PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 32583098-3 2020 The reactivation was notable for both AChE and BChE inhibited by VX, cyclosarin, sarin and paraoxon, if quinuclidinium compounds contained the benzyl group attached to the quinuclidinium moiety. cyclohexyl methylphosphonofluoridate 69-79 acetylcholinesterase (Cartwright blood group) Homo sapiens 38-42 32583098-3 2020 The reactivation was notable for both AChE and BChE inhibited by VX, cyclosarin, sarin and paraoxon, if quinuclidinium compounds contained the benzyl group attached to the quinuclidinium moiety. cyclohexyl methylphosphonofluoridate 69-79 butyrylcholinesterase Homo sapiens 47-51 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. cyclohexyl methylphosphonofluoridate 100-110 butyrylcholinesterase Homo sapiens 44-48 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. cyclohexyl methylphosphonofluoridate 158-168 butyrylcholinesterase Homo sapiens 44-48 32305437-3 2020 CatA could be stably inhibited by low microM to high nM concentrations of racemic sarin (GB), soman (GD), cyclosarin (GF), VX, and VR within minutes to hours at pH 7. cyclohexyl methylphosphonofluoridate 106-116 cathepsin A Homo sapiens 0-4 32454005-5 2020 All compounds were assessed for their ability to reactivate human acetylcholinesterase inhibited by the nerve agents VX, tabun, sarin, cyclosarin and paraoxon in vitro. cyclohexyl methylphosphonofluoridate 135-145 acetylcholinesterase (Cartwright blood group) Homo sapiens 66-86 32305437-5 2020 Bimolecular rate constants for inhibition by cyclosarin and VR were 1.3 x 103 M-1sec-1 and 1.2 x 103 M-1sec-1, respectively, and were approximately 3-orders of magnitude lower than those of human AChE indicating slower reactivity. cyclohexyl methylphosphonofluoridate 45-55 secretory blood group 1, pseudogene Homo sapiens 81-86 32305437-5 2020 Bimolecular rate constants for inhibition by cyclosarin and VR were 1.3 x 103 M-1sec-1 and 1.2 x 103 M-1sec-1, respectively, and were approximately 3-orders of magnitude lower than those of human AChE indicating slower reactivity. cyclohexyl methylphosphonofluoridate 45-55 acetylcholinesterase (Cartwright blood group) Homo sapiens 196-200 30383374-5 2018 Its overall reactivation of sarin-, VX-, and cyclosarin-inhibited AChE was, respectively, 3-, 7-, and 8-fold higher than by K027. cyclohexyl methylphosphonofluoridate 45-55 acetylcholinesterase (Cartwright blood group) Homo sapiens 66-70 30312685-4 2018 This in vitro study was undertaken to determine reactivity, affinity and overall reactivation constants of 3 l, the reference compound ADOC and two structural analogues with human AChE inhibited by paraoxon, sarin, cyclosarin and VX. cyclohexyl methylphosphonofluoridate 215-225 acetylcholinesterase (Cartwright blood group) Homo sapiens 180-184 31863869-8 2020 Rather, potential reactivators of phosphylated BChE, with its enlarged acyl pocket, were identified, especially in case of cyclosarin, where the reactivation rates of the lead reactivator was 100- and 6-times that of 2-PAM and HI-6, respectively. cyclohexyl methylphosphonofluoridate 123-133 butyrylcholinesterase Homo sapiens 47-51 31969483-3 2020 In the present study, we have demonstrated an adeno-associated virus 8 (AAV8)-mediated paraoxonase 1 variant IF-11 (PON1-IF11) gene therapy that offers asymptomatic prophylactic protection to mice against multiple lethal doses of G-type chemical warfare nerve agents, namely, tabun, sarin, cyclosarin, and soman, for up to 5 months in mice. cyclohexyl methylphosphonofluoridate 290-300 paraoxonase 1 Mus musculus 87-100 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. cyclohexyl methylphosphonofluoridate 49-59 acetylcholinesterase (Cartwright blood group) Homo sapiens 70-74 27125569-0 2017 Mechanistic studies of new oximes reactivators of human butyryl cholinesterase inhibited by cyclosarin and sarin. cyclohexyl methylphosphonofluoridate 92-102 butyrylcholinesterase Homo sapiens 56-78 30096649-7 2018 In this paper several structural derivatives of ADOC were synthesized and screened for their ability to reactivate human AChE (hAChE) inhibited by the nerve agents VX, sarin, tabun, cyclosarin and paraoxon. cyclohexyl methylphosphonofluoridate 182-192 acetylcholinesterase (Cartwright blood group) Homo sapiens 121-125 30096649-7 2018 In this paper several structural derivatives of ADOC were synthesized and screened for their ability to reactivate human AChE (hAChE) inhibited by the nerve agents VX, sarin, tabun, cyclosarin and paraoxon. cyclohexyl methylphosphonofluoridate 182-192 acetylcholinesterase (Cartwright blood group) Homo sapiens 127-132 27238725-9 2016 Compounds were screened for reactivation of cyclosarin-, sarin- and VX-inhibited AChE and BChE. cyclohexyl methylphosphonofluoridate 44-54 acetylcholinesterase (Cartwright blood group) Homo sapiens 81-85 27129421-6 2016 