Oxime K033-reactivation Activity of Cholinesterases Inhibited by Various Nerve Agents and Organophosphorus Pesticides

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62690094%3A18470%2F18%3A50014625" target="_blank" >RIV/62690094:18470/18:50014625 - isvavai.cz</a>
Alternative codes found
RIV/00179906:_____/18:10380498 RIV/60162694:G44__/18:43889581 RIV/61989100:27240/18:10241741
Result on the web
<a href="http://www.eurekaselect.com/node/163753/article/oxime-k033-reactivation-activity-of-cholinesterases-inhibited-by-various-nerve-agents-and-organophosphorus-pesticides" target="_blank" >http://www.eurekaselect.com/node/163753/article/oxime-k033-reactivation-activity-of-cholinesterases-inhibited-by-various-nerve-agents-and-organophosphorus-pesticides</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.2174/1570164615666180713112238" target="_blank" >10.2174/1570164615666180713112238</a>

Result language
angličtina
Original language name
Oxime K033-reactivation Activity of Cholinesterases Inhibited by Various Nerve Agents and Organophosphorus Pesticides
Original language description
Background: Oxime K033 was considered a promising drug candidate originally developed for the treatment of nerve agent poisoning. This study summarizes its potency to reactivate in vitro acetylcholinesterase inhibited by several nerve agents (tabun, sarin, cyclosarin, soman, VX, Russian VX), mimic agent (DFP) and organophosphorus pesticide (chlorpyrifos) to show whether this compound might be used in cases of nerve agent or pesticide poisoning and considered as a so-called "broad spectrum reactivator". Methods: Moreover, docking studies of tested oxime with human AChE (HssAChE) complexed with several OPs were performed in order to verify its stability, binding modes and ability to adopt favourable conformations and to perform the reactivation reaction with each OP under experimental study. Results & Conclusion: According to the obtained results, K033 could not be considered a universal antidote due to its poor reactivation activity in the case of tabun-, soman- and DFP-inhibited rat acetylcholinesterase. On the contrary, its very good in vitro potency in human-relevant doses for cyclosarin inhibition is highlighted.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30107 - Medicinal chemistry

Project
<a href="/en/project/GA18-01734S" target="_blank" >GA18-01734S: Butyrylcholinesterase reactivators for preparation of pseudo-catalytic scavengers applicable for organophosphorus intoxications</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2018
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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