylcholinesterase (AChE) by oximes results inevitably in the formation of highly reactive phosphyloximes (POX), which may re-inhibit the enzyme. Oximes 82-88 acetylcholinesterase (Cartwright blood group) Homo sapiens 51-71 14985944-1 2004 The reactivation of organophosphate (OP)-inhibited acetylcholinesterase (AChE) by oximes results inevitably in the formation of highly reactive phosphyloximes (POX), which may re-inhibit the enzyme. Oximes 82-88 acetylcholinesterase (Cartwright blood group) Homo sapiens 73-77 15100179-1 2004 Aryl sulfotransferase (AST) IV (also named tyrosine-ester sulfotransferase and ST1A1) is a major phenol sulfotransferase in the rat, and it catalyzes the sulfation of many drugs, carcinogens, and other xenobiotics that contain phenol, benzylic alcohol, N-hydroxy arylamine, and oxime functional groups. Oximes 278-283 sulfotransferase family 1A member 1 Rattus norvegicus 0-30 15100179-1 2004 Aryl sulfotransferase (AST) IV (also named tyrosine-ester sulfotransferase and ST1A1) is a major phenol sulfotransferase in the rat, and it catalyzes the sulfation of many drugs, carcinogens, and other xenobiotics that contain phenol, benzylic alcohol, N-hydroxy arylamine, and oxime functional groups. Oximes 278-283 sulfotransferase family 1A member 1 Rattus norvegicus 43-74 15100179-1 2004 Aryl sulfotransferase (AST) IV (also named tyrosine-ester sulfotransferase and ST1A1) is a major phenol sulfotransferase in the rat, and it catalyzes the sulfation of many drugs, carcinogens, and other xenobiotics that contain phenol, benzylic alcohol, N-hydroxy arylamine, and oxime functional groups. Oximes 278-283 sulfotransferase family 1A member 1 Rattus norvegicus 79-84 15084117-5 2004 Among the pyrazoles synthesized, the oxime (23b) was identified as the most potent COX-2 selective inhibitor. Oximes 37-42 mitochondrially encoded cytochrome c oxidase II Homo sapiens 83-88 14647978-5 2004 Human AChE inhibited by MFPCh, MFP beta Ch or MFPhCh was extremely resistant towards reactivation by oximes. Oximes 101-107 acetylcholinesterase (Cartwright blood group) Homo sapiens 6-10 14647978-8 2004 In conclusion, the unexpected results, i.e., high resistance of inhibited AChE towards oxime reactivation and aging, and much lower resistance towards spontaneous reactivation, calls for further experiments at a molecular level for a better understanding of the interactions among AChE, its inhibitors and reactivators. Oximes 87-92 acetylcholinesterase (Cartwright blood group) Homo sapiens 74-78 15171567-0 2004 Oximes-induced reactivation of rat brain acetylcholinesterase inhibited by VX agent. Oximes 0-6 acetylcholinesterase Rattus norvegicus 41-61 15099445-3 2004 The structure-activity relationship (SAR) study with 12 compounds on tumour necrosis factor (TNF)-alpha inhibition, analysed by the oxime geometry and different size of spacers between the oxime and phenyl group, indicated that there might be at least three possible hydrogen bonding sites in the inhibitor binding pocket of PDE IV. Oximes 132-137 tumor necrosis factor Mus musculus 69-103 15099445-3 2004 The structure-activity relationship (SAR) study with 12 compounds on tumour necrosis factor (TNF)-alpha inhibition, analysed by the oxime geometry and different size of spacers between the oxime and phenyl group, indicated that there might be at least three possible hydrogen bonding sites in the inhibitor binding pocket of PDE IV. Oximes 189-194 tumor necrosis factor Mus musculus 69-103 15099445-6 2004 In addition, oxime compounds also significantly inhibited both nitric oxide production from activated RAW264.7 cells and T lymphocyte proliferation elicited by concanavalin A but not IL-2. Oximes 13-18 interleukin 2 Mus musculus 183-187 15023072-1 2004 Selective mutants of mouse acetylcholinesterase (AChE; EC 3.1.1.7) phosphonylated with chiral S(P)- and R(P)-cycloheptyl, -3,3-dimethylbutyl, and -isopropyl methylphosphonyl thiocholines were subjected to reactivation by the oximes HI-6 and 2-PAM and their reactivation kinetics compared with wild-type AChE and butyrylcholinesterase (EC 3.1.1.8). Oximes 225-231 acetylcholinesterase Mus musculus 27-47 15023072-1 2004 Selective mutants of mouse acetylcholinesterase (AChE; EC 3.1.1.7) phosphonylated with chiral S(P)- and R(P)-cycloheptyl, -3,3-dimethylbutyl, and -isopropyl methylphosphonyl thiocholines were subjected to reactivation by the oximes HI-6 and 2-PAM and their reactivation kinetics compared with wild-type AChE and butyrylcholinesterase (EC 3.1.1.8). Oximes 225-231 acetylcholinesterase Mus musculus 49-53 15034887-3 2004 An iterative method for the synthesis of linear N(OMe) oligosaccharide analogues was demonstrated, based on the use of an unprotected monosaccharide building block in which an oxime functionality at C-6 is converted during the synthesis into the corresponding methoxyamino group. Oximes 176-181 complement C6 Homo sapiens 199-202 15095579-3 2004 The oxime HS-6 was an effective reactivator of sarin-inhibited AChE. Oximes 4-9 acetylcholinesterase (Cartwright blood group) Homo sapiens 63-67 15033007-9 2004 The recovery of AChE activity inhibition wasn"t involved in the treatment with memantine on dichlorvos poisoning, therefore, atropine and a proper AChE reactivator (an oxime) should be used clinically. Oximes 168-173 acetylcholinesterase Rattus norvegicus 16-20 15033007-9 2004 The recovery of AChE activity inhibition wasn"t involved in the treatment with memantine on dichlorvos poisoning, therefore, atropine and a proper AChE reactivator (an oxime) should be used clinically. Oximes 168-173 acetylcholinesterase Rattus norvegicus 147-151 15568733-1 2004 The oxime K005 [1,3-bis(2-hydroxyiminomethylpyridinium) propane dibromide] for the reactivation of the enzyme acetylcholinesterase (AChE) inhibited by cyclosarin and VX was tested. Oximes 4-9 acetylcholinesterase (Cartwright blood group) Homo sapiens 110-130 15568733-1 2004 The oxime K005 [1,3-bis(2-hydroxyiminomethylpyridinium) propane dibromide] for the reactivation of the enzyme acetylcholinesterase (AChE) inhibited by cyclosarin and VX was tested. Oximes 4-9 acetylcholinesterase (Cartwright blood group) Homo sapiens 132-136 15065394-8 2004 Obidoxime, which is the most widely used reactivator of acetylcholinesterase in the therapy of poisonings by nerve agents at present, is, like in the case of soman poisonings, a relatively least suitable oxime ensuring the survival in lethal tabun poisonings. Oximes 4-9 acetylcholinesterase Mus musculus 56-76 12893843-2 2003 Extensive in vitro tests of these oximes with acetylcholinesterase inhibited by two different organophosphate agents, echothiophate and diisopropylfluorophosphate, revealed one compound with particularly good reactivation kinetics and affinity for phosphorylated acetylcholinesterase (AChE). Oximes 34-40 acetylcholinesterase Rattus norvegicus 46-66 14529460-3 2003 The main class, including pralidoxime (2-PAM), incorporates conjugated iminium and oxime moieties that are electron affinic. Oximes 32-37 peptidylglycine alpha-amidating monooxygenase Homo sapiens 41-44 15446359-4 