Naslov
Medical chemical defence against chemical nerve agent threats

Autori
Kovarik, Zrinka ; Maček-Hrvat, Nikolina ; Zorbaz, Tamara

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
Book of Abstract of 10th Joint Meeting on Medicinal Chemistry, Dubrovnik (Srebreno) / Basarić, Nikola ; Namjesnik, Danijel ; Perković, Ivana ; Stepanić, Višnja - Zagreb : Hrvatsko kemijsko društvo, 2017, 143-143

ISBN
978-953-55232-8-4

Skup
10th Joint Meeting on Medicinal Chemistry

Mjesto i datum
Srebreno, Hrvatska; Dubrovnik, Hrvatska, 25.06.2017. - 28.06.2017

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
acetylcholinesterase, butyrylcholinesterase, organophosphorus compounds, reactivation

Sažetak
The high toxicity of organophosphorus compounds (OP ; tabun, sarin, VX, cyclosarin and soman) originates from the irreversible inhibition of acetylcholinesterase (AChE), an essential enzyme in cholinergic neurotransmission. Poisonings that lead to life-threatening toxic manifestations call for immediate treatment, which usually consists of a combined administration of anticholinergic drugs and an aldoxime as the reactivator of AChE. Finding an optimal reactivator for prophylaxis against and post-treatment of OP toxicity is a continuing challenge. We identified several oximes with significantly improved human AChE reactivating efficacy against several OP and antidotal efficacy in mice when compared to standard reactivators. Further ex vivo testing of selected oximes and AChE mutants confirmed efficient oxime-assisted catalytic bioscavenging and neutralizing of OP exposure in whole blood. Therefore, our findings offer a platform for further antidote and scavenger development for nerve agents exposure. Supported by the Croatian Science Foundation (4307).

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA