UNC10201652 is a potent Loop 1 (L1)-specific gut bacterial β-glucuronidase (GUSs) inhibitor with an IC50 value of 0.117 μM for E. coli GUS. UNC10201652 can block SN-38 glucuronide processing only in individuals whose fecal gut microbiota is highly abundant in L1 GUS enzymes.
UNC10201652 exhibits potently inhibitory activity against wild type E. coli with an EC50 of 74±7 nM[2].
References:
[1]. Jariwala PB, et al. Discovering the Microbial Enzymes Driving Drug Toxicity with Activity-Based Protein Profiling. ACS Chem Biol. 2020 Jan 17;15(1):217-225.
[2]. Pellock SJ, et al. Gut Microbial β-Glucuronidase Inhibition via Catalytic Cycle Interception. ACS Cent Sci. 2018 Jul 25;4(7):868-879.
















