Article
Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors.
Nature communications - 13 Mar 2020
Lochhead Pamela A, Tucker Julie A, Tatum Natalie J, Wang Jinhua, Oxley David, Kidger Andrew M, Johnson Victoria P, Cassidy Megan A, Gray Nathanael S, Noble Martin E M, Cook Simon J
Abstract excerpt
The dual protein kinase-transcription factor, ERK5, is an emerging drug target in cancer and inflammation, and small-molecule ERK5 kinase inhibitors have been developed. However, selective ERK5 kinase inhibitors fail to recapitulate ERK5 genetic ablation phenotypes, suggesting kinase-independent functions for ERK5. Here we show that ERK5 kinase inhibitors cause paradoxical activation of ERK5 transcriptional...
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