molecules of the year


oral non-peptide GLP-1R GPCR partial agonist

in Ph. I for Type 2 diabetes, HV study complete

from cell-based screen and opt.

PNAS, Nov. 11, 2020

Chugai, Shizuoka, JP / Eli Lilly, Indianapolis, IN

1 min read

November’s molecule, the Chugai/Lilly GLP-1R agonist LY3502970, is a highly potent and selective, oral, biased partial agonist of the GLP-1R GPCR. GLP-1R agonists have been approved for many years now to treat Type II diabetes mellitus, due to their ability to stimulate insulin secretion in pancreatic beta-cells. However, until recently, all GLP-1R agonists were all non-orally available peptides, requiring subcutaneous injection. The development of oral GLP-1R agonists has thus been a hot area in metabolic disease research, but GLP-1R has turned out to be an exceptionally challenging GPCR to drug with the desired mode of action, as the structure of LY3502970 implies! The article describes this molecules interesting mechanism of action with significant structural detail thanks to Cryo-EM, and LY3502970…

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