Direct AMP-activated protein kinase activators: a review of evidence from the patent literature

Expert Opin Ther Pat. 2012 Dec;22(12):1467-77. doi: 10.1517/13543776.2012.743994. Epub 2012 Nov 8.


Introduction: AMP-activated protein kinase (AMPK), a heterotrimeric protein complex with serine/threonine kinase activity has a central role in controlling cellular energy expenditure. Small molecule-based activation of AMPK represents an attractive therapeutic proposition because of AMPK's ability to regulate several anabolic and catabolic pathways that are critical to the development of metabolic disorders and cancer.

Areas covered: A comprehensive review of published patents that disclose direct AMPK activators is provided: 26 patents comprising 10 chemical classes, and supporting in vitro and in vivo data are discussed.

Expert opinion: AMPK activation holds promise as a possible pharmacological intervention in several disease states. The development of direct, highly specific AMPK activators is necessary to fully realize the opportunities linked to AMPK activation and appreciate the risks associated with it.

Publication types

  • Review

MeSH terms

  • AMP-Activated Protein Kinases / antagonists & inhibitors*
  • AMP-Activated Protein Kinases / metabolism
  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Drug Design*
  • Humans
  • Metabolic Diseases / drug therapy
  • Metabolic Diseases / enzymology
  • Molecular Structure
  • Molecular Targeted Therapy
  • Patents as Topic*
  • Protein Conformation
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Kinase Inhibitors / therapeutic use
  • Structure-Activity Relationship


  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • AMP-Activated Protein Kinases