Acyl Ureas as Human Liver Glycogen Phosphorylase Inhibitors for the Treatment of Type 2 Diabetes

Using a focused screening approach, acyl ureas have been discovered as a new class of inhibitors of human liver glycogen phosphorylase (hlGPa). The X-ray structure of screening hit 1 (IC50 = 2 μM) in a complex with rabbit muscle glycogen phosphorylase b reveals that 1 binds at the AMP site, the main...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Journal of medicinal chemistry 2005-10, Vol.48 (20), p.6178-6193
Hauptverfasser:	Klabunde, Thomas, Wendt, K. Ulrich, Kadereit, Dieter, Brachvogel, Volker, Burger, Hans-Jörg, Herling, Andreas W, Oikonomakos, Nikos G, Kosmopoulou, Magda N, Schmoll, Dieter, Sarubbi, Edoardo, von Roedern, Erich, Schönafinger, Karl, Defossa, Elisabeth
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine Monophosphate - chemistry Allosteric Site Animals Binding Sites Biological and medical sciences Crystallography, X-Ray Diabetes Mellitus, Type 2 - drug therapy General and cellular metabolism. Vitamins Glycogen Phosphorylase, Liver Form - antagonists & inhibitors Glycogen Phosphorylase, Liver Form - chemistry Glycogen Phosphorylase, Muscle Form - chemistry Hepatocytes - drug effects Hepatocytes - enzymology Humans In Vitro Techniques Medical sciences Models, Molecular Pharmacology. Drug treatments Quantitative Structure-Activity Relationship Rabbits Rats Urea - analogs & derivatives Urea - chemical synthesis Urea - chemistry
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Schreiben Sie den ersten Kommentar!