In:
Future Medicinal Chemistry, Future Science Ltd, Vol. 8, No. 2 ( 2016-02), p. 133-148
Abstract:
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.
Type of Medium:
Online Resource
ISSN:
1756-8919
,
1756-8927
Language:
English
Publisher:
Future Science Ltd
Publication Date:
2016
SSG:
15,3