Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen

While Ras is a promising target for cancer therapy, development of inhibitors targeting Ras signaling has proven challenging. Here, the authors report the discovery of Rasarfin, a small molecule from a phenotypic screen on G protein-coupled receptor (GPCR) endocytosis that acts as a dual Ras and ARF...

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Autores principales:	Jenna Giubilaro, Doris A. Schuetz, Tomasz M. Stepniewski, Yoon Namkung, Etienne Khoury, Mónica Lara-Márquez, Shirley Campbell, Alexandre Beautrait, Sylvain Armando, Olivier Radresa, Jean Duchaine, Nathalie Lamarche-Vane, Audrey Claing, Jana Selent, Michel Bouvier, Anne Marinier, Stéphane A. Laporte
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2021
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/ec44bf6899064e34b2049b207a9e9931
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spelling	oai:doaj.org-article:ec44bf6899064e34b2049b207a9e99312021-12-02T16:35:42ZDiscovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen10.1038/s41467-021-24968-y2041-1723https://doaj.org/article/ec44bf6899064e34b2049b207a9e99312021-08-01T00:00:00Zhttps://doi.org/10.1038/s41467-021-24968-yhttps://doaj.org/toc/2041-1723While Ras is a promising target for cancer therapy, development of inhibitors targeting Ras signaling has proven challenging. Here, the authors report the discovery of Rasarfin, a small molecule from a phenotypic screen on G protein-coupled receptor (GPCR) endocytosis that acts as a dual Ras and ARF6 inhibitor.Jenna GiubilaroDoris A. SchuetzTomasz M. StepniewskiYoon NamkungEtienne KhouryMónica Lara-MárquezShirley CampbellAlexandre BeautraitSylvain ArmandoOlivier RadresaJean DuchaineNathalie Lamarche-VaneAudrey ClaingJana SelentMichel BouvierAnne MarinierStéphane A. LaporteNature PortfolioarticleScienceQENNature Communications, Vol 12, Iss 1, Pp 1-16 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Jenna Giubilaro Doris A. Schuetz Tomasz M. Stepniewski Yoon Namkung Etienne Khoury Mónica Lara-Márquez Shirley Campbell Alexandre Beautrait Sylvain Armando Olivier Radresa Jean Duchaine Nathalie Lamarche-Vane Audrey Claing Jana Selent Michel Bouvier Anne Marinier Stéphane A. Laporte Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen
description	While Ras is a promising target for cancer therapy, development of inhibitors targeting Ras signaling has proven challenging. Here, the authors report the discovery of Rasarfin, a small molecule from a phenotypic screen on G protein-coupled receptor (GPCR) endocytosis that acts as a dual Ras and ARF6 inhibitor.
format	article
author	Jenna Giubilaro Doris A. Schuetz Tomasz M. Stepniewski Yoon Namkung Etienne Khoury Mónica Lara-Márquez Shirley Campbell Alexandre Beautrait Sylvain Armando Olivier Radresa Jean Duchaine Nathalie Lamarche-Vane Audrey Claing Jana Selent Michel Bouvier Anne Marinier Stéphane A. Laporte
author_facet	Jenna Giubilaro Doris A. Schuetz Tomasz M. Stepniewski Yoon Namkung Etienne Khoury Mónica Lara-Márquez Shirley Campbell Alexandre Beautrait Sylvain Armando Olivier Radresa Jean Duchaine Nathalie Lamarche-Vane Audrey Claing Jana Selent Michel Bouvier Anne Marinier Stéphane A. Laporte
author_sort	Jenna Giubilaro
title	Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen
title_short	Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen
title_full	Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen
title_fullStr	Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen
title_full_unstemmed	Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen
title_sort	discovery of a dual ras and arf6 inhibitor from a gpcr endocytosis screen
publisher	Nature Portfolio
publishDate	2021
url	https://doaj.org/article/ec44bf6899064e34b2049b207a9e9931
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Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen

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