2-Phenoxy-nicotinamides are Potent Agonists at the Bile Acid Receptor GPBAR1 (TGR5)

2-Phenoxy-nicotinamides are Potent Agonists at the Bile Acid Receptor GPBAR1 (TGR5)

Potency with potential: 2‐Phenoxy‐ nicotinamides were identified as potent agonists at the GPBAR1 receptor, a target in the treatment of obesity, type 2 diabetes and metabolic syndrome. Extensive structure–activity relationship studies supported by homology modeling and docking resulted in the ident...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:ChemMedChem 2013-04, Vol.8 (4), p.569-576
Hauptverfasser: Martin, Rainer E., Bissantz, Caterina, Gavelle, Olivier, Kuratli, Christoph, Dehmlow, Henrietta, Richter, Hans G. F., Obst Sander, Ulrike, Erickson, Shawn D., Kim, Kyungjin, Pietranico-Cole, Sherrie Lynn, Alvarez-Sánchez, Rubén, Ullmer, Christoph
Format: Artikel
Sprache:eng
Schlagworte:
bile acid receptors
Binding Sites
GPBAR1
Humans
metabolic disorders
Molecular Docking Simulation
Niacinamide - chemistry
Niacinamide - metabolism
nicotinamides
Protein Binding
Protein Structure, Tertiary
Quinolines - chemistry
Receptors, G-Protein-Coupled - agonists
Receptors, G-Protein-Coupled - metabolism
Structure-Activity Relationship
structure-activity relationships
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:Potency with potential: 2‐Phenoxy‐ nicotinamides were identified as potent agonists at the GPBAR1 receptor, a target in the treatment of obesity, type 2 diabetes and metabolic syndrome. Extensive structure–activity relationship studies supported by homology modeling and docking resulted in the identification of optimized GPBAR1 agonists, potent against both human and mouse receptors, endowed with favorable physicochemical properties and good metabolic stability.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.201200474