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

Redox Regulation of Epidermal Growth Factor Receptor Signaling through Cysteine Oxidation

(2012) Thu H. Truong et al.   BIOCHEMISTRY

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

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

Functionally Important Aromatic–Aromatic and Sulfur−π Interactions in the D2 Dopamine Receptor

(2012) Kristina N.-M. Daeffler et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Afatinib for patients with lung adenocarcinoma and epidermal growth factor receptor mutations (LUX-Lung 2): a phase 2 trial

(2012) James Chih-Hsin Yang et al.   LANCET ONCOLOGY

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

(2012) Juswinder Singh et al.   MedChemComm

Protein kinase biochemistry and drug discovery

(2011) