Advances in the development of AMPK-activating compounds

Apiradee Sriwijitkamol, Nicolas Musi

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

Background: AMP-activated protein kinase (AMPK) is an energy sensing enzyme that controls glucose and lipid metabolism. Objective: This review summarizes the present data on AMPK as a pharmacologic target for the treatment of metabolic disorders. Methods: The mechanisms governing AMPK activity and how this enzyme controls different metabolic pathways are reviewed briefly, and details about the effect that AMPK activators have on glucose metabolism are provided. Conclusion: Evidence obtained using the AMPK-activating compound 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside (AICAR) suggests that AMPK promotes glucose transport into skeletal muscles and that this enzyme inhibits hepatic glucose production. AICAR also induces fatty acid oxidation in muscle and inhibits cholesterol synthesis in the liver. The metabolic effects of AICAR on glucose and lipid metabolism indicate that AMPK may be a good pharmacologic target for the treatment of type 2 diabetes and hypercholesterolemia. Novel AMPK-specific compounds are allowing researchers to examine whether this enzyme is a useful pharmacologic target for the treatment of human disease and whether chronic activation of AMPK will be safe.

Original languageEnglish (US)
Pages (from-to)1167-1176
Number of pages10
JournalExpert Opinion on Drug Discovery
Volume3
Issue number10
DOIs
StatePublished - Oct 2008

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AMP-Activated Protein Kinases
Glucose
Aminoimidazole Carboxamide
Enzymes
Lipid Metabolism
Liver
Metabolic Networks and Pathways
Hypercholesterolemia
Type 2 Diabetes Mellitus
Skeletal Muscle
Chronic Disease
Fatty Acids
Cholesterol
Research Personnel
Muscles

Keywords

  • A-769662
  • ACC
  • AICAR
  • AMPK
  • Metformin

ASJC Scopus subject areas

  • Drug Discovery

Cite this

Advances in the development of AMPK-activating compounds. / Sriwijitkamol, Apiradee; Musi, Nicolas.

In: Expert Opinion on Drug Discovery, Vol. 3, No. 10, 10.2008, p. 1167-1176.

Research output: Contribution to journalArticle

Sriwijitkamol, Apiradee ; Musi, Nicolas. / Advances in the development of AMPK-activating compounds. In: Expert Opinion on Drug Discovery. 2008 ; Vol. 3, No. 10. pp. 1167-1176.
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