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

The DOI matches its Crossref record; 21 of the 21 references it cites were found in a registry or an index.

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

Open access

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

Published version of a preprint

Open this paper in CoChat — free account Open PDF

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]

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Integrity signals

Registry

Crossref · 10.1158/0008-5472.can-06-4293

Cites

21 of 21 references verified0 citation errors · 0 not checkable

Statistics

Claims the paper makes

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

Self-check

Percentages, sums and reported differences re-computed from the paper’s own numbers.

The self-check needs the paper’s full text.

Activating Mutations in the Epidermal Growth Factor Receptor Underlying Responsiveness of Non–Small-Cell Lung Cancer to Gefitinib
Lynch, T. J., Bell, D. W., Sordella, R., Gurubhagavatula, S., Okimoto, R. A., Brannigan, B. W., Harris, P. L., Haserlat, S. M., Supko, J. G., Haluska, F. G., et al. (2004) · New England Journal of Medicine · doi:10.1056/nejmoa040938 · Cited by 11,486
Self-citation
EGFR Mutations in Lung Cancer: Correlation with Clinical Response to Gefitinib Therapy
Paez, J. G., Jänne, P. A., Lee, J. C., Tracy, S., Greulich, H., Gabriel, S., Herman, P., Kaye, F. J., Lindeman, N., Boggon, T. J., et al. (2004) · Science · doi:10.1126/science.1099314 · Cited by 9,368
Cell Signaling by Receptor Tyrosine Kinases
Lemmon, M. A., & Schlessinger, J. (2010) · Cell · doi:10.1016/j.cell.2010.06.011 · Cited by 7,929
EGF receptor gene mutations are common in lung cancers from “never smokers” and are associated with sensitivity of tumors to gefitinib and erlotinib
Pao, W., Miller, V., Zakowski, M., Doherty, J., Politi, K., Sarkaria, I., Singh, B., Heelan, R., Rusch, V., Fulton, L., et al. (2004) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0405220101 · Cited by 4,338
EGFR Mutation and Resistance of Non–Small-Cell Lung Cancer to Gefitinib
Kobayashi, S., Boggon, T. J., Dayaram, T., Jänne, P. A., Kocher, O., Meyerson, M., Johnson, B. E., Eck, M. J., Tenen, D. G., & Halmos, B. (2005) · New England Journal of Medicine · doi:10.1056/nejmoa044238 · Cited by 3,964
Cell Signaling by Receptor Tyrosine Kinases
Schlessinger, J. (2000) · Cell · doi:10.1016/s0092-8674(00)00114-8 · Cited by 3,774
Acquired Resistance of Lung Adenocarcinomas to Gefitinib or Erlotinib Is Associated with a Second Mutation in the EGFR Kinase Domain
Pao, W., Miller, V. A., Politi, K. A., Riely, G. J., Somwar, R., Zakowski, M. F., Kris, M. G., & Varmus, H. (2005) · PLoS Medicine · doi:10.1371/journal.pmed.0020073 · Cited by 3,527
A small molecule–kinase interaction map for clinical kinase inhibitors
Fabian, M. A., Biggs, W., Treiber, D. K., Atteridge, C. E., Azimioara, M. D., Benedetti, M. G., Carter, T. A., Ciceri, P., Edeen, P. T., Floyd, M. B., et al. (2005) · Nature Biotechnology · doi:10.1038/nbt1068 · Cited by 1,923
Gefitinib-Sensitizing EGFR Mutations in Lung Cancer Activate Anti-Apoptotic Pathways
Sordella, R., Bell, D. W., Haber, D. A., & Settleman, J. E. (2004) · Science · doi:10.1126/science.1101637 · Cited by 1,605
Self-citation
Epidermal growth factor receptor: Mechanisms of activation and signalling
Jorissen, R. (2003) · Experimental Cell Research · doi:10.1016/s0014-4827(02)00098-8 · Cited by 1,565

