Inhibition of the T790M gatekeeper mutant of the epidermal growth factor receptor by EXEL-7647.

doi:10.1158/1078-0432.CCR-06-2590

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Article

Inhibition of the T790M gatekeeper mutant of the epidermal growth factor receptor by EXEL-7647.

Clinical cancer research : an official journal of the American Association for Cancer Research - 15 Jun 2007

Gendreau Steven B, Ventura Richard, Keast Paul, Laird A Douglas, Yakes F Michael, Zhang Wentao, Bentzien Frauke, Cancilla Belinda, Lutman Jeffery, Chu Felix, Jackman Lisa, Shi Yongchang, Yu Peiwen, Wang Jing, Aftab Dana T, Jaeger Christopher T, Meyer Stephanie M, De Costa Anushka, Engell Kelly, Chen Jason, Martini Jean-Francois, Joly Alison H

Abstract excerpt

PURPOSE: Agents inhibiting the epidermal growth factor receptor (EGFR) have shown clinical benefit in a subset of non-small cell lung cancer patients expressing amplified or mutationally activated EGFR. However, responsive patients can relapse as a result of selection for EGFR gene mutations that confer resistance to ATP competitive EGFR inhibitors, such as erlotinib and gefitinib. We describe here the activity...

Topics

Animals
Antineoplastic Agents
Apoptosis
Azabicyclo Compounds
Cell Line, Tumor
Cell Proliferation
Dose-Response Relationship, Drug
Drug Resistance, Neoplasm

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

ErbB Receptors

Erlotinib Hydrochloride

Female

Gefitinib

Humans

Immunohistochemistry

In Situ Nick-End Labeling

Mice

Mice, Nude

Mice, SCID

Source

Open in PubMed

Identifiers

PMID: 17575237
DOI: 10.1158/1078-0432.CCR-06-2590

Genes

EGFR
EGF

Variants

Provenance

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