Naslov
Native and tabun-inhibited cholinesterase interactions with oximes

Autori
Kovarik, Zrinka ; Katalinić, Maja ; Šinko, Goran

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

Izvornik
Technical Program: CBMTS Industry VI: The Fifth World Congress on Chemical, Biological and radiological Terrorism, Cavtat, Hrvatska / Bokan, Slavko - Zagreb : National Protection and Rescue Directorate, 2009, 40-40

Skup
CBMTS Industry VI: The Fifth World Congress on Chemical, Biological and radiological Terrorism

Mjesto i datum
Cavtat, Hrvatska, 05.04.2009. - 10.04.2009

Vrsta sudjelovanja
Predavanje

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
acetylcholinesterase; antidote; bioscavenger; butyrylcholinesterase; nerve agents; tabun; oxime; treatment

Sažetak
The phosphorylation of the serine hydroxyl group in the active site of acetylcholinesterase (AChE) inactivates this essential enzyme in neurotransmission. Its related enzyme butyrylcholinesterase (BChE) also interacts with organophosphorus compounds (OP) scavenging anti-cholinesterase agents and protects synaptic AChE from inhibition. Oximes are reactivators of AChE phosphorylated by OP including insecticides and nerve agents. The effectiveness of oxime-assisted reactivation is primarily attributed to the nucleophilic displacement rate of organophosphate, but efficiency varies with the structure of the bound organophosphate, the structure of the oxime as well as rates of several other cholinesterase's reactions. Besides reactivating cholinesterases, oximes also reversibly inhibit both cholinesterases and protect them from phosphorylation by OP. 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 and plasma BChE. Herein we bring an overview of in vitro interactions of native and tabun-inhibited AChE and BChE with oximes together with conformational analysis of the oximes relating molecular properties to their reactivation potency.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA