Recent progress in the identification of adenosine monophosphate-activated protein kinase (AMPK) activators

Bioorg Med Chem Lett. 2016 Nov 1;26(21):5139-5148. doi: 10.1016/j.bmcl.2016.09.065.

Kimberly O Cameron ¹, Ravi G Kurumbail ²

Affiliations

1 Pfizer Global Research and Development, Cardiovascular and Metabolic Diseases Chemistry, 610 Main Street, Cambridge, MA 02139, USA. Electronic address: kimberly.o.cameron@pfizer.com.
2 Pfizer Global Research and Development, Worldwide Medicinal Chemistry, Eastern Point Road, Groton, CT 06340, USA.

PMID: 27727125 DOI: 10.1016/j.bmcl.2016.09.065

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.

Keywords

AMPK; Allostery; CBM; CBS; Crystallography; Enzyme activators.

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