Discovery of an Orally Efficacious Positive Allosteric Modulator of the Glucagon-like Peptide‑1 Receptor

The identification of LSN3318839, a positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R), is described. LSN3318839 increases the potency and efficacy of the weak metabolite GLP-1(9-36)NH2 to become a full agonist at the GLP-1R and modestly potentiates the activity of the...

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Veröffentlicht in:	Journal of medicinal chemistry 2021-03, Vol.64 (6), p.3439-3448
Hauptverfasser:	Willard, Francis S, Wainscott, David B, Showalter, Aaron D, Stutsman, Cynthia, Ma, Wenzhen, Cardona, Guemalli R, Zink, Richard W, Corkins, Christopher M, Chen, Qi, Yumibe, Nathan, Agejas, Javier, Cumming, Graham R, Minguez, José Miguel, Jiménez, Alma, Mateo, Ana I, Castaño, Ana M, Briere, Daniel A, Sloop, Kyle W, Bueno, Ana B
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Allosteric Regulation - drug effects Animals Blood Glucose - analysis Drug Discovery Glucagon-Like Peptide-1 Receptor - agonists Glucagon-Like Peptide-1 Receptor - chemistry Glucagon-Like Peptide-1 Receptor - metabolism Humans Hypoglycemic Agents - administration & dosage Hypoglycemic Agents - chemistry Hypoglycemic Agents - pharmacology Mice Models, Molecular Rats Rats, Sprague-Dawley
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