Current Approaches in NSCLC Targeting K-RAS and EGFR

The Value of Liquid Biopsies for Guiding Therapy Decisions in Non-small Cell Lung Cancer

(2019) Jatta Saarenheimo et al.   Frontiers in Oncology

The Presence of Concomitant Mutations Affects the Activity of EGFR Tyrosine Kinase Inhibitors in EGFR-Mutant Non-Small Cell Lung Cancer (NSCLC) Patients

(2019) Anna Rachiglio et al.   Cancers

SMARCA4 loss is synthetic lethal with CDK4/6 inhibition in non-small cell lung cancer

(2019) Yibo Xue et al.   Nature Communications

First-line tyrosine kinase inhibitors in EGFR mutation-positive non-small-cell lung cancer: a network meta-analysis

(2019) Marscha S Holleman et al.   OncoTargets and Therapy

Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS–SOS1 interaction

(2019) Roman C. Hillig et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Efficacy of Immune Checkpoint Inhibitors in KRAS-Mutant Non-Small Cell Lung Cancer (NSCLC)

(2019) Arnaud Jeanson et al.   Journal of Thoracic Oncology

Correction to: Neratinib in Early-Stage Breast Cancer: A Profile of Its Use in the EU

(2019) Sohita Dhillon   CLINICAL DRUG INVESTIGATION

Targeting Epidermal Growth Factor Receptor in Non-Small-Cell-Lung Cancer: Current State and Future Perspective

(2019) Shui-ming Bao et al.   Anti-Cancer Agents in Medicinal Chemistry

Integrating Osimertinib in Clinical Practice for Non-Small Cell Lung Cancer Treatment

(2019) Senthil Rajappa et al.   ADVANCES IN THERAPY

K-RasG12D Has a Potential Allosteric Small Molecule Binding Site

(2019) Huizhong Feng et al.   BIOCHEMISTRY

Phase 1 study evaluating the safety, tolerability, pharmacokinetics (PK), and efficacy of AMG 510, a novel small molecule KRASG12C inhibitor, in advanced solid tumors.

(2019) Marwan Fakih et al.   JOURNAL OF CLINICAL ONCOLOGY

Third generation EGFR inhibitor osimertinib combined with pemetrexed or cisplatin exerts long-lasting anti-tumor effect in EGFR-mutated pre-clinical models of NSCLC

(2019) Silvia La Monica et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Single and dual targeting of mutant EGFR with an allosteric inhibitor

(2019) Ciric To et al.   Cancer Discovery

Clinical features and therapeutic options in non‐small cell lung cancer patients with concomitant mutations of EGFR , ALK , ROS1 , KRAS or BRAF

(2019) Xibin Zhuang et al.   Cancer Medicine

Drug library screen reveals benzimidazole derivatives as selective cytotoxic agents for KRAS-mutant lung cancer

(2019) Iwao Shimomura et al.   CANCER LETTERS

Clinical outcomes to pemetrexed-based versus non-pemetrexed-based platinum doublets in patients with KRAS-mutant advanced non-squamous non-small cell lung cancer

(2019) B. Ricciuti et al.   Clinical & Translational Oncology

Understanding the Mechanisms of Resistance in EGFR-Positive NSCLC: From Tissue to Liquid Biopsy to Guide Treatment Strategy

(2019) Marzia Del Re et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Conformationally constrained peptides target the allosteric kinase dimer interface and inhibit EGFR activation

(2018) Melody D. Fulton et al.   BIOORGANIC & MEDICINAL CHEMISTRY

KRAS Dimerization Impacts MEK Inhibitor Sensitivity and Oncogenic Activity of Mutant KRAS

(2018) Chiara Ambrogio et al.   CELL

Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor

(2018) Matthew R. Janes et al.   CELL

Resistance to EGFR inhibitors in non-small cell lung cancer: Clinical management and future perspectives

(2018) Chiara Tomasello et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Targeting EGFR in Lung Cancer: Current Standards and Developments

