Fake Inhibitors: AMPK Activation Trumps Inhibition

Christopher G Langendorf; John W Scott; Bruce E Kemp

doi:10.1016/j.chembiol.2017.07.005

Fake Inhibitors: AMPK Activation Trumps Inhibition

Cell Chem Biol. 2017 Jul 20;24(7):775-777. doi: 10.1016/j.chembiol.2017.07.005.

Authors

Christopher G Langendorf¹, John W Scott¹, Bruce E Kemp²

Affiliations

¹ St Vincent's Institute of Medical Research, Fitzroy, VIC 3065, Australia.
² St Vincent's Institute of Medical Research, Fitzroy, VIC 3065, Australia. Electronic address: bkemp@svi.edu.au.

PMID: 28732195
DOI: 10.1016/j.chembiol.2017.07.005

Abstract

Protein kinase inhibitors have become increasingly important therapeutic drugs for the treatment of human diseases; however, resistance and off-target effects can limit their use. In this issue of Cell Chemical Biology, Ross et al. (2017) reveal a novel off-target mechanism where the Src kinase inhibitor SU6656 paradoxically primes AMPK for phosphorylation and activation by the upstream kinase LKB1.

Publication types

Comment

MeSH terms

AMP-Activated Protein Kinases / antagonists & inhibitors*
Cell Line
Enzyme Activation / drug effects
Enzyme Inhibitors
Humans
Multienzyme Complexes
Phosphorylation / drug effects
Protein Kinase Inhibitors
Protein Serine-Threonine Kinases / antagonists & inhibitors*
Signal Transduction

Substances

Enzyme Inhibitors
Multienzyme Complexes
Protein Kinase Inhibitors
Protein Serine-Threonine Kinases
AMP-Activated Protein Kinases