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- W64069181 abstract "Cholinesterases (ChEs)—acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)—are of special concern to the toxicology of pesticides. This chapter discusses ChEs, their importance in understanding the toxicity of organophosphate esters (OPs) and carbamate pesticides (CBs), and their application to risk assessment of anticholinesterase pesticides and other agents. ChEs are specialized carboxylic ester hydrolases that break down esters of choline. The knowledge of the three-dimensional structure of the ChEs has led to a better understanding of the mechanisms of action of drugs and chemical agents that inhibit the hydrolysis of choline esters. In general, there are three major domains for inhibitors to bind: the acyl and choline pockets of the active center, and the peripheral anionic site. CBs and OP pesticides inhibit enzyme activity by acting as alternate substrates to acetylcholine (Ach). The toxicities of OPs and CBs often are correlated with the extent of their inhibitions of brain AChE. One example of a carboxyesterase is serum paraoxonase (PON1), an A-esterase associated with high-density plasma lipoproteins; PON1 destroys OPs such as the oxon analogs of parathion and chlorpyrifos. Direct evidence for its role in detoxifying OPs was provided by showing that mice exposed to chlorpyrifos were protected against cholinesterase inhibition and toxicity by administration of purified PON1." @default.
- W64069181 created "2016-06-24" @default.
- W64069181 creator A5083460601 @default.
- W64069181 date "2001-01-01" @default.
- W64069181 modified "2023-09-23" @default.
- W64069181 title "Cholinesterases" @default.
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