Three newly synthesized oxime-hydroxamate hybrids: 2PAMPr4PHA, 2PAMMeBHA and 2,4-DiPAMMeBHA were found to detoxify sarin, cyclosarin and soman in solution at 3-10-fold faster rate than 2PAM and to reactivate OP-AChE in vitro. cyclohexyl methylphosphonofluoridate 122-132 acetylcholinesterase Rattus norvegicus 211-215 27238725-9 2016 Compounds were screened for reactivation of cyclosarin-, sarin- and VX-inhibited AChE and BChE. cyclohexyl methylphosphonofluoridate 44-54 butyrylcholinesterase Homo sapiens 90-94 24912784-4 2015 The present study was initiated to determine the reactivation kinetics of 31 structurally different bispyridinium oximes with paraoxon-, tabun- and cyclosarin-inhibited human BChE. cyclohexyl methylphosphonofluoridate 148-158 butyrylcholinesterase Homo sapiens 175-179 26965078-2 2016 The inhibition kinetic parameters were determined for AChE by surrogates of cyclosarin (NCMP), sarin (NIMP, PIMP and TIMP) and VX (NEMP and TEMP) and other organophosphorus compounds derived from insecticides. cyclohexyl methylphosphonofluoridate 76-86 acetylcholinesterase Rattus norvegicus 54-58 26210933-2 2016 In order to get more insight into the ability of bispyridinium oximes to reactivate human AChE inhibited by structurally different OP the reactivation kinetics of 31 compounds was determined with tabun-, cyclosarin- and paraoxon-inhibited AChE under identical experimental conditions. cyclohexyl methylphosphonofluoridate 204-214 acetylcholinesterase (Cartwright blood group) Homo sapiens 90-94 24912784-7 2015 Several oximes showed a moderate-to-high potency with cyclosarin-inhibited BChE. cyclohexyl methylphosphonofluoridate 54-64 butyrylcholinesterase Homo sapiens 75-79 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. cyclohexyl methylphosphonofluoridate 122-132 butyrylcholinesterase Homo sapiens 72-93 25450746-3 2015 Then, the model was applied for investigating the suitability of human BChE in combination with an oxime (HLo 7) to serve as a "pseudo-catalytic" scavenger of the organophosphorus nerve agent cyclosarin. cyclohexyl methylphosphonofluoridate 192-202 butyrylcholinesterase Homo sapiens 71-75 25522658-0 2015 Effect of reversible ligands on oxime-induced reactivation of sarin- and cyclosarin-inhibited human acetylcholinesterase. cyclohexyl methylphosphonofluoridate 73-83 acetylcholinesterase (Cartwright blood group) Homo sapiens 100-120 24477626-4 2014 Recently, a chimeric PON1 mutant, IIG1, was engineered toward the hydrolysis of the toxic isomers of soman and cyclosarin with high in vitro catalytic efficiency. cyclohexyl methylphosphonofluoridate 111-121 serum paraoxonase/arylesterase 1 Cavia porcellus 21-25 25450746-4 2015 The application of different perfusion protocols demonstrated the ability of BChE-oxime combinations to prevent BChE from irreversible inhibition by cyclosarin even at toxicologically relevant concentrations. cyclohexyl methylphosphonofluoridate 149-159 butyrylcholinesterase Homo sapiens 77-81 25450746-4 2015 The application of different perfusion protocols demonstrated the ability of BChE-oxime combinations to prevent BChE from irreversible inhibition by cyclosarin even at toxicologically relevant concentrations. cyclohexyl methylphosphonofluoridate 149-159 butyrylcholinesterase Homo sapiens 112-116 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. cyclohexyl methylphosphonofluoridate 75-85 acetylcholinesterase (Cartwright blood group) Homo sapiens 101-105 24571195-2 2014 We present here synthesis and initial in vitro characterization of 14 imidazole aldoximes and their structural refinement into three efficient reactivators of human butyrylcholinesterase (hBChE) inhibited covalently by nerve agent OPs, sarin, cyclosarin, VX, and the OP pesticide metabolite, paraoxon. cyclohexyl methylphosphonofluoridate 243-253 butyrylcholinesterase Homo sapiens 188-193 24630558-1 2014 The goal of this research was to identify structurally novel, non-quaternarypyridinium reactivators of GF (cyclosarin)-inhibited hAChE that possess the capacity to mediate in vitro reactivation of GF-inhibited human acetylcholinesterase (hAChE). cyclohexyl methylphosphonofluoridate 107-117 acetylcholinesterase (Cartwright blood group) Homo sapiens 129-134 24630558-1 2014 The goal of this research was to identify structurally novel, non-quaternarypyridinium reactivators of GF (cyclosarin)-inhibited hAChE that possess the capacity to mediate in vitro reactivation of GF-inhibited human acetylcholinesterase (hAChE). cyclohexyl methylphosphonofluoridate 107-117 acetylcholinesterase (Cartwright blood group) Homo sapiens 238-243 24443939-0 2014 Exploring the physicochemical properties of oxime-reactivation therapeutics for cyclosarin, sarin, tabun, and VX inactivated acetylcholinesterase. cyclohexyl methylphosphonofluoridate 80-90 acetylcholinesterase (Cartwright blood group) Homo sapiens 