2004 Oxime K033 seems to be the most potent reactivator of cyclosarin-inhibited AChE. Oximes 0-5 acetylcholinesterase Rattus norvegicus 75-79 15008517-3 2003 Thus, the oxime K048 seems to be a relatively efficacious broad spectrum acetylcholinesterase reactivator and, therefore, it could be useful for the treatment of a nerve agent-exposed population if information about detection of the type of nerve agent is not available. Oximes 10-15 acetylcholinesterase Rattus norvegicus 73-93 12893843-2 2003 Extensive in vitro tests of these oximes with acetylcholinesterase inhibited by two different organophosphate agents, echothiophate and diisopropylfluorophosphate, revealed one compound with particularly good reactivation kinetics and affinity for phosphorylated acetylcholinesterase (AChE). Oximes 34-40 acetylcholinesterase Rattus norvegicus 263-283 12893843-2 2003 Extensive in vitro tests of these oximes with acetylcholinesterase inhibited by two different organophosphate agents, echothiophate and diisopropylfluorophosphate, revealed one compound with particularly good reactivation kinetics and affinity for phosphorylated acetylcholinesterase (AChE). Oximes 34-40 acetylcholinesterase Rattus norvegicus 285-289 12915103-13 2003 This persistence may undermine the efficacy of pretreatment with carbamates of percutaneous intoxication in particular due to gradual replacement of carbamate on AChE by (+/-)-VX, whereas classical treatment of intoxication with oximes is hampered by the short persistence of oximes relative to the agent. Oximes 229-235 acetylcholinesterase Cavia porcellus 162-166 12970475-0 2003 CYP83A1 and CYP83B1, two nonredundant cytochrome P450 enzymes metabolizing oximes in the biosynthesis of glucosinolates in Arabidopsis. Oximes 75-81 cytochrome P450, family 83, subfamily A, polypeptide 1 Arabidopsis thaliana 0-7 12970475-0 2003 CYP83A1 and CYP83B1, two nonredundant cytochrome P450 enzymes metabolizing oximes in the biosynthesis of glucosinolates in Arabidopsis. Oximes 75-81 cytochrome P450, family 83, subfamily B, polypeptide 1 Arabidopsis thaliana 12-19 12970475-2 2003 Here, we provide biochemical evidence for the functional role of the two cytochromes P450, CYP83A1 and CYP83B1, from Arabidopsis in oxime metabolism in the biosynthesis of glucosinolates. Oximes 132-137 cytochrome P450, family 83, subfamily A, polypeptide 1 Arabidopsis thaliana 91-98 12970475-2 2003 Here, we provide biochemical evidence for the functional role of the two cytochromes P450, CYP83A1 and CYP83B1, from Arabidopsis in oxime metabolism in the biosynthesis of glucosinolates. Oximes 132-137 cytochrome P450, family 83, subfamily B, polypeptide 1 Arabidopsis thaliana 103-110 12904068-4 2003 Thus, oxidation of C-6 and introduction in the C-3 position of the potent pharmacophoric group recently introduced by us, in the 17 position of the digitalis skeleton, namely, O-(omega-aminoalkyl)oxime, led to a series of substituted androstanes able to inhibit the Na(+),K(+)-ATPase, most of them with an IC(50) in the low micromolar level, and to induce a positive inotropic effect in guinea pig. Oximes 195-201 complement C3 Cavia porcellus 47-50 12837382-4 2003 Further, they suggest that the improved performance of dimeric oximes is conferred by two-site binding with one oxime pointing toward the diisopropyl ester at the catalytic site of hAChE and the other anchored at the peripheral site. Oximes 63-69 acetylcholinesterase (Cartwright blood group) Homo sapiens 181-186 12837382-4 2003 Further, they suggest that the improved performance of dimeric oximes is conferred by two-site binding with one oxime pointing toward the diisopropyl ester at the catalytic site of hAChE and the other anchored at the peripheral site. Oximes 63-68 acetylcholinesterase (Cartwright blood group) Homo sapiens 181-186 12583695-1 2003 Early treatment of organophosphate (OP) poisoning with oximes results in reactivation of acetylcholinesterase and patient recovery. Oximes 55-61 acetylcholinesterase (Cartwright blood group) Homo sapiens 89-109 11859013-1 2002 A thorough SAR study of the oxime region of the dual NK(1)/NK(2) antagonist 1 revealed several modifications that result in potent dual antagonists. Oximes 28-33 sarcosine dehydrogenase Homo sapiens 11-14 11978898-2 2002 Standard treatment involves the administration of intravenous atropine and an oxime to counter acetylcholinesterase inhibition at the synapse, but the usefulness of oximes is uncertain. Oximes 78-83 acetylcholinesterase (Cartwright blood group) Homo sapiens 95-115 15181665-7 2003 In vitro studies with human erythrocyte AChE, which is derived from the same single gene as synaptic AChE, revealed marked differences in the potency and efficacy of pralidoxime, obidoxime, HI 6 and HLo 7, the latter two oximes being considered particularly effective in nerve agent poisoning. Oximes 221-227 acetylcholinesterase (Cartwright blood group) Homo sapiens 40-44 15181665-7 2003 In vitro studies with human erythrocyte AChE, which is derived from the same single gene as synaptic AChE, revealed marked differences in the potency and efficacy of pralidoxime, obidoxime, HI 6 and HLo 7, the latter two oximes being considered particularly effective in nerve agent poisoning. Oximes 221-227 acetylcholinesterase (Cartwright blood group) Homo sapiens 101-105 15181665-17 2003 AChE aging is particularly rapid with dimethyl phosphoryl compounds and may thwart the effective reactivation by oximes, particularly in suicidal poisoning with excessive doses. Oximes 113-119 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-4 12242610-1 2002 Standard treatment of poisoning by organophosphates (OP) includes the administration of an antimuscarinic agent, e.g. atropine, and of an acetylcholinesterase (AChE) reactivator (oxime). Oximes 179-184 acetylcholinesterase (Cartwright blood group) Homo sapiens 138-158 12242610-1 2002 Standard treatment of poisoning by organophosphates (OP) includes the administration of an antimuscarinic agent, e.g. atropine, and of an acetylcholinesterase (AChE) reactivator (oxime). Oximes 179-184 acetylcholinesterase (Cartwright blood group) Homo sapiens 160-164 12242610-5 2002 In order to provide data for a better evaluation of the reactivating potency of oximes, experiments were undertaken to determine the reactivation rate constants of several oximes with human, rabbit, rat and guinea-pig AChE inhibited by the OPs sarin, cyclosarin and VX. Oximes 80-86 acetylcholinesterase Cavia porcellus 218-222 12242610-5 2002 In order to provide data for a better evaluation of the reactivating potency of oximes, experiments were undertaken to determine the reactivation rate constants of several oximes with human, rabbit, rat and guinea-pig AChE inhibited by the OPs sarin, cyclosarin and VX. Oximes 172-178 acetylcholinesterase Cavia porcellus 218-222 12411190-1 2002 OBJECTIVE: Inhibition of acetylcholinesterase (AChE) in human brain caused by phoxim or phoxim oxon, their reactivation with oxime and aging of phosphorylated AChE were studied and compared in vitro. Oximes 125-130 acetylcholinesterase (Cartwright blood group) Homo sapiens 47-51 11859013-2 2002 Follow up SAR studies on a second-generation scaffold demonstrate that certain polar groups on the oxime can improve the dual binding affinity to the subnanomolar range. Oximes 99-104 sarcosine dehydrogenase Homo sapiens 10-13 11856550-2 2002 By reduction of the oxime of 17 beta-hydroxy-androst-4-en-3-one (testosterone), a mixture of the two amino epimers of C-3 were obtained. Oximes 20-25 complement C3 Homo sapiens 118-121 11562191-0 2001 Toward new designed proteins derived from bovine pancreatic trypsin inhibitor (BPTI): covalent cross-linking of two "core modules" by oxime-forming ligation. Oximes 134-139 trophoblast Kunitz domain protein 1 Bos taurus 60-77 11749701-1 2001 A novel oxime derivative of radicicol, KF58333, binds to the heat shock protein 90 (Hsp90) and destabilizes its associated signaling molecules. Oximes 8-13 heat shock protein 90 alpha family class A member 1 Homo sapiens 61-82 11749701-1 2001 A novel oxime derivative of radicicol, KF58333, binds to the heat shock protein 90 (Hsp90) and destabilizes its associated signaling molecules. Oximes 8-13 heat shock protein 90 alpha family class A member 1 Homo sapiens 84-89 11708930-3 2001 The OH of the oxime function appears to mimic the phenolic OH present in more "classical" ER ligands because the binding reduced when the oxime OH is methylated (2) or absent (3). Oximes 14-19 estrogen receptor 1 Homo sapiens 90-92 11708930-3 2001 The OH of the oxime function appears to mimic the phenolic OH present in more "classical" ER ligands because the binding reduced when the oxime OH is methylated (2) or absent (3). Oximes 138-143 estrogen receptor 1 Homo sapiens 90-92 11700114-0 2001 Synthesis of oxime-linked mucin mimics containing the tumor-related T(N) and sialyl T(N) antigens. Oximes 13-18 LOC100508689 Homo sapiens 26-31 11700114-1 2001 [reaction--see text] The synthesis of oxime-linked mucin mimics was accomplished via the incorporation of multiple ketone residues into a peptide followed by reaction with aminooxy sugars corresponding to the tumor-related T(N) and sialyl T(N) (ST(N)) antigens. Oximes 38-43 LOC100508689 Homo sapiens 51-56 11805735-4 2002 The standard treatment consists of reactivation of the inhibited acetylcholinesterase with an oxime antidote and reversal of the biochemical effects of acetylcholine with atropine. Oximes 94-99 acetylcholinesterase (Cartwright blood group) Homo sapiens 65-85 11868969-9 2002 In an atypical reaction for oximes, BIA 2-024 in rats was rapidly (t(max) = 2h) metabolized to the non-active 10-nitro-derivative (BIA 2-254), whereas rabbits and particularly mice oxidized the oxime moiety to a much lower extent. Oximes 28-34 tripartite motif containing 58 Homo sapiens 36-41 11868969-9 2002 In an atypical reaction for oximes, BIA 2-024 in rats was rapidly (t(max) = 2h) metabolized to the non-active 10-nitro-derivative (BIA 2-254), whereas rabbits and particularly mice oxidized the oxime moiety to a much lower extent. Oximes 28-34 tripartite motif containing 58 Homo sapiens 131-136 11868969-9 2002 In an atypical reaction for oximes, BIA 2-024 in rats was rapidly (t(max) = 2h) metabolized to the non-active 10-nitro-derivative (BIA 2-254), whereas rabbits and particularly mice oxidized the oxime moiety to a much lower extent. Oximes 28-33 tripartite motif containing 58 Homo sapiens 36-41 11868969-9 2002 In an atypical reaction for oximes, BIA 2-024 in rats was rapidly (t(max) = 2h) metabolized to the non-active 10-nitro-derivative (BIA 2-254), whereas rabbits and particularly mice oxidized the oxime moiety to a much lower extent. Oximes 28-33 tripartite motif containing 58 Homo sapiens 131-136 11798323-0 2002 Asymmetric methoxyselenenylations and cyclizations with 3-camphorseleno electrophiles containing oxime substituents at C-2. Oximes 97-102 complement C2 Homo sapiens 119-122 11800598-15 2002 The formation of oxime from DPC 423 (and its analogues) was found to be mediated by rat CYP 3A1/2, which were also responsible for converting the oxime to the GSH trappable reactive intermediate. Oximes 17-22 cytochrome P450, family 3, subfamily a, polypeptide 23-polypeptide 1 Rattus norvegicus 88-97 11800598-15 2002 The formation of oxime from DPC 423 (and its analogues) was found to be mediated by rat CYP 3A1/2, which were also responsible for converting the oxime to the GSH trappable reactive intermediate. Oximes 146-151 cytochrome P450, family 3, subfamily a, polypeptide 23-polypeptide 1 Rattus norvegicus 88-97 12475193-2 2002 Included in antidotal medical countermeasures are oximes to reactivate the inhibited cholinesterase. Oximes 50-56 butyrylcholinesterase Homo sapiens 85-99 11800023-15 2001 CONCLUSIONS: These results suggest that inhibition of hsp90 function, which causes depletion of hsp90 client proteins in tumor, contributes to the antitumor activity of KF58333, and that the stereochemistry of the oxime moiety is important for the biological activity of radicicol oxime derivatives. Oximes 214-219 heat shock protein 90 alpha family class A member 1 Homo sapiens 54-59 11562191-0 2001 Toward new designed proteins derived from bovine pancreatic trypsin inhibitor (BPTI): covalent cross-linking of two "core modules" by oxime-forming ligation. Oximes 134-139 spleen trypsin inhibitor I Bos taurus 79-83 11552681-0 2001 Interaction between peroxisome proliferator-activated receptor gamma and its agonists: docking study of oximes having 5-benzyl-2,4-thiazolidinedione. Oximes 104-110 peroxisome proliferator activated receptor gamma Homo sapiens 20-68 11393267-1 2001 The temporal profile of butyrylcholinesterase (BuChE) and in vitro pralidoxime-reactivated BuChE was studied in a cohort of 25 organophosphate-poisoned patients to examine their relationship to the development of intermediate syndrome and to understand reasons for lack of efficacy of oxime treatment. Oximes 73-78 butyrylcholinesterase Homo sapiens 91-96 11393267-5 2001 Reactivation potentials of BuChE (the difference between oxime-reactivated and -unreactivated enzyme activity) declined significantly with time after organophosphate ingestion. Oximes 57-62 butyrylcholinesterase Homo sapiens 27-32 11393267-7 2001 Patients who received oxime prior to hospitalization had a higher rate of intermediate syndrome and lower levels of BuChE at admission than those who had not. Oximes 22-27 butyrylcholinesterase Homo sapiens 116-121 11429820-3 2001 Thus, when reacted with oxime methyl ethers of alpha-ketoesters, BrF3 was able to convert the oxime group into a CF2 group and through a new type of rearrangement cause a shift of the carboxylate group to the nitrogen atom. Oximes 24-29 ATPase H+ transporting accessory protein 1 Homo sapiens 113-116 11429820-3 2001 Thus, when reacted with oxime methyl ethers of alpha-ketoesters, BrF3 was able to convert the oxime group into a CF2 group and through a new type of rearrangement cause a shift of the carboxylate group to the nitrogen atom. Oximes 94-99 ATPase H+ transporting accessory protein 1 Homo sapiens 113-116 11440563-1 2001 [reaction: see text]anti-Oximes of 2-pyridylacetic acid esters are rapidly transformed to pyridine-2-carbonitrile under a variety of conditions while syn-oximes bearing tert-butyl esters can be conveniently deprotected to the corresponding carboxylic acid with subsequent fragmentation to the nitrile. Oximes 25-31 synemin Homo sapiens 150-153 11440563-1 2001 [reaction: see text]anti-Oximes of 2-pyridylacetic acid esters are rapidly transformed to pyridine-2-carbonitrile under a variety of conditions while syn-oximes bearing tert-butyl esters can be conveniently deprotected to the corresponding carboxylic acid with subsequent fragmentation to the nitrile. Oximes 154-160 synemin Homo sapiens 150-153 11333274-0 2001 CYP83b1 is the oxime-metabolizing enzyme in the glucosinolate pathway in Arabidopsis. Oximes 15-20 cytochrome P450, family 83, subfamily B, polypeptide 1 Arabidopsis thaliana 0-7 11333274-1 2001 CYP83B1 from Arabidopsis thaliana has been identified as the oxime-metabolizing enzyme in the biosynthetic pathway of glucosinolates. Oximes 61-66 cytochrome P450, family 83, subfamily B, polypeptide 1 Arabidopsis thaliana 0-7 11333274-5 2001 By a combined use of bioinformatics, published expression data, and knock-out phenotypes, we identified the cytochrome P450 CYP83B1 as the oxime-metabolizing enzyme in the glucosinolate pathway as evidenced by characterization of the recombinant protein expressed in Escherichia coli. Oximes 139-144 cytochrome P450, family 83, subfamily B, polypeptide 1 Arabidopsis thaliana 124-131 11552681-1 2001 The molecular modelling of oximes having 5-benzyl-2,4-thiazolidinedione moieties, agonists of the peroxisome proliferator-activated receptor gamma (PPAR gamma), was performed with respect to their structures complexed with the ligand binding domain of PPAR gamma. Oximes 27-33 peroxisome proliferator activated receptor gamma Homo sapiens 98-146 11552681-1 2001 The molecular modelling of oximes having 5-benzyl-2,4-thiazolidinedione moieties, agonists of the peroxisome proliferator-activated receptor gamma (PPAR gamma), was performed with respect to their structures complexed with the ligand binding domain of PPAR gamma. Oximes 27-33 peroxisome proliferator activated receptor gamma Homo sapiens 148-158 11552681-1 2001 The molecular modelling of oximes having 5-benzyl-2,4-thiazolidinedione moieties, agonists of the peroxisome proliferator-activated receptor gamma (PPAR gamma), was performed with respect to their structures complexed with the ligand binding domain of PPAR gamma. Oximes 27-33 peroxisome proliferator activated receptor gamma Homo sapiens 252-262 11055349-1 2000 Functional probing of the backbone of the Sanofi NK2 antagonist SR 48968 has resulted in the discovery of two new classes of NK1/NK2 dual antagonists: the diamine class and the oxime class. Oximes 177-182 tachykinin receptor 2 Homo sapiens 49-52 11123966-3 2000 AST IV is a major cytosolic sulfotransferase in the rat, and it catalyzes the sulfation of various phenols, benzylic alcohols, arylhydroxamic acids, oximes, and primary N-hydroxy arylamines. Oximes 149-155 sulfotransferase family 1A member 1 Rattus norvegicus 0-6 11123973-3 2000 Electric eel acetylcholinesterase (EEAChE) was inhibited with the four stereoisomers of isomalathion, and rate constants for spontaneous and oxime-mediated reactivation (k(3)) were measured. Oximes 141-146 acetylcholinesterase (Cartwright blood group) Homo sapiens 13-33 10979978-0 2000 Novel oxime derivatives of radicicol induce erythroid differentiation associated with preferential G(1) phase accumulation against chronic myelogenous leukemia cells through destabilization of Bcr-Abl with Hsp90 complex. Oximes 6-11 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 193-200 10979978-0 2000 Novel oxime derivatives of radicicol induce erythroid differentiation associated with preferential G(1) phase accumulation against chronic myelogenous leukemia cells through destabilization of Bcr-Abl with Hsp90 complex. Oximes 6-11 heat shock protein 90 alpha family class A member 1 Homo sapiens 206-211 11204553-6 2000 In contrast a substantial proportion of the erythrocyte acetylcholinesterase is found unaged and therefore sensitive to reactivation by oximes. Oximes 136-142 acetylcholinesterase (Cartwright blood group) Homo sapiens 56-76 11204553-7 2000 Samples from an occupational exposure where depressions in plasma or erythrocyte cholinesterase activity from baseline measurements were reactivated ex vivo using the oxime 2-PAM support this hypothesis. Oximes 167-172 butyrylcholinesterase Homo sapiens 81-95 11204553-8 2000 These data also confirm that the plasma enzyme is a more sensitive than erythrocyte acetylcholinesterase as an indicator of OP exposure and thus the potential value of ex vivo oxime reactivation of erythrocyte acetylcholinesterase in a blood sample to indicate subclinical OP exposure may be limited. Oximes 176-181 acetylcholinesterase (Cartwright blood group) Homo sapiens 210-230 10956056-4 2000 Conversion of this product to its bis-oxime derivative with hydroxylamine hydrochloride resulted in two syn- and two anti-oxime isomers that had chromatographic and mass spectral properties identical with the properties of products derived from an authentic standard of 4-oxo-2-nonenal. Oximes 38-43 synemin Homo sapiens 104-107 10996027-7 2000 This conclusion was supported by the fact that BA cross-linked to oxime resin bound chemokines of the CXC (stromal cell-derived factor (SDF)-1alpha, IL-8), CC (macrophage inflammatory protein (MIP)-1beta, monocyte chemotactic protein (MCP)-2), and C (lymphotactin (Ltn)) subfamilies. Oximes 66-71 C-X-C motif chemokine ligand 8 Homo sapiens 149-153 10996027-7 2000 This conclusion was supported by the fact that BA cross-linked to oxime resin bound chemokines of the CXC (stromal cell-derived factor (SDF)-1alpha, IL-8), CC (macrophage inflammatory protein (MIP)-1beta, monocyte chemotactic protein (MCP)-2), and C (lymphotactin (Ltn)) subfamilies. Oximes 66-71 C-C motif chemokine ligand 4 like 2 Homo sapiens 160-203 10996027-7 2000 This conclusion was supported by the fact that BA cross-linked to oxime resin bound chemokines of the CXC (stromal cell-derived factor (SDF)-1alpha, IL-8), CC (macrophage inflammatory protein (MIP)-1beta, monocyte chemotactic protein (MCP)-2), and C (lymphotactin (Ltn)) subfamilies. Oximes 66-71 C-C motif chemokine ligand 8 Homo sapiens 205-241 10996027-7 2000 This conclusion was supported by the fact that BA cross-linked to oxime resin bound chemokines of the CXC (stromal cell-derived factor (SDF)-1alpha, IL-8), CC (macrophage inflammatory protein (MIP)-1beta, monocyte chemotactic protein (MCP)-2), and C (lymphotactin (Ltn)) subfamilies. Oximes 66-71 X-C motif chemokine ligand 1 Homo sapiens 251-263 10996027-7 2000 This conclusion was supported by the fact that BA cross-linked to oxime resin bound chemokines of the CXC (stromal cell-derived factor (SDF)-1alpha, IL-8), CC (macrophage inflammatory protein (MIP)-1beta, monocyte chemotactic protein (MCP)-2), and C (lymphotactin (Ltn)) subfamilies. Oximes 66-71 X-C