期刊
FUTURE MEDICINAL CHEMISTRY
卷 8, 期 2, 页码 133-148出版社
FUTURE SCI LTD
DOI: 10.4155/fmc.15.178
关键词
bile acid signaling; bile acid receptor modulator; farnesoid X receptor; FXR antagonist; metabolic disorders; non-alcoholic steatohepatitis
资金
- Else Kroner-Fresenius Foundation (EKFS), Research Training Group 'Translational Research Innovation Pharma - TRIP'
Background: Bile acids can serve as signaling molecules by activating the nuclear receptor FXR and the G-protein-coupled receptor TGR5 and both bile acid receptors are prominent experimental drug targets. Results/methodology: In this study we optimized the fatty acid mimetic compound pirinixic acid to a new scaffold with the aim to develop novel FXR modulatory compounds. After a multistep structure-activity optimization process, we discovered FXR agonistic compounds and the first dual FXR antagonistic and TGR5 agonistic compound 79a. Conclusion: With this novel dual activity profile on both bile acid receptors 79a might be a valuable pharmalogical tool to further study the bile acid signaling network.
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