Discovery of a Potent and Orally Efficacious TGR5 Receptor Agonist

[Image: see text] TGR5 is a G protein-coupled receptor (GPCR), activation of which promotes secretion of glucagon-like peptide-1 (GLP-1) and modulates insulin secretion. The 2-thio-imidazole derivative 6g was identified as a novel, potent, and selective TGR5 agonist (hTGR5 EC(50) = 57 pM, mTGR5 = 62...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Agarwal, Sameer, Patil, Amit, Aware, Umesh, Deshmukh, Prashant, Darji, Brijesh, Sasane, Santosh, Sairam, Kalapatapu V. V. M., Priyadarsiny, Priyanka, Giri, Poonam, Patel, Harilal, Giri, Suresh, Jain, Mukul, Desai, Ranjit C.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2015
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4716599/
https://ncbi.nlm.nih.gov/pubmed/26819665
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00323
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