motif chemokine ligand 1 Homo sapiens 265-268 10817663-1 2000 The reactivation of organophosphate-inhibited acetylcholinesterase (AChE) by oximes inevitably results in the formation of highly reactive phosphoryloximes (POX), which are able to re-inhibit the enzyme. Oximes 77-83 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-72 11055349-1 2000 Functional probing of the backbone of the Sanofi NK2 antagonist SR 48968 has resulted in the discovery of two new classes of NK1/NK2 dual antagonists: the diamine class and the oxime class. Oximes 177-182 tachykinin receptor 1 Homo sapiens 125-128 11055349-1 2000 Functional probing of the backbone of the Sanofi NK2 antagonist SR 48968 has resulted in the discovery of two new classes of NK1/NK2 dual antagonists: the diamine class and the oxime class. Oximes 177-182 tachykinin receptor 2 Homo sapiens 129-132 11055349-2 2000 The addition of the amino or the oxime functional group results in the reversal of the stereochemical preference of the NK2 receptor. Oximes 33-38 tachykinin receptor 2 Homo sapiens 120-132 10856827-5 2000 Angiotensin II (0.091-0.91 pmol) injected into the AHA produced a pressor response in both WKY and SHR, and the pressor response to angiotensin II was greater in SHR than that of WKY. Oximes 51-54 angiotensinogen Rattus norvegicus 0-14 10801325-0 2000 Mechanism of oxime reactivation of acetylcholinesterase analyzed by chirality and mutagenesis. Oximes 13-18 acetylcholinesterase (Cartwright blood group) Homo sapiens 35-55 10801325-2 2000 We have examined the reactivation of a series of resolved enantiomeric methylphosphonate conjugates of acetylcholinesterase by two oximes, 2-pralidoxime (2-PAM) and 1-(2"-hydroxyiminomethyl-1"-pyridinium)-3-(4"-carbamoyl-1-pyridinium) (HI-6). Oximes 131-137 acetylcholinesterase (Cartwright blood group) Homo sapiens 103-123 10817663-11 2000 These reactions must be regarded as therapeutically detrimental and disqualify those oximes which are capable of forming stable POX by reactivation of BChE. Oximes 85-91 butyrylcholinesterase Homo sapiens 151-155 10817664-3 2000 Human plasma with the butyrylcholinesterase irreversibly blocked by soman was able to stimulate obidoxime-induced reactivation of concentrated erythrocyte acetylcholinesterase (Ery-AChE) to the same extent as was observed with a dilute preparation, suggesting phosphoryl oxime-destroying capacity. Oximes 100-105 acetylcholinesterase (Cartwright blood group) Homo sapiens 181-185 10714503-1 2000 Oximes having 5-benzyl-2,4-thiazolidinedione were prepared, and their PPAR gamma agonistic activities and blood glucose lowering activities were evaluated. Oximes 0-6 peroxisome proliferator activated receptor gamma Homo sapiens 70-80 10566233-3 1999 Our findings confirm that the new oxime BI-6 is a more effective reactivator of soman-inhibited acetylcholinesterase than obidoxime but not as effective as the oxime HI-6 especially in the peripheral compartment. Oximes 34-39 acetylcholinesterase Rattus norvegicus 96-116 10681099-0 2000 Comparison of oxime-initiated reactivation of organophosphorous-inhibited acetylcholinesterase in brains of avian embryos. Oximes 14-19 acetylcholinesterase (Cartwright blood group) Gallus gallus 74-94 10681099-1 2000 Organophosphorous (OP) insecticide-induced inhibition and oxime reactivation of acetylcholinesterase (AChE) was determined in whole-brain homogenates prepared from 15-d-old chick embryos. Oximes 58-63 acetylcholinesterase (Cartwright blood group) Gallus gallus 80-100 10681099-1 2000 Organophosphorous (OP) insecticide-induced inhibition and oxime reactivation of acetylcholinesterase (AChE) was determined in whole-brain homogenates prepared from 15-d-old chick embryos. Oximes 58-63 acetylcholinesterase (Cartwright blood group) Gallus gallus 102-106 10681099-3 2000 Following insecticide exposure, an in vitro system compared the capability of the oximes pralidoxime (2-PAM), obidoxime, TMB-4, and HI-6 to reactivate the OP-inhibited AChE. Oximes 82-88 peptidylglycine alpha-amidating monooxygenase Gallus gallus 104-107 10681099-3 2000 Following insecticide exposure, an in vitro system compared the capability of the oximes pralidoxime (2-PAM), obidoxime, TMB-4, and HI-6 to reactivate the OP-inhibited AChE. Oximes 82-88 acetylcholinesterase (Cartwright blood group) Gallus gallus 168-172 10681099-7 2000 These results suggest that both the OP insecticide inhibiting AChE and the oxime reactivating this enzyme can contribute to the effectiveness of the avian brain AChE reactivation. Oximes 75-80 acetylcholinesterase (Cartwright blood group) Gallus gallus 161-165 10717647-9 2000 Protonated oximes of 20-oxosteroids unsubstituted at C-21, C-17 or C-16 produced a characteristic ion at m/z 86 containing the side chain, C-16 and C-17. Oximes 11-17 TBL1X/Y related 1 Homo sapiens 53-57 10717647-9 2000 Protonated oximes of 20-oxosteroids unsubstituted at C-21, C-17 or C-16 produced a characteristic ion at m/z 86 containing the side chain, C-16 and C-17. Oximes 11-17 cytokine like 1 Homo sapiens 59-63 10717647-9 2000 Protonated oximes of 20-oxosteroids unsubstituted at C-21, C-17 or C-16 produced a characteristic ion at m/z 86 containing the side chain, C-16 and C-17. Oximes 11-17 cytokine like 1 Homo sapiens 148-152 10639282-3 1999 Whereas (RS)-4-amino-3-hydroxy-4,5,6,7-tetrahydro-1,2-benzisoxazole (8, exo-THPO) was synthesized via aluminum amalgam reduction of oxime 22a or 22b, compounds 9, 11-13, and 15-17 were obtained via reductive aminations. Oximes 132-137 5'-3' exoribonuclease 1 Mus musculus 72-75 10639282-3 1999 Whereas (RS)-4-amino-3-hydroxy-4,5,6,7-tetrahydro-1,2-benzisoxazole (8, exo-THPO) was synthesized via aluminum amalgam reduction of oxime 22a or 22b, compounds 9, 11-13, and 15-17 were obtained via reductive aminations. Oximes 132-137 thrombopoietin Mus musculus 76-80 10639284-3 1999 This effect was noted in compounds that contained a functionalized oxime moiety or an exomethylene at C-4, and the potencies were typically <10 nM for MMP-3 and <100 nM for MMP-1. Oximes 67-72 matrix metallopeptidase 3 Homo sapiens 154-159 10639284-3 1999 This effect was noted in compounds that contained a functionalized oxime moiety or an exomethylene at C-4, and the potencies were typically <10 nM for MMP-3 and <100 nM for MMP-1. Oximes 67-72 matrix metallopeptidase 1 Homo sapiens 179-184 10071778-2 1999 The peptidic oligomers were made by linking several copies of the alpha-MSH fragment analog Nle-Asp-His-[D-Phe]-Arg-Trp-Lys-NH2 to different templates through formation of oxime bonds. Oximes 172-177 proopiomelanocortin Homo sapiens 66-75 10433700-0 1999 Phosphoryl oxime inhibition of acetylcholinesterase during oxime reactivation is prevented by edrophonium. Oximes 11-16 acetylcholinesterase (Cartwright blood group) Homo sapiens 31-51 10433700-0 1999 Phosphoryl oxime inhibition of acetylcholinesterase during oxime reactivation is prevented by edrophonium. Oximes 59-64 acetylcholinesterase (Cartwright blood group) Homo sapiens 31-51 10433700-2 1999 This study with native, wild-type, and mutant recombinant DNA-expressed