Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors

Selective ERK5 inhibitors target ERK5 kinase activity, but they do not phenocopy the effects of ERK5 genetic depletion. Here, the authors demonstrate that the direct interaction of these inhibitors to ERK5 kinase domain induces conformational changes that promote ERK5 nuclear translocation and trans...

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Autores principales:	Pamela A. Lochhead, Julie A. Tucker, Natalie J. Tatum, Jinhua Wang, David Oxley, Andrew M. Kidger, Victoria P. Johnson, Megan A. Cassidy, Nathanael S. Gray, Martin E. M. Noble, Simon J. Cook
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2020
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/74f91df61c624308a4815d6adcffb1f9
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spelling	oai:doaj.org-article:74f91df61c624308a4815d6adcffb1f92021-12-02T14:41:24ZParadoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors10.1038/s41467-020-15031-32041-1723https://doaj.org/article/74f91df61c624308a4815d6adcffb1f92020-03-01T00:00:00Zhttps://doi.org/10.1038/s41467-020-15031-3https://doaj.org/toc/2041-1723Selective ERK5 inhibitors target ERK5 kinase activity, but they do not phenocopy the effects of ERK5 genetic depletion. Here, the authors demonstrate that the direct interaction of these inhibitors to ERK5 kinase domain induces conformational changes that promote ERK5 nuclear translocation and transcriptional activities.Pamela A. LochheadJulie A. TuckerNatalie J. TatumJinhua WangDavid OxleyAndrew M. KidgerVictoria P. JohnsonMegan A. CassidyNathanael S. GrayMartin E. M. NobleSimon J. CookNature PortfolioarticleScienceQENNature Communications, Vol 11, Iss 1, Pp 1-16 (2020)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Pamela A. Lochhead Julie A. Tucker Natalie J. Tatum Jinhua Wang David Oxley Andrew M. Kidger Victoria P. Johnson Megan A. Cassidy Nathanael S. Gray Martin E. M. Noble Simon J. Cook Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors
description	Selective ERK5 inhibitors target ERK5 kinase activity, but they do not phenocopy the effects of ERK5 genetic depletion. Here, the authors demonstrate that the direct interaction of these inhibitors to ERK5 kinase domain induces conformational changes that promote ERK5 nuclear translocation and transcriptional activities.
format	article
author	Pamela A. Lochhead Julie A. Tucker Natalie J. Tatum Jinhua Wang David Oxley Andrew M. Kidger Victoria P. Johnson Megan A. Cassidy Nathanael S. Gray Martin E. M. Noble Simon J. Cook
author_facet	Pamela A. Lochhead Julie A. Tucker Natalie J. Tatum Jinhua Wang David Oxley Andrew M. Kidger Victoria P. Johnson Megan A. Cassidy Nathanael S. Gray Martin E. M. Noble Simon J. Cook
author_sort	Pamela A. Lochhead
title	Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors
title_short	Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors
title_full	Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors
title_fullStr	Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors
title_full_unstemmed	Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors
title_sort	paradoxical activation of the protein kinase-transcription factor erk5 by erk5 kinase inhibitors
publisher	Nature Portfolio
publishDate	2020
url	https://doaj.org/article/74f91df61c624308a4815d6adcffb1f9
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Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors

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