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- W2893514707 endingPage "782" @default.
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- W2893514707 abstract "Farnesoid X receptor (FXR), a nuclear receptor mainly expressed in enterohepatic tissues, is a master for bile acid, lipid and glucose homeostasis. Additionally, it acts as a cell protector with unclear mechanism but may be implicated in combating against inflammation, fibrosis and cancers. FXR is thus accepted as a promising target particularly for the enterohepatic diseases, and numerous FXR modulators have been patented and developed.This review provides an update on the development of FXR modulators for enterohepatic diseases and offers an in-depth perspective on new strategies for the development of novel FXR modulators.Despite the development of numerous FXR modulators, which culminated in the successful launch of obeticholic acid (OCA), it remains a matter of debate on how the function of FXR should be exploited for therapeutic purposes. The improvement for obesity achieved by either FXR agonists or antagonists is still in confusion. Whether the side effect of pruritus induced by OCA could be exempted for non-steroidal FXR agonists needs further validation. Apart from the development of conventional FXR ligands, emerging evidence support that restoration of FXR protein level may represent a new strategy in targeting FXR for enterohepatic and metabolic diseases." @default.
- W2893514707 created "2018-10-05" @default.
- W2893514707 creator A5011573172 @default.
- W2893514707 creator A5018454768 @default.
- W2893514707 creator A5033680007 @default.
- W2893514707 creator A5048615638 @default.
- W2893514707 creator A5072541326 @default.
- W2893514707 date "2018-10-08" @default.
- W2893514707 modified "2023-10-17" @default.
- W2893514707 title "FXR modulators for enterohepatic and metabolic diseases" @default.
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