Inhibitors of BRAF dimers using an allosteric site

FDA-approved RAF inhibitors poorly inhibit BRAF dimers, which limits their clinical efficacy in tumors expressing BRAFV600E mutant monomers. Here the authors identify FDA-approved Ponatinib as an effective inhibitor of BRAF monomers and dimers and designed PHI1, an inhibitor with a unique mode of ac...

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Autores principales:	Xiomaris M. Cotto-Rios, Bogos Agianian, Nadege Gitego, Emmanouil Zacharioudakis, Orsi Giricz, Yang Wu, Yiyu Zou, Amit Verma, Poulikos I. Poulikakos, Evripidis Gavathiotis
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2020
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/164ffa3380c14391b97d067789d509e0
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spelling	oai:doaj.org-article:164ffa3380c14391b97d067789d509e02021-12-02T15:25:37ZInhibitors of BRAF dimers using an allosteric site10.1038/s41467-020-18123-22041-1723https://doaj.org/article/164ffa3380c14391b97d067789d509e02020-09-01T00:00:00Zhttps://doi.org/10.1038/s41467-020-18123-2https://doaj.org/toc/2041-1723FDA-approved RAF inhibitors poorly inhibit BRAF dimers, which limits their clinical efficacy in tumors expressing BRAFV600E mutant monomers. Here the authors identify FDA-approved Ponatinib as an effective inhibitor of BRAF monomers and dimers and designed PHI1, an inhibitor with a unique mode of action and selectivity for oncogenic BRAF dimers.Xiomaris M. Cotto-RiosBogos AgianianNadege GitegoEmmanouil ZacharioudakisOrsi GiriczYang WuYiyu ZouAmit VermaPoulikos I. PoulikakosEvripidis GavathiotisNature PortfolioarticleScienceQENNature Communications, Vol 11, Iss 1, Pp 1-16 (2020)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Xiomaris M. Cotto-Rios Bogos Agianian Nadege Gitego Emmanouil Zacharioudakis Orsi Giricz Yang Wu Yiyu Zou Amit Verma Poulikos I. Poulikakos Evripidis Gavathiotis Inhibitors of BRAF dimers using an allosteric site
description	FDA-approved RAF inhibitors poorly inhibit BRAF dimers, which limits their clinical efficacy in tumors expressing BRAFV600E mutant monomers. Here the authors identify FDA-approved Ponatinib as an effective inhibitor of BRAF monomers and dimers and designed PHI1, an inhibitor with a unique mode of action and selectivity for oncogenic BRAF dimers.
format	article
author	Xiomaris M. Cotto-Rios Bogos Agianian Nadege Gitego Emmanouil Zacharioudakis Orsi Giricz Yang Wu Yiyu Zou Amit Verma Poulikos I. Poulikakos Evripidis Gavathiotis
author_facet	Xiomaris M. Cotto-Rios Bogos Agianian Nadege Gitego Emmanouil Zacharioudakis Orsi Giricz Yang Wu Yiyu Zou Amit Verma Poulikos I. Poulikakos Evripidis Gavathiotis
author_sort	Xiomaris M. Cotto-Rios
title	Inhibitors of BRAF dimers using an allosteric site
title_short	Inhibitors of BRAF dimers using an allosteric site
title_full	Inhibitors of BRAF dimers using an allosteric site
title_fullStr	Inhibitors of BRAF dimers using an allosteric site
title_full_unstemmed	Inhibitors of BRAF dimers using an allosteric site
title_sort	inhibitors of braf dimers using an allosteric site
publisher	Nature Portfolio
publishDate	2020
url	https://doaj.org/article/164ffa3380c14391b97d067789d509e0
work_keys_str_mv	AT xiomarismcottorios inhibitorsofbrafdimersusinganallostericsite AT bogosagianian inhibitorsofbrafdimersusinganallostericsite AT nadegegitego inhibitorsofbrafdimersusinganallostericsite AT emmanouilzacharioudakis inhibitorsofbrafdimersusinganallostericsite AT orsigiricz inhibitorsofbrafdimersusinganallostericsite AT yangwu inhibitorsofbrafdimersusinganallostericsite AT yiyuzou inhibitorsofbrafdimersusinganallostericsite AT amitverma inhibitorsofbrafdimersusinganallostericsite AT poulikosipoulikakos inhibitorsofbrafdimersusinganallostericsite AT evripidisgavathiotis inhibitorsofbrafdimersusinganallostericsite
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Inhibitors of BRAF dimers using an allosteric site

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