Design, Synthesis, and Pharmacological Evaluation of Potent Positive Allosteric Modulators of the Glucagon-like Peptide-1 Receptor (GLP-1R).
Allosteric Regulation
/ drug effects
Animals
Blood Glucose
/ analysis
Cells, Cultured
Diabetes Mellitus, Type 2
/ blood
Drug Design
Glucagon-Like Peptide-1 Receptor
/ agonists
HEK293 Cells
Humans
Hypoglycemic Agents
/ chemical synthesis
Male
Mice
Mice, Inbred C57BL
Molecular Docking Simulation
Rats
Rats, Sprague-Dawley
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
12 03 2020
12 03 2020
Historique:
pubmed:
10
10
2019
medline:
1
9
2020
entrez:
10
10
2019
Statut:
ppublish
Résumé
The therapeutic success of peptidic GLP-1 receptor agonists for treatment of type 2 diabetes mellitus (T2DM) motivated our search for orally bioavailable small molecules that can activate the GLP-1 receptor (GLP-1R) as a well-validated target for T2DM. Here, the discovery and characterization of a potent and selective positive allosteric modulator (PAM) for GLP-1R based on a 3,4,5,6-tetrahydro-1
Identifiants
pubmed: 31596080
doi: 10.1021/acs.jmedchem.9b01071
doi:
Substances chimiques
Blood Glucose
0
Glucagon-Like Peptide-1 Receptor
0
Hypoglycemic Agents
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM