Cited by 192Lung Cancer Treatments and MutationsHER2/EGFR in Cancer ResearchProtein Kinase Regulation and GTPase Signaling

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Epidermal Growth Factor Receptor Mutants from Human Lung Cancers Exhibit Enhanced Catalytic Activity and Increased Sensitivity to Gefitinib

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Mulloy, Roseann, Ferrand, Audrey, Kim, Youngjoo, Sordella, Raffaella, Bell, Daphne W., Haber, Daniel A., Anderson, Karen S., Settleman, Jeffrey·2007·Cancer Research

DOI 10.1158/0008-5472.can-06-4293

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Abstract

Somatic mutations within the epidermal growth factor receptor (EGFR) kinase domain are detected in 10% to 30% of human non–small cell lung cancers and are correlated with striking clinical responses in a subset of patients treated with EGFR kinase inhibitors, such as gefitinib and erlotinib. Cell-based studies suggest that these mutant EGFRs promote increased autophosphorylating activity on a subset of EGFR COOH-terminal tyrosines and the consequent engagement of a subset of downstream effectors. Because EGFR function is regulated at multiple levels in vivo, and it is therefore difficult to assess the direct consequences of these mutations on EGFR enzyme function, we measured EGFR catalytic activity in in vitro kinase assays using purified recombinant proteins corresponding to the cytoplasmic domain of wild-type and two frequently detected EGFR mutants (DelL747-P753insS and L858R). Both mutants exhibit substantially increased autophosphorylating activity relative to wild-type EGFR, and they exhibit distinct reaction kinetics. In addition, the mutant kinases are more sensitive to kinase inhibition by gefitinib, which seems to reflect their increased drug affinity. These findings suggest that the altered signaling properties and drug sensitivity of these EGFR mutants that have been observed in vivo largely result from differences in the catalytic properties of the kinase. In addition, we find that the T790M secondary “drug resistance mutation” of EGFR, which frequently arises in relapsed patients that initially responded to treatment, confers enhanced kinase activity to primary activating EGFR alleles and may, therefore, be oncogenic in some contexts. [Cancer Res 2007;67(5):2325–30]

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Authors: Mulloy, R., Ferrand, A., Kim, Y., Sordella, R., Bell, D. W., Haber, D. A., Anderson, K. S., & Settleman, J.
Affiliations: Harvard University (US)
2Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut
Yale University (US)
ORCID: Ferrand, Audrey
Sordella, Raffaella
Bell, Daphne W.
Haber, Daniel A.
Anderson, Karen S.
Settleman, Jeffrey
Venue: Cancer Research
Publisher: American Association for Cancer Research (AACR)
Published: 2007-03-01
Volume: 67
Issue: 5
Pages: 2325-2330
ISSN: 0008-5472 (ISSN-L)
1538-7445
DOI: 10.1158/0008-5472.can-06-4293
OpenAlex: W2129787264
Cited by: 192
References: 21
Citations by year: 2026: 1 · 2025: 4 · 2024: 3 · 2023: 4 · 2022: 3 · 2021: 7 · 2020: 4 · 2019: 3 · 2018: 10 · 2017: 11 · 2016: 9 · 2015: 13 · 2014: 16 · 2013: 15 · 2012: 15
FWCI: 16.13
Type: journal article
Language: en
Open access: bronze
doi.org
Locations: Cancer Research (publishedVersion)
PubMed (publishedVersion)
Cold Spring Harbor Laboratory Institutional Repository (Cold Spring Harbor Laboratory) (acceptedVersion)
Funders: V Foundation for Cancer Research
National Institutes of Health
National Cancer Institute (R01CA115830)
National Institute of General Medical Sciences (R01-GM71805)
Topics: Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
Health Sciences › Medicine › Oncology › HER2/EGFR in Cancer Research
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
Keywords: epidermal growth factor receptor, EGFR mutation, non-small cell lung cancer, gefitinib, erlotinib, kinase activity, autophosphorylation, L858R mutation, T790M mutation, drug resistance, kinase inhibitor sensitivity, oncogenicity
MeSH terms: Gefitinib, Animals, Antineoplastic Agents, Catalysis, Cells, Cultured, Humans, Lung Neoplasms, Phosphotransferases, Quinazolines, Substrate Specificity, Baculoviridae, Spodoptera, Drug Resistance, Neoplasm, Mutant Proteins, ErbB Receptors

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Epidermal Growth Factor Receptor Mutants from Human Lung Cancers Exhibit Enhanced Catalytic Activity and Increased Sensitivity to Gefitinib

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