AChEs, each inhibited by representative OP compounds, establishes a relationship between edrophonium acceleration of oxime-induced reactivation of OP-AChE conjugates and phosphoryl oxime inhibition of the reactivated enzyme that occurs during reactivation by pyridinium oximes LuH6 and TMB4. Oximes 189-194 acetylcholinesterase (Cartwright blood group) Homo sapiens 72-76 10433700-2 1999 This study with native, wild-type, and mutant recombinant DNA-expressed AChEs, each inhibited by representative OP compounds, establishes a relationship between edrophonium acceleration of oxime-induced reactivation of OP-AChE conjugates and phosphoryl oxime inhibition of the reactivated enzyme that occurs during reactivation by pyridinium oximes LuH6 and TMB4. Oximes 253-258 acetylcholinesterase (Cartwright blood group) Homo sapiens 72-76 10433700-5 1999 However, phosphoryl oximes formed during the reactivation of the diethylphosphoryl-AChE conjugate were not sufficiently stable to be detected by (31)P NMR. Oximes 20-26 acetylcholinesterase (Cartwright blood group) Homo sapiens 83-87 10433700-7 1999 Reactivation of both ethoxy methylphosphonyl- and diethylphosphoryl-AChE by these two oximes was accelerated in the presence of rabbit serum paraoxonase, suggesting that organophosphorus hydrolase can hydrolyze phosphoryl oxime formed during the reactivation. Oximes 86-92 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-72 10433700-7 1999 Reactivation of both ethoxy methylphosphonyl- and diethylphosphoryl-AChE by these two oximes was accelerated in the presence of rabbit serum paraoxonase, suggesting that organophosphorus hydrolase can hydrolyze phosphoryl oxime formed during the reactivation. Oximes 86-91 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-72 10433700-8 1999 Our results emphasize that certain oximes, such as LuH6 and TMB4, if used in the treatment of OP pesticide poisoning may cause prolonged inhibition of AChE due to formation of phosphoryl oximes. Oximes 35-41 acetylcholinesterase (Cartwright blood group) Homo sapiens 151-155 10433700-8 1999 Our results emphasize that certain oximes, such as LuH6 and TMB4, if used in the treatment of OP pesticide poisoning may cause prolonged inhibition of AChE due to formation of phosphoryl oximes. Oximes 187-193 acetylcholinesterase (Cartwright blood group) Homo sapiens 151-155 10704134-1 1999 Newly synthesized oximes, mono and bis imidazole derivatives, which promise to be more effective acetylcholinesterase reactivators than standard antidotes used, were investigated by spectrophotometric and electrochemical methods. Oximes 18-24 acetylcholinesterase (Cartwright blood group) Homo sapiens 97-117 10704134-3 1999 Dissociation constants of those oximes were also obtained by numerical treatment of overlapping equilibria, using the Lavendberg Marquardt least square method, and when compared with the same for some similar compounds, were found to be very effective acetylcholinesterase reactivators. Oximes 32-38 acetylcholinesterase (Cartwright blood group) Homo sapiens 252-272 10704134-5 1999 The results indicated that many oxime anions will be available at physiological pH 7.4 and a relative increased ability to reactivate inhibited acetylcholinesterase could be expected. Oximes 32-37 acetylcholinesterase (Cartwright blood group) Homo sapiens 144-164 10052942-6 1999 Serine and hydroxylamine form an alpha-aminoacrylate and an oxime with PLP in CBS, respectively. Oximes 60-65 pyridoxal phosphatase Homo sapiens 71-74 10052942-6 1999 Serine and hydroxylamine form an alpha-aminoacrylate and an oxime with PLP in CBS, respectively. Oximes 60-65 cystathionine beta-synthase Homo sapiens 78-81 10052942-10 1999 The dissociation of PLP is a multistage process involving a short approximately 500 s lag phase, followed by a rapid inactivation and a slower PLP-oxime formation. Oximes 147-152 pyridoxal phosphatase Homo sapiens 20-23 10052942-10 1999 The dissociation of PLP is a multistage process involving a short approximately 500 s lag phase, followed by a rapid inactivation and a slower PLP-oxime formation. Oximes 147-152 pyridoxal phosphatase Homo sapiens 143-146 10421446-0 1999 Role of edrophonium in prevention of the re-inhibition of acetylcholinesterase by phosphorylated oxime. Oximes 97-102 acetylcholinesterase Mus musculus 58-78 10421479-3 1999 For example, the in vitro stoichiometric neutralization of sarin by AChE was increased from 1:1 to 3200:1 by the addition of the oxime HI-6, while the in vivo stoichiometry was increased to 57:1 in mice by HI-6. Oximes 129-134 acetylcholinesterase Mus musculus 68-72 10421479-4 1999 The aging rate of soman-inhibited mouse AChE was reduced 12-fold in a mutant AChE (E202Q) which resulted in a two-fold increase in oxime-assisted detoxification of soman. Oximes 131-136 acetylcholinesterase Mus musculus 40-44 10421479-4 1999 The aging rate of soman-inhibited mouse AChE was reduced 12-fold in a mutant AChE (E202Q) which resulted in a two-fold increase in oxime-assisted detoxification of soman. Oximes 131-136 acetylcholinesterase Mus musculus 77-81 10421484-1 1999 We previously demonstrated that a combination of cholinesterase (ChE) pre-treatment with an oxime is an effective measure against soman and sarin. Oximes 92-97 butyrylcholinesterase Homo sapiens 49-63 10421484-1 1999 We previously demonstrated that a combination of cholinesterase (ChE) pre-treatment with an oxime is an effective measure against soman and sarin. Oximes 92-97 butyrylcholinesterase Homo sapiens 65-68 10421484-5 1999 The ChE-sponges retained their catalytic activity under conditions of temperature, time, and drying where the native soluble enzyme would rapidly denature, and can be reused in conjunction with oximes many times. Oximes 194-200 butyrylcholinesterase Homo sapiens 4-7 10421484-6 1999 The ChE-sponge in the presence of oxime repeatedly detoxified OPs such as DFP or MEPQ. Oximes 34-39 butyrylcholinesterase Homo sapiens 4-7 10207609-2 1999 Since the oxime effectiveness is influenced not only by its reactivating potential but also by inhibition, aging and spontaneous reactivation kinetics, experiments were performed with human acetyl- (AChE) and butyrylcholinesterase (BChE) to determine the respective kinetic constants. Oximes 10-15 acetylcholinesterase (Cartwright blood group) Homo sapiens 199-203 10207609-2 1999 Since the oxime effectiveness is influenced not only by its reactivating potential but also by inhibition, aging and spontaneous reactivation kinetics, experiments were performed with human acetyl- (AChE) and butyrylcholinesterase (BChE) to determine the respective kinetic constants. Oximes 10-15 butyrylcholinesterase Homo sapiens 209-230 10207609-2 1999 Since the oxime effectiveness is influenced not only by its reactivating potential but also by inhibition, aging and spontaneous reactivation kinetics, experiments were performed with human acetyl- (AChE) and butyrylcholinesterase (BChE) to determine the respective kinetic constants. Oximes 10-15 butyrylcholinesterase Homo sapiens 232-236 10207609-7 1999 These data indicate that oximes