Katz_2015_Chembiochem_16_2205

Reference

Title : Discovery of New Classes of Compounds that Reactivate Acetylcholinesterase Inhibited by Organophosphates - Katz_2015_Chembiochem_16_2205
Author(s) : Katz FS , Pecic S , Tran TH , Trakht I , Schneider L , Zhu Z , Ton-That L , Luzac M , Zlatanic V , Damera S , MacDonald J , Landry DW , Tong L , Stojanovic MN
Ref : Chembiochem , 16 :2205 , 2015
Abstract : Acetylcholinesterase (AChE) that has been covalently inhibited by organophosphate compounds (OPCs), such as nerve agents and pesticides, has traditionally been reactivated by using nucleophilic oximes. There is, however, a clearly recognized need for new classes of compounds with the ability to reactivate inhibited AChE with improved in vivo efficacy. Here we describe our discovery of new functional groups-Mannich phenols and general bases-that are capable of reactivating OPC-inhibited AChE more efficiently than standard oximes and we describe the cooperative mechanism by which these functionalities are delivered to the active site. These discoveries, supported by preliminary in vivo results and crystallographic data, significantly broaden the available approaches for reactivation of AChE.
ESTHER : Katz_2015_Chembiochem_16_2205
PubMedSearch : Katz_2015_Chembiochem_16_2205
PubMedID: 26350723
Gene_locus related to this paper: mouse-ACHE

Related information

Gene_locus related to this paper: mouse-ACHE

Citations formats

Katz FS, Pecic S, Tran TH, Trakht I, Schneider L, Zhu Z, Ton-That L, Luzac M, Zlatanic V, Damera S, MacDonald J, Landry DW, Tong L, Stojanovic MN (2015)
Discovery of New Classes of Compounds that Reactivate Acetylcholinesterase Inhibited by Organophosphates
Chembiochem 16 :2205

Katz FS, Pecic S, Tran TH, Trakht I, Schneider L, Zhu Z, Ton-That L, Luzac M, Zlatanic V, Damera S, MacDonald J, Landry DW, Tong L, Stojanovic MN (2015)
Chembiochem 16 :2205