A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 ...
2022年6月1日 · Peptide agonists of the glucagon-like peptide-1 receptor (GLP-1R) have revolutionized diabetes therapy, but their use has been limited because they require injection. …
1139-P: Discovery of a Potent, Orally Efficacious Small Molecule ...
2024年6月14日 · Several small molecule agonists of the GLP-1 receptor have been investigated as potential alternatives to peptide-based GLP-1 agonists like Danuglipron, and Orforglipron. …
Molecular insights into ago-allosteric modulation of the human ... - Nature
2021年6月18日 · Here, we report three cryo-electron microscopy structures of GLP-1R bound to (i) compound 2 (an ago-allosteric modulator); (ii) compound 2 and GLP-1; and (iii) compound 2 …
Small-molecule agonists for the glucagon-like peptide 1 receptor
2007年1月16日 · Glucagon-like peptide (GLP)-1 is a 30-aa peptide hormone synthesized in l-cells of the small intestine . GLP-1, one of the incretins, is a natural postprandial hormone released …
Another milestone in the evolution of GLP-1-based diabetes ... - Nature
2021年6月14日 · Nature Medicine - The first clinical study of an oral small-molecule GLP-1 receptor agonist suggests effective glycemic control and weight loss in patients with type 2 …
Structural insights into the activation of GLP-1R by a small molecule ...
2020年7月28日 · Structural comparison with reported GLP-1R structures provides an insight into the mechanism of GLP-1R activation by a small molecule full agonist and a framework for …
Efficacy and Safety of Oral Small Molecule Glucagon-Like Peptide 1 ...
Treatment guidelines recommend glucagon-like peptide 1 receptor (GLP-1R) agonists in patients with type 2 diabetes (T2D) based on glycemic need and comorbidities and/or risk factors. 1,2 …
Structural basis of peptidomimetic agonism revealed by small-molecule …
Boc5 was identified as the first orthosteric nonpeptidic agonist of GLP-1R that mimics a broad spectrum of bioactivities of GLP-1 in vitro and in vivo. Here, we report the cryoelectron …
Safety and efficacy of the new, oral, small-molecule, GLP-1
2023年10月16日 · Aims: The present systematic review aimed to synthesize available data from recently published randomized trials (RCTs) investigating the efficacy and safety of the novel, …
Efficacy and Safety of Oral Small Molecule Glucagon-Like Peptide 1 ...
2023年5月1日 · Importance: Currently available glucagon-like peptide 1 receptor (GLP-1R) agonists for treating type 2 diabetes (T2D) are peptide agonists that require subcutaneous …
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