Gut Microbial β-Glucuronidase Inhibition via Catalytic Cycle Interception

Samuel J Pellock1, Benjamin C Creekmore1, William G Walton1

  • 1Department of Chemistry, Center for Integrated Chemical Biology and Drug Discovery, Eshelman School of Pharmacy, and Integrated Program for Biological and Genome Sciences, and Departments of Biochemistry and Microbiology, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.

ACS Central Science
|August 1, 2018
PubMed
Summary

Piperazine-containing compounds inhibit microbial β-glucuronidases (GUSs) by targeting their catalytic intermediate, reducing gut toxicities from various drugs. This mechanism involves forming inhibitor-glucuronide conjugates, offering a new therapeutic strategy.

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