PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 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 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 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 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 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 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 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 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 acetylcholinesterase (Cartwright blood group) Homo sapiens 101-105 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 17960099-4 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 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 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 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 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 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 16429489-3 2005 K033 is sufficient reactivator of cyclosarin-inhibited AChE. cyclohexyl methylphosphonofluoridate 34-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 55-59 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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