Insight into the Inhibition of Drug-Resistant Mutants of the Receptor Tyrosine Kinase EGFR

EGF816 Exerts Anticancer Effects in Non–Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor

(2016) Yong Jia et al.   CANCER RESEARCH

Covalent-Allosteric Kinase Inhibitors

(2015) Jörn Weisner et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

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

Acquired EGFR C797S mutation mediates resistance to AZD9291 in non–small cell lung cancer harboring EGFR T790M

(2015) Kenneth S Thress et al.   NATURE MEDICINE

Rociletinib in EGFR-Mutated Non–Small-Cell Lung Cancer

(2015) Lecia V. Sequist et al.   NEW ENGLAND JOURNAL OF MEDICINE

AZD9291 in EGFR Inhibitor–Resistant Non–Small-Cell Lung Cancer

(2015) Pasi A. Jänne et al.   NEW ENGLAND JOURNAL OF MEDICINE

Hope and Disappointment: Covalent Inhibitors to Overcome Drug Resistance in Non-Small Cell Lung Cancer

(2015) Julian Engel et al.   ACS Medicinal Chemistry Letters

Epidermal Growth Factor Receptor (EGFR) Signaling and Covalent EGFR Inhibition in Lung Cancer

(2012) Johannes M. Heuckmann et al.   JOURNAL OF CLINICAL ONCOLOGY

Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial

(2012) Rafael Rosell et al.   LANCET ONCOLOGY

The resurgence of covalent drugs

(2011) Juswinder Singh et al.   NATURE REVIEWS DRUG DISCOVERY

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

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

Chemogenomic Profiling Provides Insights into the Limited Activity of Irreversible EGFR Inhibitors in Tumor Cells Expressing the T790M EGFR Resistance Mutation

(2010) M. L. Sos et al.   CANCER RESEARCH

Characterization of Irreversible Kinase Inhibitors by Directly Detecting Covalent Bond Formation: A Tool for Dissecting Kinase Drug Resistance

(2010) Sabine Klüter  et al.   CHEMBIOCHEM

Gefitinib or Chemotherapy for Non–Small-Cell Lung Cancer with Mutated EGFR

(2010) Makoto Maemondo et al.   NEW ENGLAND JOURNAL OF MEDICINE

Gefitinib or Carboplatin–Paclitaxel in Pulmonary Adenocarcinoma

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

Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR

(2008) Anja Michalczyk et al.   BIOORGANIC & MEDICINAL CHEMISTRY