may effectively reactivate human dimethylphosphoryl-AChE. Oximes 25-31 acetylcholinesterase (Cartwright blood group) Homo sapiens 84-88 10207609-9 1999 The potency of the oximes to reactivate dimethylphosphoryl-BChE was much lower and the spontaneous reactivation slower (t1/2 9 h), while aging proceeded at a comparable rate. Oximes 19-25 butyrylcholinesterase Homo sapiens 59-63 9171871-0 1997 Anticancer and antiviral effects and inactivation of S-adenosyl-L-homocysteine hydrolase with 5"-carboxaldehydes and oximes synthesized from adenosine and sugar-modified analogues. Oximes 117-123 adenosylhomocysteinase Homo sapiens 53-88 9772214-2 1998 The protective effect of the oxime 2-PAM against inhibition of acetylcholinesterase (AChE) by paraoxon was estimated in vitro and in vivo and was correlated with the mortality of paraoxon-treated bees. Oximes 29-34 acetylcholinesterase Apis mellifera 63-83 9772214-2 1998 The protective effect of the oxime 2-PAM against inhibition of acetylcholinesterase (AChE) by paraoxon was estimated in vitro and in vivo and was correlated with the mortality of paraoxon-treated bees. Oximes 29-34 acetylcholinesterase Apis mellifera 85-89 9448738-0 1998 Combined effect of organophosphorus hydrolase and oxime on the reactivation rate of diethylphosphoryl-acetylcholinesterase conjugates. Oximes 50-55 acetylcholinesterase (Cartwright blood group) Homo sapiens 102-122 9507700-1 1998 The synthesis and biological evaluation of oximes of 2-aryl-6-methoxy-3,4-dihydronaphthalene (7a, 7b, 14a, 14b) as nonsteroidal inhibitors of 17 alpha-hydroxylase-C17,20-lyase (P450 17, CYP 17) is described. Oximes 43-49 cytochrome P450 family 17 subfamily A member 1 Homo sapiens 186-192 9359435-6 1997 Wild-type BuChE and mutants were inhibited by di-isopropylfluorophosphate at pH 8.0 and 25 degrees C. Di-isopropyl-phosphorylated enzymes were incubated with the nucleophilic oxime 2-pyridine aldoxime methiodide and their reactivatability was determined. Oximes 175-180 butyrylcholinesterase Homo sapiens 10-15 9806430-8 1998 By contrast, HLo 7 was shown to be an extremely potent reactivator of human AChE and BChE, which supports its position as a broad-spectrum oxime. Oximes 139-144 butyrylcholinesterase Homo sapiens 85-89 9547363-1 1998 Reactivation of organophosphate (OP)-inhibited acetylcholinesterase (AChE) by oximes is the primary reason for their effectiveness in the treatment of OP poisoning. Oximes 78-84 acetylcholinesterase (Cartwright blood group) Homo sapiens 69-73 9547363-4 1998 To better understand the acceleration phenomenon, we examined ligand modulations of oxime-induced reactivation of methylphosphonylated AChE using 7-(methylethoxyphosphinyloxy)-1-methylquinolinium iodide and fetal bovine serum AChE. Oximes 84-89 acetylcholinesterase (Cartwright blood group) Homo sapiens 135-139 9547363-4 1998 To better understand the acceleration phenomenon, we examined ligand modulations of oxime-induced reactivation of methylphosphonylated AChE using 7-(methylethoxyphosphinyloxy)-1-methylquinolinium iodide and fetal bovine serum AChE. Oximes 84-89 acetylcholinesterase (Cartwright blood group) Homo sapiens 226-230 9547363-9 1998 Propidium slowed the reactivation of 7-(methylethoxyphosphinyloxy)-1- methylquinolinium iodide-inhibited AChE by all oximes. Oximes 117-123 acetylcholinesterase (Cartwright blood group) Homo sapiens 105-109 9635412-5 1998 Among compounds containing oxime functional groups only OPAB, having longer methylene chain and being more lipophylic than other oximes usually used in acetylcholinesterase (AChE) reactivation studies, was effective in decreasing the rate of aging on DFP-inhibited NTE. Oximes 27-32 acetylcholinesterase (Cartwright blood group) Homo sapiens 174-178 9635412-5 1998 Among compounds containing oxime functional groups only OPAB, having longer methylene chain and being more lipophylic than other oximes usually used in acetylcholinesterase (AChE) reactivation studies, was effective in decreasing the rate of aging on DFP-inhibited NTE. Oximes 129-135 acetylcholinesterase (Cartwright blood group) Homo sapiens 152-172 9635412-5 1998 Among compounds containing oxime functional groups only OPAB, having longer methylene chain and being more lipophylic than other oximes usually used in acetylcholinesterase (AChE) reactivation studies, was effective in decreasing the rate of aging on DFP-inhibited NTE. Oximes 129-135 acetylcholinesterase (Cartwright blood group) Homo sapiens 174-178 9587020-4 1998 Since oximes are believed to act primarily through reactivation of inhibited acetylcholinesterase (AChE) and erythrocyte AChE is regarded to be a good marker for the synaptic enzyme, the reactivating potency can be investigated with human erythrocyte AChE in vitro. Oximes 6-12 acetylcholinesterase (Cartwright blood group) Homo sapiens 77-97 9587020-4 1998 Since oximes are believed to act primarily through reactivation of inhibited acetylcholinesterase (AChE) and erythrocyte AChE is regarded to be a good marker for the synaptic enzyme, the reactivating potency can be investigated with human erythrocyte AChE in vitro. Oximes 6-12 acetylcholinesterase (Cartwright blood group) Homo sapiens 99-103 9587020-5 1998 The present study was undertaken to evaluate the ability of various oximes at concentrations therapeutically relevant in humans to reactivate human erythrocyte AChE inhibited by different nerve agents. Oximes 68-74 acetylcholinesterase (Cartwright blood group) Homo sapiens 160-164 9587020-8 1998 The reactivation of human AChE by oximes was dependent on the organophosphate used. Oximes 34-40 acetylcholinesterase (Cartwright blood group) Homo sapiens 26-30 9543466-5 1998 Acetylcholinesterase inhibition produced by metrifonate occurs rapidly, is dose dependent, can be detected by inhibition measured in red blood cells, and can be reversed by oxime administration. Oximes 173-178 acetylcholinesterase Rattus norvegicus 0-20 9600150-3 1998 The subsequent antidotal therapy resulted in variously high reactivation of cyclosin-inhibited acetylcholinesterase in dependence on the selection of oxime. Oximes 150-155 acetylcholinesterase Rattus norvegicus 95-115 9292287-6 1997 Obidoxime turned out to be the most potent and most efficacious oxime in reactivating AChE inhibited by various classes of OP insecticides and tabun. Oximes 4-9 acetylcholinesterase (Cartwright blood group) Homo sapiens 86-90 9292287-10 1997 However, in suicidal mega-dose poisoning, oximes, even at optimal plasma concentrations, may be unable to cope with the fast re-inhibition of reactivated AChE in the first days following intoxication. Oximes 42-48 acetylcholinesterase (Cartwright blood group) Homo sapiens 154-158 9292288-3 1997 By virtue of in vitro findings and theoretical considerations we concluded in the preceding paper that oximes should preferably be administered by continuous infusion following an initial bolus dose for as long as reactivation of inhibited acetylcholinesterase (AChE) can be expected. Oximes 103-109 acetylcholinesterase (Cartwright blood group) Homo sapiens 240-260 9292288-3 1997 