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Updated: Mar 13, 2026

Identification of Kinase-substrate Pairs Using High Throughput Screening
Published on: August 29, 2015
Recent progress in the identification of adenosine monophosphate-activated protein kinase (AMPK) activators
Kimberly O Cameron1, Ravi G Kurumbail2
1Pfizer Global Research and Development, Cardiovascular and Metabolic Diseases Chemistry, 610 Main Street, Cambridge, MA 02139, USA.
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.
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