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- W3099724881 abstract "Significance Glucagon-like peptide-1 receptor agonists have become established as a leading class of diabetes medications. However, these peptide-based drugs are administered by subcutaneous injection or, in one case, by a complex oral dosing regimen. We now report the discovery of LY3502970, a potent and selective small-molecule GLP-1R agonist. LY3502970 exhibits preclinical pharmacology equivalent to a marketed injectable GLP-1R agonist and possesses pharmacokinetic properties compatible with oral dosing in humans. Cryoelectron microscopy (cryo-EM) studies reveal an ECD-driven receptor binding mode for LY3502970 that provides a favorable pharmacological profile." @default.
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- W3099724881 date "2020-11-11" @default.
- W3099724881 modified "2023-10-11" @default.
- W3099724881 title "Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist" @default.
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- W3099724881 doi "https://doi.org/10.1073/pnas.2014879117" @default.
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