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Current Drug Targets - Immune, Endocrine & Metabolic Disorders


ISSN (Print): 1568-0088
ISSN (Online): 1875-5917

Targeting the AMP-Activated Protein Kinase for the Treatment of Type 2 Diabetes

Author(s): Nicolas Musi and Laurie J. Goodyear

Volume 2 , Issue 2 , 2002

Page: [119 - 127] Pages: 9

DOI: 10.2174/1568005310202020119

Price: $65


The AMP-activated protein kinase (AMPK) is an energy-sensing enzyme that is activated in response to conditions of cellular stress such as muscle contraction and hypoxia. In skeletal muscle, activation of AMPK leads to increased glucose uptake, enhanced insulin sensitivity and oxidation of fatty acids. In the liver, AMPK activation causes an increase in fatty acid oxidation and inhibition of glucose production. These effects on glucose and fat metabolism make AMPK an important pharmacological target for the treatment of type 2 diabetes. Studies done in animal models of type 2 diabetes have shown that pharmacological activation of AMPK with the compound 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR) decreases blood glucose and insulin concentrations. While strong efforts are underway in order to identify novel AMPKactivating compounds, the safety of chronic pharmacological activation of AMPK remains to be determined.

Keywords: type2 diabetes, amp-activated pk, ampk, energy-sensing enzyme, amp kinase,aicar

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