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In vitro screening of acetylcholinesterase reactivating potency and oxime assisted organophosphate hydrolysis for a library of novel oxime reactivators synthesized by "click-chemistry" (CROSBI ID 544338)

Prilog sa skupa u časopisu | sažetak izlaganja sa skupa | međunarodna recenzija

Radić, Zoran ; Kalisiak, Jaroslaw ; Zhang, Limin ; Kovarik, Zrinka ; Čalić, Maja ; Amitai, Gabi ; Fokin, Valery V. ; Sharpless, Barry K. ; Taylor Palmer In vitro screening of acetylcholinesterase reactivating potency and oxime assisted organophosphate hydrolysis for a library of novel oxime reactivators synthesized by "click-chemistry" // FASEB journal. 2008

Podaci o odgovornosti

Radić, Zoran ; Kalisiak, Jaroslaw ; Zhang, Limin ; Kovarik, Zrinka ; Čalić, Maja ; Amitai, Gabi ; Fokin, Valery V. ; Sharpless, Barry K. ; Taylor Palmer

engleski

In vitro screening of acetylcholinesterase reactivating potency and oxime assisted organophosphate hydrolysis for a library of novel oxime reactivators synthesized by "click-chemistry"

Organophosphorus (OP) pesticides and nerve warfare agents stoichiometrically inactivate acetylcholinesterase (AChE ; EC 3.1.1.7) by phosphylation of the active serine 203. Catalytic activity of the covalently inhibited AChE can be effectively reclaimed only by nucleophiles stronger than water. In this study we analyzed reactivating potency of close to 100 novel oximes synthesized using [3+2] cycloaddition between alkyne and azide building blocks, the "Click reaction". Human AChE (hAChE) covalent adducts resulting from inhibition by nerve agents soman, sarin, cyclosarin, VX and tabun and pesticide derived paraoxon were used for reactivation experiments. We were able to identify several oximes with significantly improved reactivating efficacy against larger spectrum of offending OPs. We furthermore measured rates of hydrolysis of fluorescent derivatives of nerve agents soman, sarin, cyclosarin and VX assisted by oxime reactivators, for the wt AChE and Tyr337Ala mutant of hAChE, and found that in the presence of selected oximes rates of OP hydrolysis increased up to forty times with wt AChE and more with the Tyr337Ala hAChE mutant.

oximes; reactivativation; VX; tabun; human acetylcholinesterase; mutants

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Podaci o prilogu

2008.

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objavljeno

Podaci o matičnoj publikaciji

FASEB journal

0892-6638

Podaci o skupu

Experimental Biology 2008: "Today’ s Research: Tomorrow’ s Health"

poster

05.04.2008-09.04.2008

San Diego (CA), Sjedinjene Američke Države

Povezanost rada

Kemija, Temeljne medicinske znanosti

Indeksiranost