Combinatorial targeting of G-protein-coupled bile acid receptor 1 and cysteinyl leukotriene receptor 1 reveals a mechanistic role for bile acids and leukotrienes in drug-induced liver injury.

Michele BiagioliSilvia MarchianòCristina di GiorgioRosalinda RoselliMartina BordoniRachele BelliniBianca FiorilloValentina SepeBruno CatalanottiChiara CassianoMaria Chiara MontiEleonora DistruttiAngela ZampellaStefano Fiorucci

Published in: Hepatology (Baltimore, Md.) (2022)

By genetic and pharmacological approaches, we demonstrated that GPBAR1 and CYSLTR1 mutually interact in the development of DILI. A combinatorial approach designed to activate GPBAR1 while inhibiting CYSLTR1 reverses liver injury in models of DILI.

Keyphrases

drug induced
liver injury
adverse drug
signaling pathway
genome wide
cancer therapy
binding protein
gene expression
dna methylation