Design of Gut-Restricted Thiazolidine Agonists of G Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5).
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00308
Abstract: Bile acid signaling and metabolism in the gastrointestinal tract have wide-ranging influences on systemic disease. G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) is one of the major effectors in bile acid sensing, with demonstrated… read more here.
Keywords: gut restricted; coupled bile; protein coupled; acid ... See more keywords
Discovery of a First-in-Class Gut-Restricted RET Kinase Inhibitor as a Clinical Candidate for the Treatment of IBS.
Sign Up to like & getrecommendations! Published in 2018 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.8b00035
Abstract: Abdominal pain and abnormal bowel habits represent major symptoms for irritable bowel syndrome (IBS) patients that are not adequately managed. Although the etiology of IBS is not completely understood, many of the functions of the… read more here.
Keywords: gut restricted; ibs; ret kinase; kinase ... See more keywords
Bariatric surgery reveals a gut-restricted TGR5 agonist with anti-diabetic effects
Sign Up to like & getrecommendations! Published in 2020 at "Nature chemical biology"
DOI: 10.1038/s41589-020-0604-z
Abstract: Bariatric surgery, the most effective treatment for obesity and type 2 diabetes, is associated with increased levels of the incretin hormone glucagon-like peptide-1 (GLP-1) and changes in levels of circulating bile acids. The levels of… read more here.
Keywords: gut restricted; surgery; tgr5 agonist; ca7s ... See more keywords