MB06322 (CS-917): A Potent and Selective Inhibitor of Fructose 1,6-Bisphosphatase for Controlling Gluconeogenesis in Type 2 Diabetes

In type 2 diabetes, the liver produces excessive amounts of glucose through the gluconeogenesis (GNG) pathway and consequently is partly responsible for the elevated glucose levels characteristic of the disease. In an effort to find safe and efficacious GNG inhibitors, we targeted the AMP binding si...

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Veröffentlicht in:	Proceedings of the National Academy of Sciences - PNAS 2005-05, Vol.102 (22), p.7970-7975
Hauptverfasser:	Erion, Mark D., van Poelje, Paul D., Dang, Qun, Kasibhatla, Srinivas Rao, Potter, Scott C., Reddy, M. Rami, Reddy, K. Raja, Jiang, Tao, Lipscomb, William N.
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine Monophosphate - metabolism Alanine - analogs & derivatives Alanine - pharmacology Alanine - therapeutic use Analysis of Variance Animals Binding sites Biological Sciences Carbon Radioisotopes - metabolism Diabetes Diabetes Mellitus, Type 2 - drug therapy Diabetes Mellitus, Type 2 - metabolism Dose-Response Relationship, Drug Drug Design Enzymes Fructose-Bisphosphatase - antagonists & inhibitors Fructose-Bisphosphatase - metabolism Gluconeogenesis - drug effects Glucose Hepatocytes Humans Lactates Liver Liver - metabolism Male Molecular Mimicry Organophosphonates - pharmacology Organophosphonates - therapeutic use Organophosphorus Compounds - pharmacology Organophosphorus Compounds - therapeutic use Phosphates Phosphonic acids Prodrugs Rats Rats, Sprague-Dawley Rats, Zucker Spectrophotometry Thiazoles - pharmacology Thiazoles - therapeutic use Type 2 diabetes mellitus
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