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• W2050899637 abstract "The peptide hormone glucagon-like peptide (GLP)-1 has important actions resulting in glucose lowering along with weight loss in patients with type 2 diabetes. As a peptide hormone, GLP-1 has to be administered by injection. Only a few small-molecule agonists to peptide hormone receptors have been described and none in the B family of the G protein coupled receptors to which the GLP-1 receptor belongs. We have discovered a series of small molecules known as ago-allosteric modulators selective for the human GLP-1 receptor. These compounds act as both allosteric activators of the receptor and independent agonists. Potency of GLP-1 was not changed by the allosteric agonists, but affinity of GLP-1 for the receptor was increased. The most potent compound identified stimulates glucose-dependent insulin release from normal mouse islets but, importantly, not from GLP-1 receptor knockout mice. Also, the compound stimulates insulin release from perfused rat pancreas in a manner additive with GLP-1 itself. These compounds may lead to the identification or design of orally active GLP-1 agonists." @default.
• W2050899637 created "2016-06-24" @default.
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• W2050899637 date "2007-01-16" @default.
• W2050899637 modified "2023-10-03" @default.
• W2050899637 title "Small-molecule agonists for the glucagon-like peptide 1 receptor" @default.
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• W2050899637 doi "https://doi.org/10.1073/pnas.0605701104" @default.
• W2050899637 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/1783418" @default.
• W2050899637 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/17213325" @default.
• W2050899637 hasPublicationYear "2007" @default.
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