Discovery of V-0219: A Small-Molecule Positive Allosteric Modulator of the Glucagon-Like Peptide-1 Receptor toward Oral Treatment for “Diabesity”
Juan Decara, Henar Vázquez‐Villa, José Brea, Mónica Alonso, Raj Kamal Srivastava, Laura Orío, Francisco Alén, Juan Suárez, Elena Baixerás, Javier García‐Cárceles, Andrea Escobar-Peña, Beat Lutz, Ramón Rodríguez, Eva Codesido, F.J. García-Ladona, Teresa Bennett, Juan Antonio Hernández Ballesteros, Jacobo Cruces, Marı́a Isabel Loza, Bellinda Benhamú, Fernando Rodrı́guez de Fonseca, María L. López-Rodrı́guez
Abstract
behavior bolsters the interest of a small-molecule PAM of GLP-1R as a promising therapeutic approach for the increasingly prevalent obesity-associated diabetes.
Topics & Concepts
ChemistryAllosteric regulationSmall moleculeAllosteric modulatorIn vivoPharmacologyGlucagon-like peptide-1InsulinReceptorType 2 diabetesEndocrinologyDiabetes mellitusInternal medicineBiochemistryMedicineBiologyBiotechnologyDiabetes Treatment and ManagementReceptor Mechanisms and SignalingNeuropeptides and Animal Physiology