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TGR5 agonists are potential therapeutics for a variety of conditions including type 2 diabetes, obesity, and inflammatory bowel disease. After screening a library of chenodeoxycholic acid (CDCA) derivatives, it was… Click to show full abstract
TGR5 agonists are potential therapeutics for a variety of conditions including type 2 diabetes, obesity, and inflammatory bowel disease. After screening a library of chenodeoxycholic acid (CDCA) derivatives, it was determined that a range of modifications could be made to the acid moiety of CDCA which significantly increased TGR5 agonist potency. Surprisingly, methylation of the 7-hydroxyl of CDCA led to a further dramatic increase in potency, allowing the identification of 5.6 nM TGR5 agonist 17.
Keywords:
potency;
increase;
chenodeoxycholic acid;
methylation chenodeoxycholic;
tgr5
Journal Title: Journal of medicinal chemistry
Year Published: 2019
Link to full text (if available)
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Journal Title: Journal of medicinal chemistry
Year Published: 2019
Link to full text (if available)
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recommendations!