125-145 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. cyclohexyl methylphosphonofluoridate 49-59 acetylcholinesterase (Cartwright blood group) Homo sapiens 20-24 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. cyclohexyl methylphosphonofluoridate 75-85 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. cyclohexyl methylphosphonofluoridate 152-162 acetylcholinesterase (Cartwright blood group) Homo sapiens 105-109 22561105-4 2012 In the present study we investigated the kinetic interactions of a homologous series of bispyridinium monoximes bearing C1 to C12 alkylketone groups on the second pyridinium ring with native and cyclosarin-inhibited human AChE. cyclohexyl methylphosphonofluoridate 195-205 acetylcholinesterase (Cartwright blood group) Homo sapiens 222-226 23929454-0 2013 In vivo acetylcholinesterase reactivation in male guinea pigs and rhesus macaques following cyclosarin exposure and treatment with 1,1"-methylenebis{4-[(hydroxyimino)methyl] pyridinium} dimethanesulfonate. cyclohexyl methylphosphonofluoridate 92-102 acetylcholinesterase Cavia porcellus 8-28 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. cyclohexyl methylphosphonofluoridate 182-192 acetylcholinesterase (Cartwright blood group) Homo sapiens 141-146 23216060-2 2013 We identified TAB2OH (2-trimethylammonio-6-hydroxybenzaldehyde oxime) as an efficient reactivator of OP-hBChE conjugates formed by the nerve agents VX and cyclosarin, and the pesticide paraoxon. cyclohexyl methylphosphonofluoridate 155-165 butyrylcholinesterase Homo sapiens 104-109 23216060-4 2013 A 3-5-fold enhancement of in vitro reactivation of VX-, cyclosarin- and paraoxon-inhibited hBChE was observed when compared with the commonly used N-methylpyridinium aldoxime reactivator, 2PAM (2-pyridinealdoxime methiodide). cyclohexyl methylphosphonofluoridate 56-66 butyrylcholinesterase Homo sapiens 91-96 23376121-1 2013 Nerve agents such as tabun, cyclosarin and Russian VX inhibit the essential enzyme acetylcholinesterase (AChE) by organophosphorylating the catalytic serine residue. cyclohexyl methylphosphonofluoridate 28-38 acetylcholinesterase (Cartwright blood group) Homo sapiens 83-103 23376121-1 2013 Nerve agents such as tabun, cyclosarin and Russian VX inhibit the essential enzyme acetylcholinesterase (AChE) by organophosphorylating the catalytic serine residue. cyclohexyl methylphosphonofluoridate 28-38 acetylcholinesterase (Cartwright blood group) Homo sapiens 105-109 23376121-4 2013 To examine the structural basis for the pronounced substrate specificity of HI-6, we determined the binary crystal structures of Mus musculus AChE (mAChE) conjugated by cyclosarin and Russian VX and found a conformational mobility of the side chains of Phe338 and His447. cyclohexyl methylphosphonofluoridate 169-179 acetylcholinesterase Mus musculus 142-146 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. cyclohexyl methylphosphonofluoridate 120-130 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. cyclohexyl methylphosphonofluoridate 312-322 acetylcholinesterase (Cartwright blood group) Homo sapiens 40-44 22520752-4 2012 Our selection for prevention of acetylcholinesterase inhibition also resulted in the complete reversion of PON1"s stereospecificity, from an enantiomeric ratio (E) < 6.3 x 10(-4) in favor of the R(P) isomer of a cyclosarin analog in wild-type PON1, to E > 2,500 for the S(P) isomer in an evolved variant. cyclohexyl methylphosphonofluoridate 215-225 acetylcholinesterase (Cartwright blood group) Homo sapiens 32-52 22520752-4 2012 Our selection for prevention of acetylcholinesterase inhibition also resulted in the complete reversion of PON1"s stereospecificity, from an enantiomeric ratio (E) < 6.3 x 10(-4) in favor of the R(P) isomer of a cyclosarin analog in wild-type PON1, to E > 2,500 for the S(P) isomer in an evolved variant. cyclohexyl methylphosphonofluoridate 215-225 paraoxonase 1 Homo sapiens 107-111 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. cyclohexyl methylphosphonofluoridate 179-189 acetylcholinesterase (Cartwright blood group) Homo sapiens 145-150 22720164-6 2012 Based on the G2E6 polar mutations, we "humanized" an engineered variant of PON1 with high activity against cyclosarin (GF) and found that it was still very active against GF with much greater similarity to the human sequence. cyclohexyl methylphosphonofluoridate 107-117 paraoxonase 1 Homo sapiens 75-79 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. cyclohexyl methylphosphonofluoridate 49-59 acetylcholinesterase Rattus norvegicus 87-107 21930118-4 2011 Now, an in vitro study was performed to determine the reactivation kinetics of MINA with tabun-, sarin-, cyclosarin-, VX- and paraoxon-inhibited human AChE. cyclohexyl methylphosphonofluoridate 105-115 acetylcholinesterase (Cartwright blood group) Homo sapiens 151-155 22238531-6 2011 Among the