A brief perspective of drug resistance toward EGFR inhibitors: the crystal structures of EGFRs and their variants

Trials and Tribulations of EGFR and MET Inhibitor Combination Therapy in NSCLC

(2017) Benjamin Solomon   Journal of Thoracic Oncology

EPHA2 Blockade Overcomes Acquired Resistance to EGFR Kinase Inhibitors in Lung Cancer

(2016) Katherine R. Amato et al.   CANCER RESEARCH

Abstract 1068: The promise of miR-205 in HER2+ breast cancer: predicting response to Trastuzumab and overcoming resistance

(2016) Claudia Piovan et al.   CANCER RESEARCH

A Phase III Clinical Trial of the Epidermal Growth Factor Vaccine CIMAvax-EGF as Switch Maintenance Therapy in Advanced Non-Small Cell Lung Cancer Patients

(2016) P. C. Rodriguez et al.   CLINICAL CANCER RESEARCH

The Membrane Mimetic Affects the Spatial Structure and Mobility of EGFR Transmembrane and Juxtamembrane Domains

(2015) Konstantin S. Mineev et al.   BIOCHEMISTRY

Acquired resistance to anti-EGFR mAb ICR62 in cancer cells is accompanied by an increased EGFR expression, HER-2/HER-3 signalling and sensitivity to pan HER blockers

(2015) Said A Khelwatty et al.   BRITISH JOURNAL OF CANCER

Exon 19 deletion was associated with better survival outcomes in advanced lung adenocarcinoma with mutant EGFR treated with EGFR-TKIs as second-line therapy after first-line chemotherapy: a retrospective analysis of 128 patients

(2015) Y. Wang et al.   Clinical & Translational Oncology

SEARCH: A Phase III, Randomized, Double-Blind, Placebo-Controlled Trial of Sorafenib Plus Erlotinib in Patients With Advanced Hepatocellular Carcinoma

(2015) Andrew X. Zhu et al.   JOURNAL OF CLINICAL ONCOLOGY

Epigenetic Changes of EGFR Have an Important Role in BRAF Inhibitor–Resistant Cutaneous Melanomas

(2015) Jinhua Wang et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach

(2015) Julian Engel et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemoradiotherapy with or without panitumumab in patients with unresected, locally advanced squamous-cell carcinoma of the head and neck (CONCERT-1): a randomised, controlled, open-label phase 2 trial

(2015) Ricard Mesía et al.   LANCET ONCOLOGY

Gefitinib plus chemotherapy versus placebo plus chemotherapy in EGFR-mutation-positive non-small-cell lung cancer after progression on first-line gefitinib (IMPRESS): a phase 3 randomised trial

(2015) Jean-Charles Soria et al.   LANCET ONCOLOGY

Efficacy of EGFR tyrosine kinase inhibitors in patients with EGFR-mutated non-small cell lung cancer except both exon 19 deletion and exon 21 L858R: A retrospective analysis in Korea

(2015) Jin Ho Baek et al.   LUNG CANCER

Rare occurrence of EGFRvIII deletion in head and neck squamous cell carcinoma

(2015) Arun Khattri et al.   ORAL ONCOLOGY

Epidermal growth factor receptor variant III mutation in Chinese patients with squamous cell cancer of the lung

(2015) Jianchun Duan et al.   Thoracic Cancer

Mechanisms of resistance to EGFR tyrosine kinase inhibitors

(2015) Lihua Huang et al.   Acta Pharmaceutica Sinica B

Cationic Polyamidoamine Dendrimers as Modulators of EGFR Signaling In Vitro and In Vivo

(2015) Saghir Akhtar et al.   PLoS One

Mode of cell death induced by the HSP90 inhibitor 17-AAG (tanespimycin) is dependent on the expression of pro-apoptotic BAX

(2015) Marissa V Powers et al.   Oncotarget

Hsp90 Chaperone Inhibitor 17-AAG Attenuates A -Induced Synaptic Toxicity and Memory Impairment

(2014) Y. Chen et al.   JOURNAL OF NEUROSCIENCE

Pyrimido[4,5-d]pyrimidin-4(1H)-one Derivatives as Selective Inhibitors of EGFR Threonine790to Methionine790(T790M) Mutants

(2013) Tianfeng Xu et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Architecture and Membrane Interactions of the EGF Receptor

(2013) Anton Arkhipov et al.   CELL

Conformational Coupling across the Plasma Membrane in Activation of the EGF Receptor

(2013) Nicholas F. Endres et al.   CELL

Ins and Outs of Kinase DFG Motifs

(2013) Daniel K. Treiber et al.   CHEMISTRY & BIOLOGY

Design, Synthesis, and Biological Evaluation of 2-Oxo-3,4-dihydropyrimido[4,5-d]pyrimidinyl Derivatives as New Irreversible Epidermal Growth Factor Receptor Inhibitors with Improved Pharmacokinetic Properties

(2013) Shilin Xu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Erlotinib resistance in EGFR-amplified glioblastoma cells is associated with upregulation of EGFRvIII and PI3Kp110 

(2013) A. Schulte et al.   NEURO-ONCOLOGY

Mechanism for activation of mutated epidermal growth factor receptors in lung cancer

(2013) M. Red Brewer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Transitions to catalytically inactive conformations in EGFR kinase

(2013) Y. Shan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural, Biochemical, and Clinical Characterization of Epidermal Growth Factor Receptor (EGFR) Exon 20 Insertion Mutations in Lung Cancer

(2013) H. Yasuda et al.   Science Translational Medicine

Structural investigation of deleterious non-synonymous SNPs of EGFR gene

(2013) Dhwani Raghav et al.   Interdisciplinary Sciences-Computational Life Sciences

An Epithelial-Mesenchymal Transition Gene Signature Predicts Resistance to EGFR and PI3K Inhibitors and Identifies Axl as a Therapeutic Target for Overcoming EGFR Inhibitor Resistance

(2012) L. A. Byers et al.   CLINICAL CANCER RESEARCH

Pretreatment Epidermal Growth Factor Receptor (EGFR) T790M Mutation Predicts Shorter EGFR Tyrosine Kinase Inhibitor Response Duration in Patients With Non–Small-Cell Lung Cancer

(2012) Kang-Yi Su et al.   JOURNAL OF CLINICAL ONCOLOGY

Structural basis for the altered drug sensitivities of non-small cell lung cancer-associated mutants of human epidermal growth factor receptor

(2012) S Yoshikawa et al.   ONCOGENE

EGFR-mutated oncogene-addicted non-small cell lung cancer: Current trends and future prospects

(2011) Jean-Charles Soria et al.   CANCER TREATMENT REVIEWS

EGFR Exon 19 Insertions: A New Family of Sensitizing EGFR Mutations in Lung Adenocarcinoma

(2011) M. He et al.   CLINICAL CANCER RESEARCH

EGFR and EGFRvIII interact with PUMA to inhibit mitochondrial translocalization of PUMA and PUMA-mediated apoptosis independent of EGFR kinase activity

(2010) Hu Zhu et al.   CANCER LETTERS

Structural Evidence for Loose Linkage between Ligand Binding and Kinase Activation in the Epidermal Growth Factor Receptor

(2010) C. Lu et al.   MOLECULAR AND CELLULAR BIOLOGY

Spatial control of EGF receptor activation by reversible dimerization on living cells

(2010) Inhee Chung et al.   NATURE

EGFRvIV: a previously uncharacterized oncogenic mutant reveals a kinase autoinhibitory mechanism

(2010) G Pines et al.   ONCOGENE

Robust Detection of EGFR Copy Number Changes and EGFR Variant III: Technical Aspects and Relevance for Glioma Diagnostics

(2009) Judith Jeuken et al.   BRAIN PATHOLOGY

EGFRvIII and DNA Double-Strand Break Repair: A Molecular Mechanism for Radioresistance in Glioblastoma

(2009) B. Mukherjee et al.   CANCER RESEARCH

The Juxtamembrane Region of the EGF Receptor Functions as an Activation Domain

(2009) Monica Red Brewer et al.   MOLECULAR CELL

EphrinA5 acts as a tumor suppressor in glioma by negative regulation of epidermal growth factor receptor

(2009) J-J Li et al.   ONCOGENE

Oncogenic EGFR signaling cooperates with loss of tumor suppressor gene functions in gliomagenesis

(2009) Haihao Zhu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Oncogenic EGFR Signaling Networks in Glioma

(2009) P. H. Huang et al.   Science Signaling

Matuzumab Binding to EGFR Prevents the Conformational Rearrangement Required for Dimerization

(2008) Judith Schmiedel et al.   CANCER CELL

Hsp90 Inhibition Suppresses Mutant EGFR-T790M Signaling and Overcomes Kinase Inhibitor Resistance

(2008) T. Shimamura et al.   CANCER RESEARCH

Lung Cancer with Epidermal Growth Factor Receptor Exon 20 Mutations Is Associated with Poor Gefitinib Treatment Response

(2008) J.-Y. Wu et al.   CLINICAL CANCER RESEARCH

Spatial Structure of the Dimeric Transmembrane Domain of the Growth Factor Receptor ErbB2 Presumably Corresponding to the Receptor Active State

(2008) Eduard V. Bocharov et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Lung adenocarcinoma: guiding EGFR-targeted therapy and beyond

(2008) Marc Ladanyi et al.   MODERN PATHOLOGY

The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

(2008) C.-H. Yun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA