Small molecule adenosine 5′-monophosphate activated protein kinase (AMPK) modulators and human diseases

Sandeep Rana, Elizabeth C. Blowers, Amarnath Natarajan

Research output: Contribution to journalArticle

45 Scopus citations

Abstract

Adenosine 5′-monophosphate activated protein kinase (AMPK) is a master sensor of cellular energy status that plays a key role in the regulation of whole-body energy homeostasis. AMPK is a serine/threonine kinase that is activated by upstream kinases LKB1, CaMKKβ, and Tak1, among others. AMPK exists as αβγ trimeric complexes that are allosterically regulated by AMP, ADP, and ATP. Dysregulation of AMPK has been implicated in a number of metabolic diseases including type 2 diabetes mellitus and obesity. Recent studies have associated roles of AMPK with the development of cancer and neurological disorders, making it a potential therapeutic target to treat human diseases. This review focuses on the structure and function of AMPK, its role in human diseases, and its direct substrates and provides a brief synopsis of key AMPK modulators and their relevance in human diseases.

Original languageEnglish (US)
Pages (from-to)2-29
Number of pages28
JournalJournal of Medicinal Chemistry
Volume58
Issue number1
DOIs
StatePublished - Jan 8 2015

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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