Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention

Buparlisib/BKM120 is in phase 3 clinical trials as a phosphoinositide 3-kinase (PI3K) inhibitor. Here, Bohnackeret al. combine chemical biology and structural biology approaches to segregate BKM120’s biological actions, and suggest that it causes mitotic arrest predominantly by binding microtubules...

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Autores principales:	Thomas Bohnacker, Andrea E. Prota, Florent Beaufils, John E. Burke, Anna Melone, Alison J. Inglis, Denise Rageot, Alexander M. Sele, Vladimir Cmiljanovic, Natasa Cmiljanovic, Katja Bargsten, Amol Aher, Anna Akhmanova, J. Fernando Díaz, Doriano Fabbro, Marketa Zvelebil, Roger L. Williams, Michel O. Steinmetz, Matthias P. Wymann
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2017
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/a5212909a4a7490db4d79600c172c822
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spelling	oai:doaj.org-article:a5212909a4a7490db4d79600c172c8222021-12-02T14:42:34ZDeconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention10.1038/ncomms146832041-1723https://doaj.org/article/a5212909a4a7490db4d79600c172c8222017-03-01T00:00:00Zhttps://doi.org/10.1038/ncomms14683https://doaj.org/toc/2041-1723Buparlisib/BKM120 is in phase 3 clinical trials as a phosphoinositide 3-kinase (PI3K) inhibitor. Here, Bohnackeret al. combine chemical biology and structural biology approaches to segregate BKM120’s biological actions, and suggest that it causes mitotic arrest predominantly by binding microtubules and disrupting their dynamics.Thomas BohnackerAndrea E. ProtaFlorent BeaufilsJohn E. BurkeAnna MeloneAlison J. InglisDenise RageotAlexander M. SeleVladimir CmiljanovicNatasa CmiljanovicKatja BargstenAmol AherAnna AkhmanovaJ. Fernando DíazDoriano FabbroMarketa ZvelebilRoger L. WilliamsMichel O. SteinmetzMatthias P. WymannNature PortfolioarticleScienceQENNature Communications, Vol 8, Iss 1, Pp 1-13 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Thomas Bohnacker Andrea E. Prota Florent Beaufils John E. Burke Anna Melone Alison J. Inglis Denise Rageot Alexander M. Sele Vladimir Cmiljanovic Natasa Cmiljanovic Katja Bargsten Amol Aher Anna Akhmanova J. Fernando Díaz Doriano Fabbro Marketa Zvelebil Roger L. Williams Michel O. Steinmetz Matthias P. Wymann Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention
description	Buparlisib/BKM120 is in phase 3 clinical trials as a phosphoinositide 3-kinase (PI3K) inhibitor. Here, Bohnackeret al. combine chemical biology and structural biology approaches to segregate BKM120’s biological actions, and suggest that it causes mitotic arrest predominantly by binding microtubules and disrupting their dynamics.
format	article
author	Thomas Bohnacker Andrea E. Prota Florent Beaufils John E. Burke Anna Melone Alison J. Inglis Denise Rageot Alexander M. Sele Vladimir Cmiljanovic Natasa Cmiljanovic Katja Bargsten Amol Aher Anna Akhmanova J. Fernando Díaz Doriano Fabbro Marketa Zvelebil Roger L. Williams Michel O. Steinmetz Matthias P. Wymann
author_facet	Thomas Bohnacker Andrea E. Prota Florent Beaufils John E. Burke Anna Melone Alison J. Inglis Denise Rageot Alexander M. Sele Vladimir Cmiljanovic Natasa Cmiljanovic Katja Bargsten Amol Aher Anna Akhmanova J. Fernando Díaz Doriano Fabbro Marketa Zvelebil Roger L. Williams Michel O. Steinmetz Matthias P. Wymann
author_sort	Thomas Bohnacker
title	Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention
title_short	Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention
title_full	Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention
title_fullStr	Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention
title_full_unstemmed	Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention
title_sort	deconvolution of buparlisib’s mechanism of action defines specific pi3k and tubulin inhibitors for therapeutic intervention
publisher	Nature Portfolio
publishDate	2017
url	https://doaj.org/article/a5212909a4a7490db4d79600c172c822
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Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention

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