Abstract

AMP-activated protein kinase (AMPK) is the key component of a regulatory system that senses changes in cellular energy status (AMP:ATP ratio) and modifies multiple catabolic and anabolic pathways to re-establish proper ATP concentrations. Recent findings have also indicated a significant role for the kinase in regulating whole body energy metabolism including many of the parameters that are defective in type 2 diabetes. In fact, a large body of evidences suggests that pharmacological activation of the kinase could have multiple beneficial effects with regard to the metabolic abnormalities associated with diabetes. This review provides a brief overview of how AMPK regulates glucose and fat metabolism and how activation of the kinase might affect the metabolic abnormalities of type 2 diabetes. In addition, an update is provided on the small number of novel AMPK activators that have recently been generated from targeted drug discovery programs.

Keywords: type diabetes, antidiabetic agents, ampk activators, energy balance, dephosphorylation, drug target