The L730V/I RET roof mutations display different activities toward pralsetinib and selpercatinib

Abstract Recently Food and Drug Administration (FDA)-approved pralsetinib (BLU-667) and selpercatinib (LOXO-292) are RET-selective protein tyrosine kinase inhibitors for treating RET-altered cancers, but whether they have distinct activity was unknown. The L730V/I mutations at the roof of the solven...

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Autores principales:	Tao Shen, Xueqing Hu, Xuan Liu, Vivek Subbiah, Blaine H. M. Mooers, Jie Wu
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2021
Materias:	Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
Acceso en línea:	https://doaj.org/article/a56a59cbb9894e42849b0e49e6d4e170
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spelling	oai:doaj.org-article:a56a59cbb9894e42849b0e49e6d4e1702021-12-02T15:02:49ZThe L730V/I RET roof mutations display different activities toward pralsetinib and selpercatinib10.1038/s41698-021-00188-x2397-768Xhttps://doaj.org/article/a56a59cbb9894e42849b0e49e6d4e1702021-06-01T00:00:00Zhttps://doi.org/10.1038/s41698-021-00188-xhttps://doaj.org/toc/2397-768XAbstract Recently Food and Drug Administration (FDA)-approved pralsetinib (BLU-667) and selpercatinib (LOXO-292) are RET-selective protein tyrosine kinase inhibitors for treating RET-altered cancers, but whether they have distinct activity was unknown. The L730V/I mutations at the roof of the solvent-front site of the RET kinase were identified as strongly resistant to pralsetinib but not to selpercatinib. Selpercatinib effectively inhibited these mutants and the KIF5B-RET(L730V/I) oncogene-driven tumors.Tao ShenXueqing HuXuan LiuVivek SubbiahBlaine H. M. MooersJie WuNature PortfolioarticleNeoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENnpj Precision Oncology, Vol 5, Iss 1, Pp 1-4 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
spellingShingle	Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 Tao Shen Xueqing Hu Xuan Liu Vivek Subbiah Blaine H. M. Mooers Jie Wu The L730V/I RET roof mutations display different activities toward pralsetinib and selpercatinib
description	Abstract Recently Food and Drug Administration (FDA)-approved pralsetinib (BLU-667) and selpercatinib (LOXO-292) are RET-selective protein tyrosine kinase inhibitors for treating RET-altered cancers, but whether they have distinct activity was unknown. The L730V/I mutations at the roof of the solvent-front site of the RET kinase were identified as strongly resistant to pralsetinib but not to selpercatinib. Selpercatinib effectively inhibited these mutants and the KIF5B-RET(L730V/I) oncogene-driven tumors.
format	article
author	Tao Shen Xueqing Hu Xuan Liu Vivek Subbiah Blaine H. M. Mooers Jie Wu
author_facet	Tao Shen Xueqing Hu Xuan Liu Vivek Subbiah Blaine H. M. Mooers Jie Wu
author_sort	Tao Shen
title	The L730V/I RET roof mutations display different activities toward pralsetinib and selpercatinib
title_short	The L730V/I RET roof mutations display different activities toward pralsetinib and selpercatinib
title_full	The L730V/I RET roof mutations display different activities toward pralsetinib and selpercatinib
title_fullStr	The L730V/I RET roof mutations display different activities toward pralsetinib and selpercatinib
title_full_unstemmed	The L730V/I RET roof mutations display different activities toward pralsetinib and selpercatinib
title_sort	l730v/i ret roof mutations display different activities toward pralsetinib and selpercatinib
publisher	Nature Portfolio
publishDate	2021
url	https://doaj.org/article/a56a59cbb9894e42849b0e49e6d4e170
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The L730V/I RET roof mutations display different activities toward pralsetinib and selpercatinib

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