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Small Molecule Drug A-769662 and AMP...
Journal article

Small Molecule Drug A-769662 and AMP Synergistically Activate Naive AMPK Independent of Upstream Kinase Signaling

Abstract

The AMP-activated protein kinase (AMPK) is a metabolic stress-sensing αβγ heterotrimer responsible for energy homeostasis, making it a therapeutic target for metabolic diseases such as type 2 diabetes and obesity. AMPK signaling is triggered by phosphorylation on the AMPK α subunit activation loop Thr172 by upstream kinases. Dephosphorylated, naive AMPK is thought to be catalytically inactive and insensitive to allosteric regulation by AMP and …

Authors

Scott JW; Ling N; Issa SMA; Dite TA; O’Brien MT; Chen Z-P; Galic S; Langendorf CG; Steinberg GR; Kemp BE

Journal

Cell Chemical Biology, Vol. 21, No. 5, pp. 619–627

Publisher

Elsevier

Publication Date

May 2014

DOI

10.1016/j.chembiol.2014.03.006

ISSN

2451-9456