Title : Selective and irreversible inhibitors of mosquito acetylcholinesterases for controlling malaria and other mosquito-borne diseases.

Pub. Date : 2009 Aug 28

PMID : 19714254






8 Functional Relationships(s)
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1 We previously reported the finding of a free cysteine (Cys) residue at the entrance of the active site of acetylcholinesterase (AChE) in some insects but not in mammals, birds, and fish. Cysteine acetylcholinesterase (Cartwright blood group) Homo sapiens
2 We previously reported the finding of a free cysteine (Cys) residue at the entrance of the active site of acetylcholinesterase (AChE) in some insects but not in mammals, birds, and fish. Cysteine acetylcholinesterase (Cartwright blood group) Homo sapiens
3 These insects have two AChE genes (AP and AO), and only AP-AChE carries the Cys residue. Cysteine acetylcholinesterase (Cartwright blood group) Homo sapiens
4 Recently we reported a Cys-targeting small molecule that irreversibly inhibited all AChE activity extracted from aphids while an identical exposure caused no effect on the human AChE. Cysteine acetylcholinesterase (Cartwright blood group) Homo sapiens
5 Full inhibition of AChE in aphids indicates that AP-AChE contributes most of the enzymatic activity and suggests that the Cys residue might serve as a target for developing better aphicides. Cysteine acetylcholinesterase (Cartwright blood group) Homo sapiens
6 Full inhibition of AChE in aphids indicates that AP-AChE contributes most of the enzymatic activity and suggests that the Cys residue might serve as a target for developing better aphicides. Cysteine acetylcholinesterase (Cartwright blood group) Homo sapiens
7 This type of inhibition is fast ( approximately 30 min) and due to conjugation of the inhibitor to the active-site Cys of mosquito AP-AChE, according to our observed reactivation of the methanethiosulfonate-inhibited AChE by 2-mercaptoethanol. Cysteine acetylcholinesterase (Cartwright blood group) Homo sapiens
8 This type of inhibition is fast ( approximately 30 min) and due to conjugation of the inhibitor to the active-site Cys of mosquito AP-AChE, according to our observed reactivation of the methanethiosulfonate-inhibited AChE by 2-mercaptoethanol. Cysteine acetylcholinesterase (Cartwright blood group) Homo sapiens