Skip to main page content
U.S. flag

An official website of the United States government

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2024 Aug 7;15(9):3026-3037.
doi: 10.1039/d4md00473f. eCollection 2024 Sep 19.

Recent advancements in the structural exploration of TGR5 agonists for diabetes treatment

Rachana S Bhimanwar  1   2 , Amit Mittal  2 , Snehal Chaudhari  3 , Vikas Sharma  2
Affiliations
Review

Recent advancements in the structural exploration of TGR5 agonists for diabetes treatment

Rachana S Bhimanwar et al. RSC Med Chem. .

Abstract

TGR5, a receptor that interacts with bile acids on cell surfaces, has become a promising therapeutic target for type II diabetes due to its ability to regulate energy expenditure and blood sugar levels. While several TGR5 agonists have been identified, only a few are currently in clinical trials. This article reviews the promising TGR5 agonists discovered in recent years, highlighting the chemical structure and pharmacological profile of the most effective compounds. With the limited number of effective drugs available for treating type II diabetes, the search for a potent TGR5 agonist with high efficacy and fewer side effects continues. The goal of this article is to provide an overview of the latest advancements in TGR5 agonists and offer insights for the future development of novel, potent TGR5 agonists for diabetes treatment. A noteworthy aspect addressed in the discussion is the common side effect associated with TGR5 agonist treatment - gallbladder filling. The review also explores potential strategies to mitigate this side effect, with the goal of improving the overall safety and tolerability of TGR5-targeted therapies.

PubMed Disclaimer

Conflict of interest statement

The authors have declared no conflicts of interest.

Similar articles

See all similar articles

References

    1. IDF Diabetes Atlas, 10th edn, 2022, https://www.diabetesatlas.org/en/ (retrieved on 04-April-2023
    1. Kawamata Y. Fujii R. Hosoya M. Harada M. Yoshida H. J. Biol. Chem. 2003;278:9435–9440. doi: 10.1074/jbc.M209706200. - DOI - PubMed

    2. , pmid:12524422

    1. Thomas C. Pellicciari R. Pruzanski M. Auwerx J. Schoonjans K. Nat. Rev. Drug Discovery. 2008;7:678–693. doi: 10.1038/nrd2619. - DOI - PubMed
    1. Houten S. M. Watanabe M. Auwerx J. EMBO J. 2006;25:1419–1425. doi: 10.1038/sj.emboj.7601049. - DOI - PMC - PubMed
    1. Foord S. M. Bonner T. I. Neubig R. R. Rosser E. M. Pin J. P. Davenport A. P. Pharmacol. Rev. 2005;57:279–288. doi: 10.1124/pr.57.2.5. - DOI - PubMed

LinkOut - more resources