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Metabolic Enzymes of Cocaine Metabolite Benzoylecgonine

Cocaine is one of the most addictive drugs without a U.S. Food and Drug Administration (FDA)-approved medication. Enzyme therapy using an efficient cocaine-metabolizing enzyme is recognized as the most promising approach to cocaine overdose treatment. The actual enzyme, known as RBP-8000, under current clinical development for cocaine overdose treatment is our previously designed T172R/G173Q mutant of bacterial cocaine esterase (CocE). The T172R/G173Q mutant is effective in hydrolyzing cocaine but inactive against benzoylecgonine (a major, biologically active metabolite of cocaine). Unlike cocaine itself, benzoylecgonine has an unusually stable zwitterion structure resistant to further hydrolysis in the body and environment. In fact, benzoylecgonine can last in the body for a very long time (a few days) and, thus, is responsible for the long-term toxicity of cocaine and a commonly used marker for drug addiction diagnosis in pre-employment drug tests. Because CocE and its mutants are all active against coc...

Authors:   Xiabin Chen; Xirong Zheng; Max Zhan; Ziyuan Zhou; Chang-Guo Zhan; Fang Zheng
Journal:   ACS Chemical Biology
Year:   2016
DOI:   10.1021/acschembio.6b00277
Publication date:   09-Jun-2016
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