EGFR T790M: revealing the secrets of a gatekeeper

Brian Ko, Daniel Paucar, Balazs Halmos Department of Oncology, Montefiore Medical Center, Albert Einstein College of Medicine, New York, NY, USA Abstract: Non-small-cell lung cancers that harbor activating mutations in the EGFR gene represent an important molecularly defined subset...

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Autores principales:	Ko B, Paucar D, Halmos B
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2017
Materias:	lung cancer epidermal growth factor receptor T790M targeted therapy resistance Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
Acceso en línea:	https://doaj.org/article/3a360430f7c248bd9678fc8417144304
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spelling	oai:doaj.org-article:3a360430f7c248bd9678fc84171443042021-12-02T00:58:15ZEGFR T790M: revealing the secrets of a gatekeeper1179-2728https://doaj.org/article/3a360430f7c248bd9678fc84171443042017-10-01T00:00:00Zhttps://www.dovepress.com/egfr-t790m-revealing-the-secrets-of-a-gatekeeper-peer-reviewed-article-LCTThttps://doaj.org/toc/1179-2728Brian Ko, Daniel Paucar, Balazs Halmos Department of Oncology, Montefiore Medical Center, Albert Einstein College of Medicine, New York, NY, USA Abstract: Non-small-cell lung cancers that harbor activating mutations in the EGFR gene represent an important molecularly defined subset of lung cancer. Despite dramatic initial responses with first- and second-generation EGFR-directed tyrosine-kinase inhibitors (TKIs) against these cancers, the development of a dominant and frequent resistance mechanism through a threonine–methionine amino acid substitution at position 790 (T790M) of EGFR has limited the long-term efficacy of these targeted therapies. This “gatekeeper” EGFR T790M alteration remains the only validated and relevant second-site resistance mutation for EGFR, allowing for focused research to understand and overcome EGFR T790M-mediated resistance. The current review focuses on EGFR T790M by discussing mechanisms of resistance mediated by EGFR T790M, reviewing development of novel third-generation EGFR TKIs targeting EGFR T790M, and highlighting current research on overcoming resistance to third-generation EGFR T790M TKIs. Keywords: lung cancer, epidermal growth factor receptor, T790M, targeted therapy, resistanceKo BPaucar DHalmos BDove Medical Pressarticlelung cancerepidermal growth factor receptorT790Mtargeted therapyresistanceNeoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENLung Cancer: Targets and Therapy, Vol Volume 8, Pp 147-159 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	lung cancer epidermal growth factor receptor T790M targeted therapy resistance Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
spellingShingle	lung cancer epidermal growth factor receptor T790M targeted therapy resistance Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 Ko B Paucar D Halmos B EGFR T790M: revealing the secrets of a gatekeeper
description	Brian Ko, Daniel Paucar, Balazs Halmos Department of Oncology, Montefiore Medical Center, Albert Einstein College of Medicine, New York, NY, USA Abstract: Non-small-cell lung cancers that harbor activating mutations in the EGFR gene represent an important molecularly defined subset of lung cancer. Despite dramatic initial responses with first- and second-generation EGFR-directed tyrosine-kinase inhibitors (TKIs) against these cancers, the development of a dominant and frequent resistance mechanism through a threonine–methionine amino acid substitution at position 790 (T790M) of EGFR has limited the long-term efficacy of these targeted therapies. This “gatekeeper” EGFR T790M alteration remains the only validated and relevant second-site resistance mutation for EGFR, allowing for focused research to understand and overcome EGFR T790M-mediated resistance. The current review focuses on EGFR T790M by discussing mechanisms of resistance mediated by EGFR T790M, reviewing development of novel third-generation EGFR TKIs targeting EGFR T790M, and highlighting current research on overcoming resistance to third-generation EGFR T790M TKIs. Keywords: lung cancer, epidermal growth factor receptor, T790M, targeted therapy, resistance
format	article
author	Ko B Paucar D Halmos B
author_facet	Ko B Paucar D Halmos B
author_sort	Ko B
title	EGFR T790M: revealing the secrets of a gatekeeper
title_short	EGFR T790M: revealing the secrets of a gatekeeper
title_full	EGFR T790M: revealing the secrets of a gatekeeper
title_fullStr	EGFR T790M: revealing the secrets of a gatekeeper
title_full_unstemmed	EGFR T790M: revealing the secrets of a gatekeeper
title_sort	egfr t790m: revealing the secrets of a gatekeeper
publisher	Dove Medical Press
publishDate	2017
url	https://doaj.org/article/3a360430f7c248bd9678fc8417144304
work_keys_str_mv	AT kob egfrt790mrevealingthesecretsofagatekeeper AT paucard egfrt790mrevealingthesecretsofagatekeeper AT halmosb egfrt790mrevealingthesecretsofagatekeeper
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EGFR T790M: revealing the secrets of a gatekeeper

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