Show all 21 references

Sorted by citations

Items 101–192 of 192

Epidermal growth factor receptor and mammalian target of rapamycin as therapeutic targets in malignant glioma: current clinical status and perspectives
Ronellenfitsch, M. W., Steinbach, J. P., & Wick, W. (2010) · Targeted Oncology · doi:10.1007/s11523-010-0154-5 · Cited by 28
Imaging of human epidermal growth factor receptors for patient selection and response monitoring – From PET imaging and beyond
Pereira, P. M. R., Abma, L., Henry, K. E., & Lewis, J. S. (2018) · Cancer Letters · doi:10.1016/j.canlet.2018.01.052 · Cited by 26
Secondary Resistant Mutations to Small Molecule Inhibitors in Cancer Cells
Hamid, A. B., & Petreaca, R. C. (2020) · Cancers · doi:10.3390/cancers12040927 · Cited by 29
Akt kinase-interacting protein1, a novel therapeutic target for lung cancer with EGFR-activating and gatekeeper mutations
Yamada, T., Takeuchi, S., Fujita, N., Nakamura, A., Wang, W., Li, Q., Oda, M., Mitsudomi, T., Yatabe, Y., Sekido, Y., et al. (2012) · Oncogene · doi:10.1038/onc.2012.446 · Cited by 26
Role of Network Branching in Eliciting Differential Short‐Term Signaling Responses in the Hypersensitive Epidermal Growth Factor Receptor Mutants Implicated in Lung Cancer
Purvis, J. E., Ilango, V., & Radhakrishnan, R. (2008) · Biotechnology Progress · doi:10.1021/bp070405o · Cited by 26
Nexus of signaling and endocytosis in oncogenesis driven by non-small cell lung cancer-associated epidermal growth factor receptor mutants
Chung, B. M. (2014) · World Journal of Clinical Oncology · doi:10.5306/wjco.v5.i5.806 · Cited by 25
Functional analysis of cancer-associated EGFR mutants using a cellular assay with YFP-tagged EGFR intracellular domain
de Gunst, M. M., Gallegos-Ruiz, M. I., Giaccone, G., & Rodríguez, J. A. (2007) · Molecular Cancer · doi:10.1186/1476-4598-6-56 · Cited by 24
Evaluation of Three Small Molecular Drugs for Targeted Therapy to Treat Nonsmall Cell Lung Cancer
Ni, J., & Zhang, L. (2016) · Chinese Medical Journal · doi:10.4103/0366-6999.174484 · Cited by 24
Tumor Cell Killing Mechanisms of Epidermal Growth Factor Receptor (EGFR) Antibodies Are Not Affected by Lung Cancer-Associated EGFR Kinase Mutations
Peipp, M., Schneider‐Merck, T., Dechant, M., Beyer, T. D., van Bueren, J. J. L., Bleeker, W. K., Parren, P. W. H. I., van de Winkel, J. G. J., & Valerius, T. (2008) · The Journal of Immunology · doi:10.4049/jimmunol.180.6.4338 · Cited by 24
Ligand-independent phosphorylation of Y869 (Y845) links mutant EGFR signaling to stat-mediated gene expression
Yang, S., Park, K., Turkson, J., & Arteaga, C. L. (2007) · Experimental Cell Research · doi:10.1016/j.yexcr.2007.09.002 · Cited by 23
Analysis of Somatic Mutations in Cancer: Molecular Mechanisms of Activation in the ErbB Family of Receptor Tyrosine Kinases
Shih, A., Telesco, S., & Radhakrishnan, R. (2011) · Cancers · doi:10.3390/cancers3011195 · Cited by 23
Correlation Between 18F-Fluorodeoxyglucose Uptake and Epidermal Growth Factor Receptor Mutations in Advanced Lung Cancer
Choi, Y., Cho, B. C., Jeong, Y. H., Seo, H. J., Kim, H. J., Cho, A. E.-H., Lee, J., Yun, M., Jeon, T. J., Lee, J. D., et al. (2012) · Nuclear Medicine and Molecular Imaging · doi:10.1007/s13139-012-0142-z · Cited by 22
Differential Effects of Tyrosine Kinase Inhibitors on Normal and Oncogenic EGFR Signaling and Downstream Effectors
Kim, Y., Apetri, M. M., Luo, B.-B., Settleman, J., & Anderson, K. (2015) · Molecular Cancer Research · doi:10.1158/1541-7786.mcr-14-0326 · Cited by 25
Self-citation
Targeted next-generation sequencing for analyzing the genetic alterations in atypical adenomatous hyperplasia and adenocarcinoma in situ
Xu, X., Li, N., Zhao, R., Zhu, L., Shao, J., & Zhang, J. (2017) · Journal of Cancer Research and Clinical Oncology · doi:10.1007/s00432-017-2500-9 · Cited by 22
EGFR tyrosine kinase inhibitors and multidrug resistance: perspectives
Nicola, A. C. (2010) · Frontiers in bioscience · doi:10.2741/3823 · Cited by 21
Carboxyamidotriazole Synergizes with Sorafenib to Combat Non–Small Cell Lung Cancer through Inhibition of NANOG and Aggravation of Apoptosis
Chen, C., Jü, R., Shi, J., Chen, W., Sun, F., Zhu, L., Li, J., Zhang, D., Ye, C., & Guo, L. (2017) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.117.240986 · Cited by 21
Molecular determinants of response to matuzumab in combination with paclitaxel for patients with advanced non-small cell lung cancer
Schittenhelm, M. M., Kollmannsberger, C., Oechsle, K., Harlow, A., Morich, J. R., Honecker, F. U., Kurek, R., Störkel, S., Kanz, L., Corless, C. L., et al. (2009) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-08-1068 · Cited by 20
Aucklandia lappa DC. extract enhances gefitinib efficacy in gefitinib-resistance secondary epidermal growth factor receptor mutations
Huang, G. J., Tong, Y., He, Q., Wang, J., & Chen, Z. (2017) · Journal of Ethnopharmacology · doi:10.1016/j.jep.2017.06.011 · Cited by 18
Inducible EGFR T790M-Mediated Gefitinib Resistance in Non-small Cell Lung Cancer Cells Does Not Modulate Sensitivity to PI103 Provoked Autophagy
Moreira-Leite, F. F., Harrison, L., Mironov, A., Roberts, R. A., & Dive, C. (2010) · Journal of Thoracic Oncology · doi:10.1097/jto.0b013e3181d95d93 · Cited by 17
A digital PCR assay development to detect EGFR T790M mutation in NSCLC patients
Zhou, R., Cai, Y., Li, Z., Shen, S., Sha, M., Head, S. R., & Wang, Y. (2018) · Frontiers in Laboratory Medicine · doi:10.1016/j.flm.2018.08.002 · Cited by 17
Treatment sequences in EGFR mutant advanced NSCLC
Wespiser, M., Swalduz, A., & Pérol, M. (2024) · Lung Cancer · doi:10.1016/j.lungcan.2024.107895 · Cited by 16
Epidermal Growth Factor Receptor P753S Mutation in Cutaneous Squamous Cell Carcinoma Responsive to Cetuximab-Based Therapy
Ganesan, P., Ali, S. M., Wang, K., Blumenschein, G. R., Esmaeli, B., Wolff, R. A., Miller, V. A., Stephens, P. J., Ross, J. S., Palmer, G. A., et al. (2014) · Journal of Clinical Oncology · doi:10.1200/jco.2013.50.3516 · Cited by 16
EGFR T790M Mutation in TKI-Naïve Clinical Samples: Frequency, Tissue Mosaicism, Predictive Value and Awareness on Artifacts
Lavdovskaia, E. D., Iyevleva, A. G., Соколенко, А. П., Mitiushkina, N. V., Преображенская, Е. В., Tiurin, V. I., Ivantsov, A. O., Валерьевич, Б. И., Stelmakh, L. V., Moiseenko, F. V., et al. (2018) · Oncology Research and Treatment · doi:10.1159/000491441 · Cited by 17
