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SAR studies on FXR modulators led to the discovery of the first combined FXR antagonistic/TGR5 agonistic compound

Lamers, Christina and Merk, Daniel and Gabler, Matthias and Flesch, Daniel and Kaiser, Astrid and Schubert-Zsilavecz, Manfred. (2016) SAR studies on FXR modulators led to the discovery of the first combined FXR antagonistic/TGR5 agonistic compound. Future medicinal chemistry, 8 (2). pp. 133-148.

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Official URL: https://edoc.unibas.ch/70321/

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Abstract

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.; 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.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Molekulare Pharmazie (Ricklin)
UniBasel Contributors:Lamers, Christina
Item Type:Article, refereed
Article Subtype:Research Article
ISSN:1756-8927
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:17 May 2020 20:43
Deposited On:17 May 2020 20:43

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