nine compounds investigated, one exhibited remarkable activity, completely preventing acetylcholinesterase inhibition by the (-)-enantiomer of cyclosarin within seconds under the conditions of the assay. cyclohexyl methylphosphonofluoridate 153-163 acetylcholinesterase (Cartwright blood group) Homo sapiens 96-116 21217689-6 2011 We also developed a direct screen for protection of acetylcholinesterase from inactivation by nerve agents and used it to isolate variants that degrade the toxic isomer of the coumarin analog and cyclosarin itself with k(cat)/K(M) ~ 10(7) M(-1) min(-1). cyclohexyl methylphosphonofluoridate 196-206 acetylcholinesterase (Cartwright blood group) Homo sapiens 52-72 20051531-0 2010 Human carboxylesterase 1 stereoselectively binds the nerve agent cyclosarin and spontaneously hydrolyzes the nerve agent sarin. cyclohexyl methylphosphonofluoridate 65-75 carboxylesterase 1 Homo sapiens 6-24 21117832-1 2011 This study examined whether pro-2-PAM, a pro-drug dihydropyridine derivative of the oxime 2-pralidoxime (2-PAM) that can penetrate the brain, could prevent or reverse the central toxic effects of three nerve agents; sarin, cyclosarin, and VX. cyclohexyl methylphosphonofluoridate 223-233 peptidyl-glycine alpha-amidating monooxygenase Cavia porcellus 28-37 21117832-4 2011 Pro-2-PAM produced 9-25% reactivation of cyclosarin-inhibited ChE in blood, heart, and spinal cord, but no reactivation in brain or muscle tissues. cyclohexyl methylphosphonofluoridate 41-51 peptidyl-glycine alpha-amidating monooxygenase Cavia porcellus 6-9 21117832-10 2011 Pro-2-PAM was able to reactivate blood, heart, and spinal cord ChE inhibited by cyclosarin, but was not effective against cyclosarin-induced seizures. cyclohexyl methylphosphonofluoridate 80-90 peptidyl-glycine alpha-amidating monooxygenase Cavia porcellus 6-9 20510679-4 2010 In the present study, reactivation kinetics of tabun-, sarin-, cyclosarin-, VX- or paraoxon-ethyl-inhibited human AChE (hAChE) with a homologous series of bis-ortho-pyridiniumaldoximes, Ortho-4 - Ortho-9, was investigated with a robot-assisted setting, allowing determination of second-order reactivation rate constants as well as model calculations. cyclohexyl methylphosphonofluoridate 63-73 acetylcholinesterase (Cartwright blood group) Homo sapiens 114-118 20510679-4 2010 In the present study, reactivation kinetics of tabun-, sarin-, cyclosarin-, VX- or paraoxon-ethyl-inhibited human AChE (hAChE) with a homologous series of bis-ortho-pyridiniumaldoximes, Ortho-4 - Ortho-9, was investigated with a robot-assisted setting, allowing determination of second-order reactivation rate constants as well as model calculations. cyclohexyl methylphosphonofluoridate 63-73 acetylcholinesterase (Cartwright blood group) Homo sapiens 120-125 20510679-8 2010 In contrast, k(r) decreased with increasing linker length for sarin- and cyclosarin-inhibited hAChE. cyclohexyl methylphosphonofluoridate 73-83 acetylcholinesterase (Cartwright blood group) Homo sapiens 94-99 20192902-4 2010 In the case of cyclosarin- and soman-inhibited AChE, oxime K027 did not reach sufficient reactivation potency. cyclohexyl methylphosphonofluoridate 15-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 47-51 20888357-5 2010 By applying a modified kinetic approach, allowing the use of necessary high MMB-4 concentrations, it was possible to determine the reactivation constants with sarin-, cyclosarin-, VX-, VR- and tabun-inhibited AChE. cyclohexyl methylphosphonofluoridate 167-177 acetylcholinesterase (Cartwright blood group) Homo sapiens 209-213 20051531-4 2010 However, the ability of wild-type hCE1 to process the G-type nerve agents sarin and cyclosarin has not been determined. cyclohexyl methylphosphonofluoridate 84-94 carboxylesterase 1 Homo sapiens 34-38 20051531-5 2010 We report the crystal structure of hCE1 in complex with the nerve agent cyclosarin. cyclohexyl methylphosphonofluoridate 72-82 carboxylesterase 1 Homo sapiens 35-39 20051531-6 2010 We further use stereoselective nerve agent analogs to establish that hCE1 exhibits a 1700- and 2900-fold preference for the P(R) enantiomers of analogs of soman and cyclosarin, respectively, and a 5-fold preference for the P(S) isomer of a sarin analog. cyclohexyl methylphosphonofluoridate 165-175 carboxylesterase 1 Homo sapiens 69-73 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. cyclohexyl methylphosphonofluoridate 73-83 acetylcholinesterase Rattus norvegicus 133-137 18686075-11 2009 CONCLUSIONS: K206 and K269 are as effective in the reactivation of cyclosarin-inhibited AChE in rats and in the reduction of lethal toxic effects of cyclosarin in mice as obidoxime, but because their reactivating and therapeutic potency is significantly lower than that of HI-6, they are not suitable replacements for the currently available oximes for the treatment of cyclosarin poisoning. cyclohexyl methylphosphonofluoridate 67-77 acetylcholinesterase Rattus norvegicus 88-92 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. cyclohexyl methylphosphonofluoridate 73-83 acetylcholinesterase Rattus norvegicus 259-263 18565503-1 2008 Exposure to the organophosphorus nerve agents such as sarin, soman, cyclosarin, and VX causes acute intoxication by inhibiting acetylcholinesterase (AChE), where the serine residue of the active site can attack the phosphorous atom of the organophosphorus agents to form a strong P-O bond. cyclohexyl methylphosphonofluoridate 68-78 acetylcholinesterase (Cartwright blood group) Homo sapiens 127-147 18565503-1 2008 Exposure to the organophosphorus nerve agents such as sarin, soman, cyclosarin, and VX causes acute intoxication by inhibiting acetylcholinesterase (AChE), where the serine residue of the active site can attack the phosphorous atom of the organophosphorus agents to form a strong P-O bond. cyclohexyl methylphosphonofluoridate 68-78 acetylcholinesterase (Cartwright blood group) Homo sapiens 149-153 18547554-4 2008 In vivo determined percentage of reactivation of cyclosarin-inhibited blood and brain acetylcholinesterase in poisoned rats showed that HI-6 is the most efficacious reactivator of cyclosarin-inhibited acetylcholinesterase among studied oximes. cyclohexyl methylphosphonofluoridate 49-59 acetylcholinesterase Rattus norvegicus 86-106 20020898-1 2008 ABSTRACT This study describes the evaluation of the in vitro ability of two acetylcholinesterase (EC 3.1.1.7) reactivators, HI-6 and HLo-7, very promising at present, to reactivate human brain cholinesterases inhibited by the nerve agent cyclosarin. cyclohexyl methylphosphonofluoridate 238-248 acetylcholinesterase (Cartwright blood group) Homo sapiens 76-96 18547554-4 2008 In vivo determined percentage of reactivation of cyclosarin-inhibited blood and brain acetylcholinesterase in poisoned rats showed that HI-6 is the most efficacious reactivator of cyclosarin-inhibited acetylcholinesterase among studied oximes. cyclohexyl methylphosphonofluoridate 180-190 acetylcholinesterase Rattus norvegicus 86-106 18547554-4 2008 In vivo determined percentage of reactivation of cyclosarin-inhibited blood and brain acetylcholinesterase in poisoned rats showed that HI-6 is the most efficacious reactivator of cyclosarin-inhibited acetylcholinesterase among studied oximes. cyclohexyl methylphosphonofluoridate 180-190 acetylcholinesterase Rattus norvegicus 201-221 18588863-9 2008 TOX was also shown to be a better reactivator than 2-PAM for AChE inhibited by the nerve agents VX and cyclosarin. cyclohexyl methylphosphonofluoridate 103-113 peptidylglycine alpha-amidating monooxygenase Homo sapiens 53-56 18588863-9 2008 TOX was also shown to be a better reactivator than 2-PAM for AChE inhibited by the nerve agents VX and cyclosarin. cyclohexyl methylphosphonofluoridate 103-113 acetylcholinesterase (Cartwright blood group) Homo sapiens 61-65 17370251-5 2007 In order to investigate the feasibility of combining obidoxime and HI 6, human AChE inhibited by sarin, cyclosarin, VX, tabun and paraoxon was reactivated by these oximes either alone or in combination. cyclohexyl methylphosphonofluoridate 104-114 acetylcholinesterase (Cartwright blood group) Homo sapiens 79-83 17960099-3 2007 The reactivation ability of this reactivator was tested on tabun- and cyclosarin-inhibited AChE. cyclohexyl methylphosphonofluoridate 70-80 acetylcholinesterase (Cartwright blood group) Homo sapiens 91-95 17960099-4 2007 According to the results obtained, the new compound (without substitution and with decreased molecule size) showed increased reactivation potency in case of cyclosarin inhibited AChE. cyclohexyl methylphosphonofluoridate 157-167 acetylcholinesterase (Cartwright blood group) Homo sapiens 178-182 17129656-2 2007 We have previously identified three key positions in PON1 that affect OP hydrolysis: Leu69, Val346 and His115, that significantly enhance the hydrolysis of cyclosarin (GF), soman, chlorpyrifos-oxon (ChPo), O-isopropyl-O-(p-nitrophenyl)methylphosphonate (IMP-pNP) and diisopropyl fluorophosphate (DFP). cyclohexyl methylphosphonofluoridate 156-166 paraoxonase 1 Homo sapiens 53-57 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. cyclohexyl methylphosphonofluoridate 169-179 peptidylglycine alpha-amidating monooxygenase Homo sapiens 81-84 17503257-0 2007 Potency of five structurally different acetylcholinesterase reactivators to reactivate human brain cholinesterases inhibited by cyclosarin. cyclohexyl methylphosphonofluoridate 128-138 acetylcholinesterase (Cartwright blood group) Homo sapiens 39-59 17503257-3 2007 In this article, we compared the reactivation potency of five structurally different AChE reactivators (pralidoxime, trimedoxime, methoxime, HS-6, and BI-6) to reactivate cyclosarin-inhibited cholinesterases