Comparison of the Efficacy of Gefitinib in Patients with Non-Small Cell Lung Cancer according to the Type of Epidermal Growth Factor Receptor Mutation
Igawa, S., Kasajima, M., Ishihara, M., Kimura, M., Hiyoshi, Y., Asakuma, M., Otani, S., Katono, K., Sasaki, J., & Masuda, N. (2014) · Oncology · doi:10.1159/000362603 · Cited by 14
Molecular modeling of ErbB4/HER4 kinase in the context of the HER4 signaling network helps rationalize the effects of clinically identified HER4 somatic mutations on the cell phenotype
Telesco, S., Vadigepalli, R., & Radhakrishnan, R. (2013) · Biotechnology Journal · doi:10.1002/biot.201300022 · Cited by 14
Combined inhibition of rho-associated protein kinase and EGFR suppresses the invasive phenotype in EGFR-dependent lung cancer cells
Umelo, I. A., Wever, O. D., Kronenberger, P., Noor, A., Teugels, E., Chen, G., Bracke, M., & Grève, J. D. (2015) · Lung Cancer · doi:10.1016/j.lungcan.2015.08.008 · Cited by 13
Highly Sensitive Droplet Digital PCR Method for Detection of de novo EGFR T790M Mutation in Patients with Non-Small Cell Lung Cancer
Wang, X., Li, X., Guo, H., Zhu, L., Peng, Z., Wang, J., Yang, F., & Guo, Y. S. (2020) · OncoTargets and Therapy · doi:10.2147/ott.s267677 · Cited by 13
Postoperative survival of EGFR-TKI-targeted therapy in non-small cell lung cancer patients with EGFR 19 or 21 mutations: a retrospective study
Yang, W., Gao, Y., Li, X., Zhang, J., Liu, T., Feng, X., Pan, H., Yang, X., Xie, S., Feng, X., et al. (2017) · World Journal of Surgical Oncology · doi:10.1186/s12957-017-1251-z · Cited by 13
Molecular Basis of Drug Resistance: Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors and Anaplastic Lymphoma Kinase Inhibitors
Yang, S. H. (2013) · Tuberculosis & respiratory diseases · doi:10.4046/trd.2013.75.5.188 · Cited by 11
Epidermal growth factor receptor mutation in combination with expression of MIG6 alters gefitinib sensitivity
Naruo, Y., Nagashima, T., Ushikoshi‐Nakayama, R., Saeki, Y., Nakakuki, T., Naka, T., Tanaka, H., Tsai, S., & Okada, M. (2011) · BMC Systems Biology · doi:10.1186/1752-0509-5-29 · Cited by 10
Investigating mutation-specific biological activities of small molecules using quantitative structure-activity relationship for epidermal growth factor receptor in cancer
Anoosha, P., Sakthivel, R., & Gromiha, M. M. (2017) · Mutation research. Fundamental and molecular mechanisms of mutagenesis · doi:10.1016/j.mrfmmm.2017.08.003 · Cited by 10
Mechanistic Study of Potent Fluorinated EGFR Kinase Inhibitors with a Quinazoline Scaffold against L858R/T790M/C797S Resistance Mutation: Unveiling the Fluorine Substituent Cooperativity Effect on the Inhibitory Activity
Akher, F. B., Farrokhzadeh, A., Ravenscroft, N., & Kuttel, M. M. (2020) · The Journal of Physical Chemistry B · doi:10.1021/acs.jpcb.0c03440 · Cited by 11
Structural Systems Biology and Multiscale Signaling Models
Telesco, S., & Radhakrishnan, R. (2012) · Annals of Biomedical Engineering · doi:10.1007/s10439-012-0576-6 · Cited by 9
Major Clinical Response to Afatinib Monotherapy in Lung Adenocarcinoma Harboring EGFR Exon 20 Insertion Mutation
Urbán, L., Dóczi, R., Vodicska, B., Tihanyi, D., Horváth, M., Kormos, D., Takács, I., Pápai-Székely, Z., Póka-Farkas, Z., Várkondi, E., et al. (2020) · Clinical Lung Cancer · doi:10.1016/j.cllc.2020.09.005 · Cited by 10
