An inhibitor of bile salt hydrolases
BSH-IN-1 is a covalent inhibitor of bile salt hydrolases.1 It is selective for bile salt hydrolases over the farnesoid X receptor (FXR) and G protein-coupled bile acid activated receptor (GP-BAR) at 100 ?M. BSH-IN-1 inhibits the bile salt hydrolases of the Gram-negative bacterium B. theta and the Gram-positive bacterium B. longum (IC50s = 427 and 108 nM, respectively). It also inhibits deconjugation of bile acids in a variety of bacteria and in resuspended mouse feces. Oral administration of BSH-IN-1 (10 mg/kg) decreases bile salt hydrolase activity and deconjugated bile acid levels in feces in mice.
1.Adhikari, A.A., Seegar, T.C., Ficarro, S.B., et al.Development of a covalent inhibitor of gut bacterial bile salt hydrolasesNat. Chem. Biol.16(3)318-326(2020)
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