title: Recent progress in the identification of adenosine monophosphate-activated protein kinase (AMPK) activators.
abstract: Adenosine monophosphate-activated protein kinase (AMPK), a serine/threonine heterotrimeric protein kinase, is a critical regulator of cellular and whole body energy homeostasis. There are twelve known AMPK isoforms that are differentially expressed in tissues and species. Dysregulation of AMPK signaling is associated with a multitude of human pathologies. Hence isoform-selective activators of AMPK are actively being sought for the treatment of cardiovascular and metabolic diseases. The present review summarizes the status of direct AMPK activators from the patent and published literature.
authors.affiliation: Pfizer Global Research and Development, Cardiovascular and Metabolic Diseases Chemistry, 610 Main Street, Cambridge, MA 02139, USA. Electronic address: kimberly.o.cameron@pfizer.com.
authors.forename: Kimberly O
authors.initials: KO
authors.lastname: Cameron
authors.affiliation: Pfizer Global Research and Development, Worldwide Medicinal Chemistry, Eastern Point Road, Groton, CT 06340, USA.
authors.forename: Ravi G
authors.initials: RG
authors.lastname: Kurumbail
mesh_terms: D055372:AMP-Activated Protein Kinases / Q000737:chemistry / Q000378:metabolism*; D000818:Animals; D004789:Enzyme Activation; D020536:Enzyme Activators / Q000494:pharmacology*; D006801:Humans; D010766:Phosphorylation; D011487:Protein Conformation
chemical_list: D020536:Enzyme Activators; D055372:AMP-Activated Protein Kinases
keywords: AMPK; Allostery; CBM; CBS; Crystallography; Enzyme activators