(2018) Asunción Díaz-Serrano et al.   DRUGS

Acquired resistance in oncogene-addicted non-small-cell lung cancer

(2018) Claudio Sini et al.   Future Oncology

Combination Strategies Using EGFR-TKi in NSCLC Therapy: Learning from the Gap between Pre-Clinical Results and Clinical Outcomes

(2018) Zheng Yang et al.   International Journal of Biological Sciences

IASLC Statement Paper: Liquid Biopsy for Advanced Non-Small Cell Lung Cancer (NSCLC)

(2018) Christian Rolfo et al.   Journal of Thoracic Oncology

Management of acquired resistance to EGFR TKI–targeted therapy in advanced non-small cell lung cancer

(2018) Shang-Gin Wu et al.   Molecular Cancer

Third generation EGFR TKIs: current data and future directions

(2018) Chee-Seng Tan et al.   Molecular Cancer

Mechanisms and clinical activity of an EGFR and HER2 exon 20–selective kinase inhibitor in non–small cell lung cancer

(2018) Jacqulyne P. Robichaux et al.   NATURE MEDICINE

EGFR-TKIs in non-small-cell lung cancer: focus on clinical pharmacology and mechanisms of resistance

(2018) Stefano Fogli et al.   PHARMACOGENOMICS

Blocking Ras inhibition as an antitumor strategy

(2018) Nagore I. Marín-Ramos et al.   SEMINARS IN CANCER BIOLOGY

Concomitant driver mutations in advanced EGFR-mutated non-small-cell lung cancer and their impact on erlotinib treatment

(2018) Jan Nyrop Jakobsen et al.   Oncotarget

Efficacy and Safety of Afatinib for EGFR-mutant Non-small Cell Lung Cancer, Compared with Gefitinib or Erlotinib

(2018) Youjin Kim et al.   Cancer Research and Treatment

Phosphorylated EGFR Dimers Are Not Sufficient to Activate Ras

(2018) Samantha I. Liang et al.   Cell Reports

Global cancer statistics 2018: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries

(2018) Freddie Bray et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Phase 1B Study of Momelotinib Combined With Trametinib in Metastatic, Kirsten Rat Sarcoma Viral Oncogene Homolog - Mutated Non–Small-Cell Lung Cancer After Platinum-Based Chemotherapy Treatment Failure

(2018) David A. Barbie et al.   Clinical Lung Cancer

Therapeutic approaches for T790M mutation positive non-small-cell lung cancer

(2018) Ilaria Attili et al.   Expert Review of Anticancer Therapy

Targeting the EMT transcription factor TWIST1 overcomes resistance to EGFR inhibitors in EGFR-mutant non-small-cell lung cancer

(2018) Zachary A. Yochum et al.   ONCOGENE

Targeting oncogenic drivers in lung cancer: Recent progress, current challenges and future opportunities

(2018) Satoshi Yoda et al.   PHARMACOLOGY & THERAPEUTICS

The effectiveness of afatinib and osimertinib in a Chinese patient with advanced lung adenocarcinoma harboring a rare triple EGFR mutation (R670W/H835L/L833V): a case report and literature review

(2018) Bao-Dong Qin et al.   OncoTargets and Therapy

KRAS G12C NSCLC Models Are Sensitive to Direct Targeting of KRAS in Combination with PI3K Inhibition

(2018) Sandra Misale et al.   CLINICAL CANCER RESEARCH

Emerging drugs for EGFR-mutated non-small cell lung cancer

(2018) Vineeth Sukrithan et al.   EXPERT OPINION ON EMERGING DRUGS

Tumor clonality and resistance mechanisms in EGFR mutation-positive non-small-cell lung cancer: implications for therapeutic sequencing

(2018) Shinji Kohsaka et al.   Future Oncology

Small molecule inhibitors targeting the EGFR/ErbB family of protein-tyrosine kinases in human cancers

(2018) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Dacomitinib versus gefitinib as first-line treatment for patients with EGFR -mutation-positive non-small-cell lung cancer (ARCHER 1050): a randomised, open-label, phase 3 trial