of human brain. cyclohexyl methylphosphonofluoridate 171-181 acetylcholinesterase (Cartwright blood group) Homo sapiens 85-89 17674811-5 2007 In vivo determined percentage of reactivation of cyclosarin-inhibited blood and brain acetylcholinesterase in poisoned rats showed that HI-6 is the most efficacious reactivator of cyclosarin-inhibited acetylcholinesterase among the studied oximes in the peripheral (blood) as well as central (brain) compartment although the differences between the oxime HI-6 and other tested oximes in the brain were not significant. cyclohexyl methylphosphonofluoridate 49-59 acetylcholinesterase Rattus norvegicus 86-106 17674811-5 2007 In vivo determined percentage of reactivation of cyclosarin-inhibited blood and brain acetylcholinesterase in poisoned rats showed that HI-6 is the most efficacious reactivator of cyclosarin-inhibited acetylcholinesterase among the studied oximes in the peripheral (blood) as well as central (brain) compartment although the differences between the oxime HI-6 and other tested oximes in the brain were not significant. cyclohexyl methylphosphonofluoridate 180-190 acetylcholinesterase Rattus norvegicus 86-106 17674811-5 2007 In vivo determined percentage of reactivation of cyclosarin-inhibited blood and brain acetylcholinesterase in poisoned rats showed that HI-6 is the most efficacious reactivator of cyclosarin-inhibited acetylcholinesterase among the studied oximes in the peripheral (blood) as well as central (brain) compartment although the differences between the oxime HI-6 and other tested oximes in the brain were not significant. cyclohexyl methylphosphonofluoridate 180-190 acetylcholinesterase Rattus norvegicus 201-221 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. cyclohexyl methylphosphonofluoridate 228-238 acetylcholinesterase (Cartwright blood group) Homo sapiens 35-39 17194020-0 2006 New group of xylene linker-containing acetylcholinesterase reactivators as antidotes against the nerve agent cyclosarin. cyclohexyl methylphosphonofluoridate 109-119 acetylcholinesterase (Cartwright blood group) Homo sapiens 38-58 18045198-6 2007 In this review, we would like to discuss relationship between structure of currently available AChE reactivators and their potency to reactivate cyclosarin-inhibited AChE. cyclohexyl methylphosphonofluoridate 145-155 acetylcholinesterase (Cartwright blood group) Homo sapiens 95-99 18045198-6 2007 In this review, we would like to discuss relationship between structure of currently available AChE reactivators and their potency to reactivate cyclosarin-inhibited AChE. cyclohexyl methylphosphonofluoridate 145-155 acetylcholinesterase (Cartwright blood group) Homo sapiens 166-170 18045198-7 2007 All outlined structural factors presented in this work should be helpful for the design of new generation of reactivators of cyclosarin-inhibited AChE. cyclohexyl methylphosphonofluoridate 125-135 acetylcholinesterase (Cartwright blood group) Homo sapiens 146-150 17265677-0 2006 Substituted monoquaternary oximes as reactivators of cyclosarin--and chlorpyrifos--inhibited acetylcholinesterase. cyclohexyl methylphosphonofluoridate 53-63 acetylcholinesterase Rattus norvegicus 93-113 17265677-10 2006 None of the tested AChE reactivators, reference compounds included, could be considered universal for both chlorpyrifos- and cyclosarin-inhibited AChE. cyclohexyl methylphosphonofluoridate 125-135 acetylcholinesterase Rattus norvegicus 146-150 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. cyclohexyl methylphosphonofluoridate 176-186 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. cyclohexyl methylphosphonofluoridate 176-186 acetylcholinesterase (Cartwright blood group) Homo sapiens 143-147 17194020-1 2006 Nerve agents such as sarin, cyclosarin and tabun are organophosphorus substances able to inhibit the enzyme acetylcholinesterase (AChE; EC 3.1.1.7). cyclohexyl methylphosphonofluoridate 28-38 acetylcholinesterase (Cartwright blood group) Homo sapiens 108-128 17194020-1 2006 Nerve agents such as sarin, cyclosarin and tabun are organophosphorus substances able to inhibit the enzyme acetylcholinesterase (AChE; EC 3.1.1.7). cyclohexyl methylphosphonofluoridate 28-38 acetylcholinesterase (Cartwright blood group) Homo sapiens 130-134 17438836-1 2006 In this work, in vitro potency of novel serie of monoquaternary pyridinium oximes to reactivate cyclosarin-inhibited acetylcholinesterase (AChE) was tested. cyclohexyl methylphosphonofluoridate 96-106 acetylcholinesterase (Cartwright blood group) Homo sapiens 117-137 16640555-2 2006 Mammalian paraoxonase (PON1) was found to be more active than Pseudomonas diminuta OP hydrolase (OPH) and squid O,O-di-isopropyl fluorophosphatase (DFPase) in detoxifying cyclosarin (O-cyclohexyl methylphosphonofluoridate) and soman (O-pinacolyl methylphosphonofluoridate). cyclohexyl methylphosphonofluoridate 171-181 paraoxonase 1 Homo sapiens 23-27 16640555-3 2006 Subsequently, nine directly evolved PON1 variants, selected for increased hydrolytic rates with a fluorogenic diethylphosphate ester, were tested for detoxification of cyclosarin, soman, O-isopropyl-O-(p-nitrophenyl) methyl phosphonate (IMP-pNP), DFP, and chlorpyrifos-oxon (ChPo). cyclohexyl methylphosphonofluoridate 168-178 paraoxonase 1 Homo sapiens 36-40 16640555-6 2006 Cyclosarin detoxification was approximately 10-fold faster with PON1 mutants V346A and L69V. cyclohexyl methylphosphonofluoridate 0-10 paraoxonase 1 Homo sapiens 64-68 16640555-11 2006 GC/pulsed flame photometer detector analysis, compared with assay of residual acetylcholinesterase inhibition, displayed stereoselective hydrolysis of cyclosarin, soman, and IMP-pNP, indicating that PON1 is less active toward the more toxic optical isomers. cyclohexyl methylphosphonofluoridate 151-161 paraoxonase 1 Homo sapiens 199-203 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. cyclohexyl methylphosphonofluoridate 121-131 acetylcholinesterase (Cartwright blood group) Homo sapiens 142-146 17438836-1 2006 In this work, in vitro potency of novel serie of monoquaternary pyridinium oximes to reactivate cyclosarin-inhibited acetylcholinesterase (AChE) was tested. cyclohexyl methylphosphonofluoridate 96-106 acetylcholinesterase (Cartwright blood group) Homo sapiens 139-143 16025528-0 2005 In vitro reactivation potency of some acetylcholinesterase reactivators against sarin- and cyclosarin-induced inhibitions. cyclohexyl methylphosphonofluoridate 91-101 acetylcholinesterase Rattus norvegicus 38-58 16429489-3 2005 K033 is sufficient reactivator of cyclosarin-inhibited AChE. cyclohexyl methylphosphonofluoridate 34-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 55-59 16025528-1 2005 In our study, we have tested six acetylcholinesterase (AChE) reactivators (pralidoxime, obidoxime, HI-6, trimedoxime, BI-6 and Hlo-7) for reactivation of sarin- and cyclosarin-inhibited AChE using an in vitro reactivation test. cyclohexyl methylphosphonofluoridate 165-175 acetylcholinesterase Rattus norvegicus 33-53 16025528-1 2005 In our study, we have tested six acetylcholinesterase (AChE) reactivators (pralidoxime, obidoxime, HI-6, trimedoxime, BI-6 and Hlo-7) for reactivation of sarin- and cyclosarin-inhibited AChE using an in vitro reactivation test. cyclohexyl methylphosphonofluoridate 165-175 acetylcholinesterase Rattus norvegicus 55-59 16025528-4 2005 On the other hand, only HI-6 is able to reactivate satisfactorily cyclosarin-inhibited AChE. cyclohexyl methylphosphonofluoridate 66-76 acetylcholinesterase Rattus norvegicus 87-91 16170392-10 2005 The same results were obtained for cyclosarin-inhibited AChE. cyclohexyl methylphosphonofluoridate 35-45 acetylcholinesterase Rattus norvegicus 56-60 15911280-2 2005 In the test of their potency to reactivate AChE inhibited by cyclosarin, the bis-pyridinium oxime 6b achieved reactivation potency higher than 10% at the lower concentration 10(-4)M. cyclohexyl methylphosphonofluoridate 61-71 acetylcholinesterase (Cartwright blood group) Homo sapiens 43-47 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. cyclohexyl methylphosphonofluoridate 95-105 acetylcholinesterase Rattus norvegicus 116-136 16170392-5 2005 Efficacies of new reactivators to reactivate tabun-, sarin-, cyclosarin- and VX-inhibited AChE were compared with the currently used AChE reactivators (pralidoxime, obidoxime and HI-6). cyclohexyl methylphosphonofluoridate 61-71 acetylcholinesterase Rattus norvegicus 90-94 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. cyclohexyl methylphosphonofluoridate 151-161 acetylcholinesterase (Cartwright blood group) Homo sapiens 110-130 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. cyclohexyl methylphosphonofluoridate 78-88 acetylcholinesterase (Cartwright blood group) Homo sapiens 99-119 14985944-4 2004 Reactivation of paraoxon-, sarin-, soman- and VX-inhibited AChE by obidoxime was impaired by POX-induced re-inhibition whereas no deviation of pseudo first-order kinetics was observed with tabun, cyclosarin and VR. cyclohexyl methylphosphonofluoridate 196-206 acetylcholinesterase (Cartwright blood group) Homo sapiens 59-63 15202491-0 2004 Reactivation of cyclosarin-inhibited rat brain acetylcholinesterase by pyridinium--oximes. cyclohexyl methylphosphonofluoridate 16-26 acetylcholinesterase Rattus norvegicus 47-67 15202491-2 2004 To gain insight into the reactivation kinetics, rat brain acetylcholinesterase (AChE) was inhibited in vitro by cyclosarin (pH 8.0, 25 degrees C) and reactivated with 22 different pyridiniumoximes. cyclohexyl methylphosphonofluoridate 112-122 acetylcholinesterase Rattus norvegicus 58-78 15202491-2 2004 To gain insight into the reactivation kinetics, rat brain acetylcholinesterase (AChE) was inhibited