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Fake Inhibitors: AMPK Activation Trumps Inhibition.

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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… Click to show full 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.

Keywords: inhibitors ampk; ampk activation; biology; fake inhibitors; activation; activation trumps

Journal Title: Cell chemical biology
Year Published: 2017

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