Catalytic activities of a highly efficient cocaine hydrolase for hydrolysis of biologically active cocaine metabolites norcocaine and benzoylecgonine.

ABSTRACT: Cocaine is a widely abused, hepatotoxic drug without an FDA-approved pharmacotherapy specific for cocaine addiction or overdose. It is recognized as a promising therapeutic strategy to accelerate cocaine metabolism which can convert cocaine to pharmacologically inactive metabolite(s) using an efficient cocaine-metabolizing enzyme. Our previous studies have successfully designed and discovered a highly efficient cocaine hydrolase, denoted as CocH5-Fc(M6), capable of rapidly hydrolyzing cocaine at the benzoyl ester moiety. In the present study, we determined the kinetic parameters of CocH5-Fc(M6) against norcocaine (k_cat = 9,210 min^-1, K_M = 20.9 μM, and k_cat/K_M = 1.87 × 10⁵ min^-1 M^-1) and benzoylecgonine

SUBMITTER: Shang L 

PROVIDER: S-EPMC9837138 | biostudies-literature | 2023 Jan

REPOSITORIES: biostudies-literature