Recent Advances in the Medicinal Chemistry of Farnesoid X Receptor

Yuanying Fang, Lamees Hegazy, Brian N. Finck, Bahaa Elgendy

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

Abstract

Farnesoid X receptor (FXR) is an important regulator of bile acid, lipid, amino acid, and glucose homeostasis, hepatic inflammation, regeneration, and fibrosis. FXR has been recognized as a promising drug target for various metabolic diseases such as lipid disorders, nonalcoholic fatty liver disease (NAFLD), nonalcoholic steatohepatitis (NASH), and chronic kidney disease. A large number of FXR ligands have been developed by pharmaceutical companies and academic institutions, and several candidates have progressed into clinical trials in the past decade. However, it is continually a challenge to discover drugs targeting FXR due to side effects associated with long-term administration. In this perspective, we summarize the research progress on medicinal chemistry of FXR modulators from 2018 to the present by discussing the diverse structures of synthetic FXR modulators including steroidal and non-steroidal ligands, their structure–activity relationships (SARs), and their therapeutic applications.

Original languageEnglish
Pages (from-to)17545-17571
Number of pages27
JournalJournal of Medicinal Chemistry
Volume64
Issue number24
DOIs
StatePublished - Dec 23 2021

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