Modulating multi-functional ERK complexes by covalent targeting of a recruitment site in vivo

The ERK signalling pathway is activated in many cancers, however ERK1 and ERK2 are difficult to target pharmacologically. Here, the authors identify a small molecule inhibitor that binds covalently to the D-recruitment site of ERK and induces cell death and reduces tumour growth in mice.

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Autores principales:	Tamer S. Kaoud, William H. Johnson, Nancy D. Ebelt, Andrea Piserchio, Diana Zamora-Olivares, Sabrina X. Van Ravenstein, Jacey R. Pridgen, Ramakrishna Edupuganti, Rachel Sammons, Micael Cano, Mangalika Warthaka, Matthew Harger, Clint D. J. Tavares, Jihyun Park, Mohamed F. Radwan, Pengyu Ren, Eric V. Anslyn, Kenneth Y. Tsai, Ranajeet Ghose, Kevin N. Dalby
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2019
Materias:	Science Q
Acceso en línea:	https://doaj.org/article/a5398760f41b41118e32f8afccdebe49
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spelling	oai:doaj.org-article:a5398760f41b41118e32f8afccdebe492021-12-02T14:38:47ZModulating multi-functional ERK complexes by covalent targeting of a recruitment site in vivo10.1038/s41467-019-12996-82041-1723https://doaj.org/article/a5398760f41b41118e32f8afccdebe492019-11-01T00:00:00Zhttps://doi.org/10.1038/s41467-019-12996-8https://doaj.org/toc/2041-1723The ERK signalling pathway is activated in many cancers, however ERK1 and ERK2 are difficult to target pharmacologically. Here, the authors identify a small molecule inhibitor that binds covalently to the D-recruitment site of ERK and induces cell death and reduces tumour growth in mice.Tamer S. KaoudWilliam H. JohnsonNancy D. EbeltAndrea PiserchioDiana Zamora-OlivaresSabrina X. Van RavensteinJacey R. PridgenRamakrishna EdupugantiRachel SammonsMicael CanoMangalika WarthakaMatthew HargerClint D. J. TavaresJihyun ParkMohamed F. RadwanPengyu RenEric V. AnslynKenneth Y. TsaiRanajeet GhoseKevin N. DalbyNature PortfolioarticleScienceQENNature Communications, Vol 10, Iss 1, Pp 1-15 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Science Q
spellingShingle	Science Q Tamer S. Kaoud William H. Johnson Nancy D. Ebelt Andrea Piserchio Diana Zamora-Olivares Sabrina X. Van Ravenstein Jacey R. Pridgen Ramakrishna Edupuganti Rachel Sammons Micael Cano Mangalika Warthaka Matthew Harger Clint D. J. Tavares Jihyun Park Mohamed F. Radwan Pengyu Ren Eric V. Anslyn Kenneth Y. Tsai Ranajeet Ghose Kevin N. Dalby Modulating multi-functional ERK complexes by covalent targeting of a recruitment site in vivo
description	The ERK signalling pathway is activated in many cancers, however ERK1 and ERK2 are difficult to target pharmacologically. Here, the authors identify a small molecule inhibitor that binds covalently to the D-recruitment site of ERK and induces cell death and reduces tumour growth in mice.
format	article
author	Tamer S. Kaoud William H. Johnson Nancy D. Ebelt Andrea Piserchio Diana Zamora-Olivares Sabrina X. Van Ravenstein Jacey R. Pridgen Ramakrishna Edupuganti Rachel Sammons Micael Cano Mangalika Warthaka Matthew Harger Clint D. J. Tavares Jihyun Park Mohamed F. Radwan Pengyu Ren Eric V. Anslyn Kenneth Y. Tsai Ranajeet Ghose Kevin N. Dalby
author_facet	Tamer S. Kaoud William H. Johnson Nancy D. Ebelt Andrea Piserchio Diana Zamora-Olivares Sabrina X. Van Ravenstein Jacey R. Pridgen Ramakrishna Edupuganti Rachel Sammons Micael Cano Mangalika Warthaka Matthew Harger Clint D. J. Tavares Jihyun Park Mohamed F. Radwan Pengyu Ren Eric V. Anslyn Kenneth Y. Tsai Ranajeet Ghose Kevin N. Dalby
author_sort	Tamer S. Kaoud
title	Modulating multi-functional ERK complexes by covalent targeting of a recruitment site in vivo
title_short	Modulating multi-functional ERK complexes by covalent targeting of a recruitment site in vivo
title_full	Modulating multi-functional ERK complexes by covalent targeting of a recruitment site in vivo
title_fullStr	Modulating multi-functional ERK complexes by covalent targeting of a recruitment site in vivo
title_full_unstemmed	Modulating multi-functional ERK complexes by covalent targeting of a recruitment site in vivo
title_sort	modulating multi-functional erk complexes by covalent targeting of a recruitment site in vivo
publisher	Nature Portfolio
publishDate	2019
url	https://doaj.org/article/a5398760f41b41118e32f8afccdebe49
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Modulating multi-functional ERK complexes by covalent targeting of a recruitment site in vivo

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