AMP-activated protein kinase as a drug target

DG Hardie - Annu. Rev. Pharmacol. Toxicol., 2007 - annualreviews.org
Annu. Rev. Pharmacol. Toxicol., 2007annualreviews.org
The AMP-activated protein kinase (AMPK) system is a regulator of energy balance at both
the cellular and whole-body levels that, once activated by low energy status, effects a switch
from ATP-consuming anabolic pathways to ATP-producing catabolic pathways. It now
appears to be the major target for two existing classes of drug used to treat type 2 diabetes,
ie, the biguanides and thiazolidinediones. However, in both cases these activate AMPK
indirectly, and an interesting question concerns whether a drug that directly activated AMPK …
Abstract
The AMP-activated protein kinase (AMPK) system is a regulator of energy balance at both the cellular and whole-body levels that, once activated by low energy status, effects a switch from ATP-consuming anabolic pathways to ATP-producing catabolic pathways. It now appears to be the major target for two existing classes of drug used to treat type 2 diabetes, i.e., the biguanides and thiazolidinediones. However, in both cases these activate AMPK indirectly, and an interesting question concerns whether a drug that directly activated AMPK would retain the therapeutic benefits of the existing drugs while eliminating unwanted side effects. AMPK activators also now have potential as anticancer drugs.
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