(2017) Yi-Long Wu et al.   LANCET ONCOLOGY

Optimal management of EGFR -mutant non-small cell lung cancer with disease progression on first-line tyrosine kinase inhibitor therapy

(2017) Bin-Chi Liao et al.   LUNG CANCER

Personalized In Vitro and In Vivo Cancer Models to Guide Precision Medicine

(2017) Chantal Pauli et al.   Cancer Discovery

Synthetic Lethal Vulnerabilities in KRAS -Mutant Cancers

(2017) Andrew J. Aguirre et al.   Cold Spring Harbor Perspectives in Medicine

Second-Generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Lung Cancers

(2017) Helena A. Yu et al.   Journal of the National Comprehensive Cancer Network

A Small Molecule RAS-Mimetic Disrupts RAS Association with Effector Proteins to Block Signaling

(2016) Sai Krishna Athuluri-Divakar et al.   CELL

Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers

(2016) Gérald Lelais et al.   JOURNAL OF MEDICINAL CHEMISTRY

K-Ras protein as a drug target

(2016) Frank McCormick   JOURNAL OF MOLECULAR MEDICINE-JMM

Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors

(2016) Yong Jia et al.   NATURE

Targeting the KRAS Pathway in Non-Small Cell Lung Cancer

(2016) P. Tomasini et al.   ONCOLOGIST

Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism

(2016) P. Lito et al.   SCIENCE

Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State

(2016) M. P. Patricelli et al.   Cancer Discovery

Efficacy and Safety of Abemaciclib, an Inhibitor of CDK4 and CDK6, for Patients with Breast Cancer, Non-Small Cell Lung Cancer, and Other Solid Tumors

(2016) A. Patnaik et al.   Cancer Discovery

Drug resistance in cancer: molecular evolution and compensatory proliferation

(2016) Ran Friedman   Oncotarget

Targeted therapies for the treatment of non-small-cell lung cancer: Monoclonal antibodies and biological inhibitors

(2016) Ana P. S. Silva et al.   Human Vaccines & Immunotherapeutics

Direct Modulation of Small GTPase Activity and Function

(2015) Philipp M. Cromm et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A Structural Perspective on the Regulation of the Epidermal Growth Factor Receptor

(2015) Erika Kovacs et al.   Annual Review of Biochemistry

Activation of transmembrane cell-surface receptors via a common mechanism? The “rotation model”

(2015) Ichiro N. Maruyama   BIOESSAYS

KRAS as a Therapeutic Target

(2015) F. McCormick   CLINICAL CANCER RESEARCH

Mapping inhibitor response to the in-frame deletions, insertions and duplications of epidermal growth factor receptor (EGFR) in non-small cell lung cancer

(2015) Jingheng Ning et al.   JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION

In vitro modeling to determine mutation specificity of EGFR tyrosine kinase inhibitors against clinically relevant EGFR mutants in non-small-cell lung cancer

(2015) Toshiyuki Hirano et al.   Oncotarget

Epidermal growth factor receptor (EGFR) mutations in lung cancer: preclinical and clinical data

(2014) S.E.D.C. Jorge et al.   BRAZILIAN JOURNAL OF MEDICAL AND BIOLOGICAL RESEARCH

Putting together structures of epidermal growth factor receptors

(2014) Nicholas J Bessman et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Interdependent epidermal growth factor receptor signalling and trafficking

(2014) Sylwia Jones et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Different Epidermal Growth Factor (EGF) Receptor Ligands Show Distinct Kinetics and Biased or Partial Agonism for Homodimer and Heterodimer Formation

(2014) Jennifer L. Macdonald-Obermann et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Afatinib versus cisplatin plus gemcitabine for first-line treatment of Asian patients with advanced non-small-cell lung cancer harbouring EGFR mutations (LUX-Lung 6): an open-label, randomised phase 3 trial

(2014) Yi-Long Wu et al.   LANCET ONCOLOGY

The EGFR Family: Not So Prototypical Receptor Tyrosine Kinases

(2014) M. A. Lemmon et al.   Cold Spring Harbor Perspectives in Biology

AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer

(2014) D. A. E. Cross et al.   Cancer Discovery

Phase III Study of Afatinib or Cisplatin Plus Pemetrexed in Patients With Metastatic Lung Adenocarcinoma WithEGFRMutations