Computational studies of anaplastic lymphoma kinase mutations reveal common mechanisms of oncogenic activation
Patil, K., Jordan, E. J., Park, J. H., Suresh, K., Smith, C. M., Lemmon, A. A., Mossé, Y. P., Lemmon, M. A., & Radhakrishnan, R. (2021) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.2019132118 · Cited by 9
Class act: safety comparison of approved tyrosine kinase inhibitors for non-small-cell lung carcinoma
Burotto, M., Ali, S. A., & Coyne, G. O. (2014) · Expert Opinion on Drug Safety · doi:10.1517/14740338.2014.973400 · Cited by 9
Regulation of Cell Transformation by Rb-Controlled Redox Homeostasis
Zhu, Z., Wang, Y., Liang, Z., Wang, W., Zhang, H., Li, B., & Ying, G. (2014) · PLoS ONE · doi:10.1371/journal.pone.0102582 · Cited by 9
STX-721, a Covalent EGFR/HER2 Exon 20 Inhibitor, Utilizes Exon 20–Mutant Dynamic Protein States and Achieves Unique Mutant Selectivity Across Human Cancer Models
Pagliarini, R. A., Henderson, J. A., Milgram, B. C., Borrelli, D. R., Brooijmans, N., Hilbert, B. J., Huff, M. R., Ito, T., Kryukov, G. V., Ladd, B., et al. (2025) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-24-3833 · Cited by 10
Amivantamab: A narrative drug review
John, A., Noronha, V., Singh, A. K., Menon, N. S., & Prabhash, K. (2023) · Cancer Research Statistics and Treatment · doi:10.4103/crst.crst_166_23 · Cited by 8
Does the efficacy of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor differ according to the type of EGFR mutation in non-small cell lung cancer?
Choi, Y. W., & Choi, J. (2017) · The Korean Journal of Internal Medicine · doi:10.3904/kjim.2016.190 · Cited by 8
EGFR Inhibitors as the First-Line Systemic Treatment for Advanced Non-Small-Cell Lung Cancer
Kao, H., Lin, C., & Yang, J. C. (2013) · Future Oncology · doi:10.2217/fon.13.56 · Cited by 7
Lazertinib versus Gefitinib as First-Line Treatment for EGFR-mutated Locally Advanced or Metastatic NSCLC: LASER301 Korean Subset
Lee, K. H., Cho, B. C., Ahn, M., Lee, Y., Lee, Y., Lee, J.-S., Kim, J.-H., Min, Y. J., Lee, G., Lee, S. S., et al. (2023) · Cancer Research and Treatment · doi:10.4143/crt.2023.453 · Cited by 7
Novel monoclonal antibodies recognizing the active conformation of epidermal growth factor receptor
Ise, N., Omi, K., Miwa, K., Honda, H., Higashiyama, S., & Goishi, K. (2010) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2010.03.052 · Cited by 7
Validation of gefitinib effectiveness in a broad panel of head and neck squamous carcinoma cells
Sebastian, S., Azzariti, A., Accardi, R., Conti, D., Pilato, B., Lacalamita, R., Porcelli, L., Simone, G., Tommasi, S., Tommasino, M., et al. (2008) · International Journal of Molecular Medicine · doi:10.3892/ijmm.21.6.809 · Cited by 7
Safety and Efficacy of Osimertinib in the Treatment of a Patient With Metastatic Lung Cancer and Concurrent Somatic EGFR L858R and Germline EGFR T790M Mutations
Ma, W., Gong, J., Shan, J., Lewis, D. A., Xiao, W., Moore, E. H., Zhang, Y., Hung, J., MANS, N. Z., Wei, S., et al. (2018) · JCO Precision Oncology · doi:10.1200/po.18.00076 · Cited by 5
Exons 19 and 21 of Epidermal Growth Factor Receptor Are Highly Conserved in Squamous Cell Cancer of the Head and Neck
