AMP-activated protein kinase as a drug target

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    196 Citations (Scopus)


    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.
    Original languageEnglish
    Pages (from-to)185-210
    Number of pages26
    JournalAnnual Review of Pharmacology and Toxicology
    Publication statusPublished - Feb 2007


    • AMP-Activated Protein Kinases
    • Antineoplastic Agents
    • Biguanides
    • Diabetes Mellitus, Type 2
    • Drug Delivery Systems
    • Humans
    • Multienzyme Complexes
    • Protein-Serine-Threonine Kinases
    • Thiazolidinediones


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