(2013) Lecia V. Sequist et al.   JOURNAL OF CLINICAL ONCOLOGY

Natural History and Molecular Characteristics of Lung Cancers Harboring EGFR Exon 20 Insertions

(2013) Geoffrey R. Oxnard et al.   Journal of Thoracic Oncology

Uncommon Epidermal Growth Factor Receptor mutations in non-small cell lung cancer and their mechanisms of EGFR tyrosine kinase inhibitors sensitivity and resistance

(2013) Erminia Massarelli et al.   LUNG CANCER

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

(2013) Jonathan M. Ostrem et al.   NATURE

The quest to overcome resistance to EGFR-targeted therapies in cancer

(2013) Curtis R Chong et al.   NATURE MEDICINE

The ErbB/HER family of protein-tyrosine kinases and cancer

(2013) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance

(2013) P. A. Schwartz 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

Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

(2013) A. O. Walter et al.   Cancer Discovery

Synthetic Lethal Interaction of Combined BCL-XL and MEK Inhibition Promotes Tumor Regressions in KRAS Mutant Cancer Models

(2012) Ryan B. Corcoran et al.   CANCER CELL

The GATA2 Transcriptional Network Is Requisite for RAS Oncogene-Driven Non-Small Cell Lung Cancer

(2012) Madhu S. Kumar et al.   CELL

Molecular Epidemiology of EGFR and KRAS Mutations in 3,026 Lung Adenocarcinomas: Higher Susceptibility of Women to Smoking-Related KRAS-Mutant Cancers

(2012) S. Dogan et al.   CLINICAL CANCER RESEARCH

Prevalence, Clinicopathologic Associations, and Molecular Spectrum of ERBB2 (HER2) Tyrosine Kinase Mutations in Lung Adenocarcinomas

(2012) M. E. Arcila et al.   CLINICAL CANCER RESEARCH

The Role of EGFR Tyrosine Kinase Inhibitors in the First-Line Treatment of Advanced Non Small Cell Lung Cancer Patients Harboring EGFR Mutation

(2012) A. Sgambato et al.   CURRENT MEDICINAL CHEMISTRY

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

Development of PI3K/AKT/mTOR Pathway Inhibitors and Their Application in Personalized Therapy for Non–Small-Cell Lung Cancer

(2012) Vassiliki Papadimitrakopoulou   Journal of Thoracic Oncology

Lung cancers with acquired resistance to EGFR inhibitors occasionally harbor BRAF gene mutations but lack mutations in KRAS, NRAS, or MEK1

(2012) K. Ohashi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Superiority of a novel EGFR targeted covalent inhibitor over its reversible counterpart in overcoming drug resistance

(2012) Juswinder Singh et al.   MedChemComm

Reactivation of ERK Signaling Causes Resistance to EGFR Kinase Inhibitors

(2012) Dalia Ercan et al.   Cancer Discovery

HER2 Amplification: A Potential Mechanism of Acquired Resistance to EGFR Inhibition in EGFR -Mutant Lung Cancers That Lack the Second-Site EGFR T790M Mutation

(2012) Ken Takezawa et al.   Cancer Discovery

Phase I/II Trial of Cetuximab and Erlotinib in Patients with Lung Adenocarcinoma and Acquired Resistance to Erlotinib

(2011) Y. Y. Janjigian et al.   CLINICAL CANCER RESEARCH

Pretreatment EGFR T790M Mutation and BRCA1 mRNA Expression in Erlotinib-Treated Advanced Non-Small-Cell Lung Cancer Patients with EGFR Mutations

(2011) R. Rosell et al.   CLINICAL CANCER RESEARCH

Lung Cancer: Epidemiology, Etiology, and Prevention

(2011) Charles S. Dela Cruz et al.   CLINICS IN CHEST MEDICINE

EGFR exon 20 insertion mutations in non-small-cell lung cancer: preclinical data and clinical implications