Carlson, M. L., Wuertz, B. R. K., Lin, J., Taylor, R., & Ondrey, F. G. (2009) · International Journal of Otolaryngology · doi:10.1155/2009/649615 · Cited by 5
Orthogonal validation of PROTAC mediated degradation of the integral membrane proteins EGFR and c-MET
Ruffilli, C., Röth, S., Zelcer, N., & Moreau, K. (2025) · Scientific Reports · doi:10.1038/s41598-024-84217-2 · Cited by 4
Small Molecule Inhibitors
Chen, X., & Jin, J. J. (2016) · Springer eBooks · doi:10.1007/978-1-59745-458-2_40 · Cited by 6
Differential efficacy of tyrosine kinase inhibitors according to the types of EGFR mutations and agents in non-small cell lung cancer: a real-world study
Kim, T., Choi, J., Ahn, M. S., Lee, H. W., Kang, S. Y., Choi, Y. W., Koh, Y. W., & Sheen, S. S. (2024) · BMC Cancer · doi:10.1186/s12885-023-11782-6 · Cited by 6
Resistance to Targeted Therapies As a Result of Mutation(s) in the Target
Cortot, A. B., & Janne, P. A. (2011) · Humana Press eBooks · doi:10.1007/978-1-60761-478-4_1 · Cited by 4
The antibody sc-33040-R fails to specifically recognize phosphorylation of ErbB4 on tyrosine1056
Gallo, R. M., & Riese, D. J. (2007) · Growth Factors · doi:10.1080/08977190701804008 · Cited by 4
Computational delineation of tyrosyl-substrate recognition and catalytic landscapes by the epidermal growth factor receptor tyrosine kinase domain
Liu, Y., & Radhakrishnan, R. (2014) · Molecular BioSystems · doi:10.1039/c3mb70620f · Cited by 4
Mechanisms of resistance to EGFR tyrosine kinase inhibitors: implications for patient selection and drug combination strategies
Eyzaguirre, A., Buck, E. A., Iwata, K. K., Haley, J. D., & Miglarese, M. R. (2008) · Targeted Oncology · doi:10.1007/s11523-008-0093-6 · Cited by 5
Epidermal growth factor receptor gene mutations in patients with lung adenocarcinoma differ by frequency and type between Uighur and Han ethnic groups in Xinjiang Autonomous Region
Li, X., Wang, X., Zhu, H., Liu, C., Zhou, X. Y., Zhao, B., Duan, H., Yang, J., Gu, G., Zhan, Y., et al. (2015) · BMC Genetics · doi:10.1186/s12863-015-0181-4 · Cited by 4
Predictive molecular markers for EGFR-TKI in non-small cell lung cancer patients: new insights and critical aspects
Ulivi, P., Calistri, D., Zoli, W., & Amadori, D. (2010) · Journal of Nucleic Acids Investigation · doi:10.4081/jnai.2010.e10 · Cited by 4
Mapping EGFR1 Mutations in Patients With Lung Adenocarcinoma
Vlastos, F., Zinszner, J., Hussenet, T., du Manoir, S., Vordonis, L., Nikolakopoulou, S., Hardavella, G. F., Lacomme, S., Vignaud, J.-M., & Martinet, N. (2010) · Diagnostic Molecular Pathology · doi:10.1097/pdm.0b013e3181d32605 · Cited by 3
EGFR inhibition generates drug-tolerant persister cells by blocking AKT activity
(2015) · Cancer Cell & Microenvironment · doi:10.14800/ccm.1045 · Cited by 3
Case report of three EGFR TKI naïve lung adenocarcinoma containing double EGFR mutations (L858R/T790M or Exon 19 Deletion/T790M); Comparing genetic information and histology
Sakashita, S., Shiba‐Ishii, A., Murata, Y., Sekimoto, R., Minami, Y., Sato, Y., & Noguchi, M. (2018) · Pathology - Research and Practice · doi:10.1016/j.prp.2018.05.016 · Cited by 3
Double PIK3CA Alterations and Parallel Evolution in Colorectal Cancers
Lin, M.-T., Zheng, G., Rodriguez, E. F., Tseng, L., Parini, V., Xian, R. R., Zou, Y. S., Gocke, C. D., & Eshleman, J. R. (2021) · American Journal of Clinical Pathology · doi:10.1093/ajcp/aqab119 · Cited by 2
Molecular Biology and Genetics of Lung Cancer
Milanović, D. (2011) · Medical radiology · doi:10.1007/174_2011_310 · Cited by 2
Molecular imaging metrics to evaluate response to preclinical therapeutic regimens
Adam Smith, R. (2010) · Frontiers in bioscience · doi:10.2741/3694 · Cited by 2
Predictive Tumor Biomarkers for EGFR Inhibitors
Kim, L., Liu, G., & Tsao, M. (2014) · Lung Cancer · doi:10.1002/9781118468791.ch28 · Cited by 2
Biological Principles and Clinical Application of EGFR Inhibitors in Cancer
Chen, Z., Ramalingam, S. S., & Shin, D. M. (2016) · Springer eBooks · doi:10.1007/978-1-59745-458-2_37 · Cited by 1
Multiple Mutations within Individual Oncogenes: Examples and Clinical Implications
Kataoka, K., & Saito, Y. (2023) · The Keio Journal of Medicine · doi:10.2302/kjm.2022-0026-oa · Cited by 1
Treatment Outcomes From Erlotinib and Gefitinib in Advanced Epidermal Growth Factor Receptor–Mutated Nonsquamous Non–Small Cell Lung Cancer in Aotearoa New Zealand From 2010 to 2020: Nationwide Whole-of-Patient-Population Retrospective Cohort Study
Aye, P. S., Barnes, J., Laking, G. R., Cameron, L., Anderson, M., Luey, B., Delany, S., Harris, D. L., McLaren, B. R., Brenman, E., et al. (2025) · JMIR Cancer · doi:10.2196/65118 · Cited by 1
Overcoming Resistance to EGF Receptor Tyrosine Kinase Inhibitors in EGFR -mutated NSCLC
Saad, S., Huang, K., & Halmos, B. (2014) · Lung Cancer Management · doi:10.2217/lmt.14.35 · Cited by 1
Designing inhibitors for EGFR to improve anti-cancer therapy: An in silico approach
Ahire, V. R., Das, D., Mishra, K. P., & Kulkarni, G. (2014) · European Journal of Biotechnology and Bioscience · Cited by 1
EGFR Resistance
Bourdeanu, L., Liu, E. Y., Brint, S., & Langdon, D. E. (2017) · Resistance to targeted anti-cancer therapeutics · doi:10.1007/978-3-319-70142-4_4 · Cited by 1
Molecular Diagnostics Testing for Lung Adenocarcinoma
Sholl, L. M., & Lindeman, N. I. (2010) · Pathology Case Reviews · doi:10.1097/pcr.0b013e3181e71270 · Cited by 1
EGFR Mutations, Other Molecular Alterations Related To Sensitivity to EGFR Inhibitors, and Molecular Testing for EGFR-Targeted Therapies in Non-Small Cell Lung Cancer
Eberhard, D. A. (2008) · Humana Press eBooks · doi:10.1007/978-1-59745-356-1_20 · Cited by 1
Receptor Tyrosine Kinases
Matthews, D. J., & Gerritsen, M. E. (2010) · Wiley eBooks · doi:10.1002/9780470555293.ch3
Unveiling the Molecular Mechanisms Regulating the Activation of the ErbB Family Receptors at Atomic Resolution through Molecular Modeling and Simulations
Shih, A. (2011) · ScholarlyCommons (University of Pennsylvania)
THE PHARMACOGENOMICS OF EGFR-DEPENDENT NSCLC: PREDICTING AND ENHANCING RESPONSE TO TARGETED EGFR THERAPY
Balko, J. M. (2009) · UKnowledge (University of Kentucky)
Molecular Pathology and Diagnostics of Non-small Cell Lung Carcinoma
Quigley, B., Ducker, S., & Khalil, F. K. (2013) · Springer eBooks · doi:10.1007/978-94-007-7192-5_4
Molecular pathology in lung cancer
Cooper, W. A., & O’Toole, S. A. (2013) · Cancer Forum
Quantitative Analysis of ( 11 C)-Erlotinib PET Demonstrates Specific Binding for Activating Mutations of the EGFR
Petrulli, J. R., Sullivan, J. M., Zheng, M., Bennett, D. C., Charest, J., Huang, Y. H., Morris, E. D., & Contessa, J. N. (2013)
Contrôle de la signalisation oncogénique du mutant L858R de l'EGFR par la protéine
Ozenne, P. (2011)
Reviewmechanisms of acquired resistance to tyrosine kinase targeted therapy
Sierra, J. R., Cepero, V., & Giordano, S. (2010)
Phosphatidylinositol 3-Kinase (PI3K) as a therapeutic target in NSCLC
Stamatkin, C. W. (2014) · UKnowledge (University of Kentucky)
Stromal Lysyl Oxidase-Like 1 Increases Extracellular Matrix Stiffness and Enhances Collagen Fibre Alignment in Non-Small Cell Lung Cancer
Pasko, E. (2015) · TSpace (University of Toronto)
Genetic biomarkers of chemotherapy response and resistance in lung cancer patients
Nelmes, D. (2018) · ORCA Online Research @Cardiff (Cardiff University)
Mechanisms of epidermal growth factor receptor tyrosine kinase activation and nuclear trafficking
Brewer, M. R. (2009)
Molecular Targetable Pathways – EGFR
Lee, R. E., Jr., Girard, N., & Popat, S. (2021) · Elsevier eBooks · doi:10.1016/b978-0-08-102723-3.00146-3
Data from Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non–Small Cell Lung Cancer
(2023) · doi:10.1158/2159-8290.c.6549370.v1
Mutation Analysis of Epidermal Growth Factor Receptor Gene in Non-small Cell Lung Cancer for Selection of Patients Eligible for Tyrosine Kinase Inhibitor Therapy
Ansar, Z., Nasir, A., & Moatter, T. (2024) · Journal of Cancer & Allied Specialties · doi:10.37029/jcas.v10i1.569
MECHANISMS UNDERLYING DISTINCT EGFR VERSUS FGFR-3 AND -1 DEPENDENCY IN HUMAN BLADDER CANCER CELLS
Cheng, T. (2014) · Digital Commons-TMC (Texas Medical Center)
Intracellular Signaling Mechanisms of Resistance to EGFR-Targeting Agents
Quesnelle, K. M. (2012) · D-Scholarship@Pitt (University of Pittsburgh)
Évaluation du patrimoine tumoral circulant dans la prise en charge thérapeutique des patients atteints de cancer broncho-pulmonaire
Garcia, J. (2019) · theses.fr (ABES) · doi:10.70675/f648973az2136z4580z91b5z75a3710f1907
Natural products from Streptomyces cavourensis as candidate modulators of EGFR and KRAS signaling in lung cancer
Kani, U. N., Amini, A., Otalora, K., Davies‐Bolorunduro, O. F., & Behnam, B. (2026) · In Silico Research in Biomedicine · doi:10.1016/j.insi.2026.100427
BindingDB Entry 50009854: Discovery and Structural Optimization of N5-Substituted 6,7-Dioxo-6,7-dihydropteridines as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation.
BindingDB (2021) · UC San Diego · doi:10.7270/q2qv3r1f
BindingDB Entry 50022481: BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models.
BindingDB (2025) · UC San Diego · doi:10.7270/q2rb79br
BindingDB Entry 50000700: Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.
BindingDB (2019) · UC San Diego · doi:10.7270/q28w3gs9

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

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review

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

Abstract

Overview

Integrity signals

Verification

Claims the paper makes

Claims other papers make about this one

Self-check

Citations

Cites

Cited by

Related

Metadata

Record

About these checks