By virtue of in vitro findings and theoretical considerations we concluded in the preceding paper that oximes should preferably be administered by continuous infusion following an initial bolus dose for as long as reactivation of inhibited acetylcholinesterase (AChE) can be expected. Oximes 103-109 acetylcholinesterase (Cartwright blood group) Homo sapiens 262-266 9271331-3 1997 Aging has proven to be a major barrier to achieving oxime reactivation of acetylcholinesterase (AChE) inhibited by the more potent OPs. Oximes 52-57 acetylcholinesterase Mus musculus 74-94 9271331-3 1997 Aging has proven to be a major barrier to achieving oxime reactivation of acetylcholinesterase (AChE) inhibited by the more potent OPs. Oximes 52-57 acetylcholinesterase Mus musculus 96-100 9209694-1 1997 The efficiency of newly synthesized oxime derivatives of quinuclidinium were tested in vitro on soman inhibited acetylcholinesterase (AChE) of human erythrocytes and in vivo using soman poisoned mice. Oximes 36-41 acetylcholinesterase (Cartwright blood group) Homo sapiens 112-132 9209694-1 1997 The efficiency of newly synthesized oxime derivatives of quinuclidinium were tested in vitro on soman inhibited acetylcholinesterase (AChE) of human erythrocytes and in vivo using soman poisoned mice. Oximes 36-41 acetylcholinesterase (Cartwright blood group) Homo sapiens 134-138 8619258-0 1996 Oxime-induced reactivation of acetylcholinesterase inhibited by phosphoramidates. Oximes 0-5 acetylcholinesterase (Cartwright blood group) Homo sapiens 30-50 8691435-3 1996 Among these naphthoic acids, oxime derivative 12 was identified as a potent RAR gamma-selective retinoid, while olefinic derivative 11 was found to be comparable to retinoic acid and slightly RAR beta,gamma selective. Oximes 29-34 retinoic acid receptor gamma Homo sapiens 76-85 8902275-4 1996 Studies on the biochemical mechanism of oxime formation suggested that cis-oxime formation in the presence of adult human liver microsomes was largely dependent on the human flavin-containing monooxygenase (form 3). Oximes 40-45 flavin containing dimethylaniline monoxygenase 3 Homo sapiens 174-213 8794905-0 1996 Interactions of oxime reactivators with diethylphosphoryl adducts of human acetylcholinesterase and its mutant derivatives. Oximes 16-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 75-95 8911635-2 1996 Although oximes have been designed to reactivate the inhibited acetylcholinesterase (AChE), clinical experience has indicated that they are not always very effective as reactivators and at this very moment none of them can be regarded as a broad-spectrum antidote. Oximes 9-15 acetylcholinesterase (Cartwright blood group) Homo sapiens 63-83 8783813-0 1996 Reactivation by various oximes of human erythrocyte acetylcholinesterase inhibited by different organophosphorus compounds. Oximes 24-30 acetylcholinesterase (Cartwright blood group) Homo sapiens 52-72 8783813-5 1996 The oximes significantly, but not completely, reactivated organophosphate inhibited AChE. Oximes 4-10 acetylcholinesterase (Cartwright blood group) Homo sapiens 84-88 8911635-2 1996 Although oximes have been designed to reactivate the inhibited acetylcholinesterase (AChE), clinical experience has indicated that they are not always very effective as reactivators and at this very moment none of them can be regarded as a broad-spectrum antidote. Oximes 9-15 acetylcholinesterase (Cartwright blood group) Homo sapiens 85-89 8603667-1 1996 The oxime HI-6 dichloride [1-(2 hydroxyiminomethyl -1-pyridino)-3-(4-carbamoyl-1-pyridino)-2-oxapropane dichloride monohydrate] has shown to be a potent reactivator of cholinesterase activity and may have efficacy for the treatment of organophosphate intoxication [SIPRI, 1976; Schenk et al. Oximes 4-9 butyrylcholinesterase Rattus norvegicus 168-182 8582034-7 1996 Of the two isoforms of cyclooxygenase (COX-1 and COX-2), COX-1 activity was inhibited by oxime-2 and 4"-piperidinoacetophenone oxime (oxime-3) with IC50 values of 50 and 130 microM, respectively, while COX-2 activity was not inhibited. Oximes 89-94 mitochondrially encoded cytochrome c oxidase I Homo sapiens 39-44 8582034-7 1996 Of the two isoforms of cyclooxygenase (COX-1 and COX-2), COX-1 activity was inhibited by oxime-2 and 4"-piperidinoacetophenone oxime (oxime-3) with IC50 values of 50 and 130 microM, respectively, while COX-2 activity was not inhibited. Oximes 89-94 mitochondrially encoded cytochrome c oxidase II Homo sapiens 49-54 8582034-7 1996 Of the two isoforms of cyclooxygenase (COX-1 and COX-2), COX-1 activity was inhibited by oxime-2 and 4"-piperidinoacetophenone oxime (oxime-3) with IC50 values of 50 and 130 microM, respectively, while COX-2 activity was not inhibited. Oximes 89-94 mitochondrially encoded cytochrome c oxidase I Homo sapiens 57-62 8582034-7 1996 Of the two isoforms of cyclooxygenase (COX-1 and COX-2), COX-1 activity was inhibited by oxime-2 and 4"-piperidinoacetophenone oxime (oxime-3) with IC50 values of 50 and 130 microM, respectively, while COX-2 activity was not inhibited. Oximes 89-94 mitochondrially encoded cytochrome c oxidase II Homo sapiens 202-207 8582034-7 1996 Of the two isoforms of cyclooxygenase (COX-1 and COX-2), COX-1 activity was inhibited by oxime-2 and 4"-piperidinoacetophenone oxime (oxime-3) with IC50 values of 50 and 130 microM, respectively, while COX-2 activity was not inhibited. Oximes 127-132 mitochondrially encoded cytochrome c oxidase I Homo sapiens 39-44 8582034-7 1996 Of the two isoforms of cyclooxygenase (COX-1 and COX-2), COX-1 activity was inhibited by oxime-2 and 4"-piperidinoacetophenone oxime (oxime-3) with IC50 values of 50 and 130 microM, respectively, while COX-2 activity was not inhibited. Oximes 127-132 mitochondrially encoded cytochrome c oxidase II Homo sapiens 49-54 8582034-7 1996 Of the two isoforms of cyclooxygenase (COX-1 and COX-2), COX-1 activity was inhibited by oxime-2 and 4"-piperidinoacetophenone oxime (oxime-3) with IC50 values of 50 and 130 microM, respectively, while COX-2 activity was not inhibited. Oximes 127-132 mitochondrially encoded cytochrome c oxidase I Homo sapiens 57-62 8582034-7 1996 Of the two isoforms of cyclooxygenase (COX-1 and COX-2), COX-1 activity was inhibited by oxime-2 and 4"-piperidinoacetophenone oxime (oxime-3) with IC50 values of 50 and 130 microM, respectively, while COX-2 activity was not inhibited. Oximes 127-132 mitochondrially encoded cytochrome c oxidase II Homo sapiens 202-207 8582034-8 1996 The in vitro inhibitory effect of oxime-2 and oxime-3 on COX-1 activity decreased with O-acylation of the oximes. Oximes 34-39 mitochondrially encoded cytochrome c oxidase I Homo sapiens 57-62 8582034-8 1996 The in vitro inhibitory effect of oxime-2 and oxime-3 on COX-1 activity decreased with O-acylation of the oximes. Oximes 46-51 mitochondrially encoded cytochrome c oxidase I Homo sapiens 57-62 8582034-8 1996 The in vitro inhibitory effect of oxime-2 and oxime-3 on COX-1 activity decreased with O-acylation of the oximes. Oximes 106-112 mitochondrially encoded cytochrome c oxidase I Homo sapiens 57-62