(2011) Hiroyuki Yasuda et al.   LANCET ONCOLOGY

An orthosteric inhibitor of the Ras-Sos interaction

(2011) Anupam Patgiri et al.   Nature Chemical Biology

Harnessing synthetic lethal interactions in anticancer drug discovery

(2011) Denise A. Chan et al.   NATURE REVIEWS DRUG DISCOVERY

Feedback regulation of EGFR signalling: decision making by early and delayed loops

(2011) Roi Avraham et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Genotypic and Histological Evolution of Lung Cancers Acquiring Resistance to EGFR Inhibitors

(2011) L. V. Sequist et al.   Science Translational Medicine

A Synthetic Lethal Interaction between K-Ras Oncogenes and Cdk4 Unveils a Therapeutic Strategy for Non-small Cell Lung Carcinoma

(2010) Marta Puyol et al.   CANCER CELL

An ErbB3 Antibody, MM-121, Is Active in Cancers with Ligand-Dependent Activation

(2010) B. Schoeberl et al.   CANCER RESEARCH

Cell Signaling by Receptor Tyrosine Kinases

(2010) Mark A. Lemmon et al.   CELL

Targeting the Dimerization of Epidermal Growth Factor Receptors with Small-Molecule Inhibitors

(2010) Robert Y. C. Yang et al.   Chemical Biology & Drug Design

Neratinib, an Irreversible Pan-ErbB Receptor Tyrosine Kinase Inhibitor: Results of a Phase II Trial in Patients With Advanced Non–Small-Cell Lung Cancer

(2010) Lecia V. Sequist et al.   JOURNAL OF CLINICAL ONCOLOGY

Neratinib, an Irreversible ErbB Receptor Tyrosine Kinase Inhibitor, in Patients With Advanced ErbB2-Positive Breast Cancer

(2010) Harold J. Burstein et al.   JOURNAL OF CLINICAL ONCOLOGY

EGFR T790M Mutation: A Double Role in Lung Cancer Cell Survival?

(2010) Kenichi Suda et al.   Journal of Thoracic Oncology

Comparison of gefitinib and erlotinib in advanced NSCLC and the effect of EGFR mutations

(2010) Jenn-Yu Wu et al.   LUNG CANCER

Asymmetric tyrosine kinase arrangements in activation or autophosphorylation of receptor tyrosine kinases

(2010) Jae Hyun Bae et al.   MOLECULES AND CELLS

Structural and mechanistic underpinnings of the differential drug sensitivity of EGFR mutations in non-small cell lung cancer

(2009) Michael J. Eck et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

ErbB receptors and signaling pathways in cancer

(2009) Nancy E Hynes et al.   CURRENT OPINION IN CELL BIOLOGY

Gefitinib or Carboplatin–Paclitaxel in Pulmonary Adenocarcinoma

(2009) Tony S. Mok et al.   NEW ENGLAND JOURNAL OF MEDICINE

Differential Effects of EGFR Ligands on Endocytic Sorting of the Receptor

(2009) Kirstine Roepstorff et al.   TRAFFIC

Structure-Based View of Epidermal Growth Factor Receptor Regulation

(2008) Kathryn M. Ferguson   Annual Review of Biophysics

Oncogene Addiction

(2008) I. B. Weinstein et al.   CANCER RESEARCH

Acquired Resistance to Epidermal Growth Factor Receptor Kinase Inhibitors Associated with a Novel T854A Mutation in a Patient with EGFR-Mutant Lung Adenocarcinoma

(2008) J. Bean et al.   CLINICAL CANCER RESEARCH

Ligand-induced ErbB receptor dimerization

(2008) Mark A. Lemmon   EXPERIMENTAL CELL RESEARCH

Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers

(2008) Jeffrey A Engelman et al.   NATURE MEDICINE

Detection of Mutations inEGFRin Circulating Lung-Cancer Cells

(2008) Shyamala Maheswaran et al.   NEW ENGLAND JOURNAL OF MEDICINE

BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models

(2008) D Li et al.   ONCOGENE

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