AMP-activated protein kinase as a drug target

Annu Rev Pharmacol Toxicol. 2007;47:185-210. doi: 10.1146/annurev.pharmtox.47.120505.105304.


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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • AMP-Activated Protein Kinases
  • Antineoplastic Agents / pharmacology
  • Biguanides / pharmacology*
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Drug Delivery Systems*
  • Humans
  • Multienzyme Complexes / drug effects*
  • Multienzyme Complexes / physiology
  • Protein-Serine-Threonine Kinases / drug effects*
  • Protein-Serine-Threonine Kinases / physiology
  • Thiazolidinediones / pharmacology*


  • Antineoplastic Agents
  • Biguanides
  • Multienzyme Complexes
  • Thiazolidinediones
  • Protein-Serine-Threonine Kinases
  • AMP-Activated Protein Kinases