in vitro by cyclosarin (pH 8.0, 25 degrees C) and reactivated with 22 different pyridiniumoximes. cyclohexyl methylphosphonofluoridate 112-122 acetylcholinesterase Rattus norvegicus 80-84 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. cyclohexyl methylphosphonofluoridate 151-161 acetylcholinesterase (Cartwright blood group) Homo sapiens 132-136 12373455-3 2002 The reactivating properties of the two salts were compared on human erythrocyte AChE inhibited with paraoxon, sarin, cyclosarin and agent VX. cyclohexyl methylphosphonofluoridate 117-127 acetylcholinesterase (Cartwright blood group) Homo sapiens 80-84 15639788-1 2004 We investigated the relationship between the chemical structure of acetylcholinesterase (AChE; EC 3.1.1.7) reactivators and their potency in reactivating this enzyme, after prior inhibition by VX (O-ethyl-S-(2-diisopropylaminoethyl)-methylthiophosphonate), tabun, sarin, and cyclosarin. cyclohexyl methylphosphonofluoridate 275-285 acetylcholinesterase Rattus norvegicus 67-87 15639788-1 2004 We investigated the relationship between the chemical structure of acetylcholinesterase (AChE; EC 3.1.1.7) reactivators and their potency in reactivating this enzyme, after prior inhibition by VX (O-ethyl-S-(2-diisopropylaminoethyl)-methylthiophosphonate), tabun, sarin, and cyclosarin. cyclohexyl methylphosphonofluoridate 275-285 acetylcholinesterase Rattus norvegicus 89-93 15446359-0 2004 In vitro reactivation of acetylcholinesterase inhibited by cyclosarin using bisquaternary pyridinium aldoximes K005, K033, K027 AND K048. cyclohexyl methylphosphonofluoridate 59-69 acetylcholinesterase Rattus norvegicus 25-45 15446359-4 2004 Oxime K033 seems to be the most potent reactivator of cyclosarin-inhibited AChE. cyclohexyl methylphosphonofluoridate 54-64 acetylcholinesterase Rattus norvegicus 75-79 9587020-6 1998 Isolated human erythrocyte AChE was inhibited with soman, sarin, cyclosarin, tabun or VX for 30 min and reactivated in the absence of inhibitory activity over 5-60 min by obidoxime, pralidoxime, HI 6 or HLo 7 (10 and 30 microM). cyclohexyl methylphosphonofluoridate 65-75 acetylcholinesterase (Cartwright blood group) Homo sapiens 27-31 9806430-2 1998 To give more insight into the inhibition, reactivation and aging kinetics, human acetyl-(AChE) and butyrylcholinesterase (BChE) were inhibited by cyclosarin (k2 of 7.4 and 3.8 x 10(8) M(-1) min(-1), respectively; pH 7.4, 37 degrees C) and reactivated with obidoxime, pralidoxime and three experimental oximes. cyclohexyl methylphosphonofluoridate 146-156 acetylcholinesterase (Cartwright blood group) Homo sapiens 89-93 9806430-2 1998 To give more insight into the inhibition, reactivation and aging kinetics, human acetyl-(AChE) and butyrylcholinesterase (BChE) were inhibited by cyclosarin (k2 of 7.4 and 3.8 x 10(8) M(-1) min(-1), respectively; pH 7.4, 37 degrees C) and reactivated with obidoxime, pralidoxime and three experimental oximes. cyclohexyl methylphosphonofluoridate 146-156 butyrylcholinesterase Homo sapiens 99-120 9806430-2 1998 To give more insight into the inhibition, reactivation and aging kinetics, human acetyl-(AChE) and butyrylcholinesterase (BChE) were inhibited by cyclosarin (k2 of 7.4 and 3.8 x 10(8) M(-1) min(-1), respectively; pH 7.4, 37 degrees C) and reactivated with obidoxime, pralidoxime and three experimental oximes. cyclohexyl methylphosphonofluoridate 146-156 butyrylcholinesterase Homo sapiens 122-126 9587020-10 1998 Obidoxime and pralidoxime were weak reactivators of cyclosarin-inhibited AChE. cyclohexyl methylphosphonofluoridate 52-62 acetylcholinesterase (Cartwright blood group) Homo sapiens 73-77 1482284-1 1992 Cyclohexylmethylphosphonofluoridate (CMPF) is an organophosphate cholinesterase inhibitor with military significance. cyclohexyl methylphosphonofluoridate 0-35 butyrylcholinesterase Macaca mulatta 65-79 9600150-1 1998 In experiments on male rats the reactivating effects of oxime HI-6 and obidoxime in combination with atropine on acetylcholinesterase, inhibited by the highly toxic organophoshate cyclosin, were compared in various parts of the brain (frontal cortex, pontomedullar region, hypothalamus, hippocampus, basal ganglia) and the diaphragm. cyclohexyl methylphosphonofluoridate 180-188 acetylcholinesterase Rattus norvegicus 113-133 1482284-1 1992 Cyclohexylmethylphosphonofluoridate (CMPF) is an organophosphate cholinesterase inhibitor with military significance. cyclohexyl methylphosphonofluoridate 37-41 butyrylcholinesterase Macaca mulatta 65-79 35526478-4 2022 Mono-fluorinated oximes showed comparable reactivation to non-halogenated (except asoxime) and mono-chlorinated oximes in case of AChE inhibited by sarin, cyclosarin, VX, and tabun, but were less efficient than di-chlorinated ones. cyclohexyl methylphosphonofluoridate 155-165 acetylcholinesterase (Cartwright blood group) Homo sapiens 130-134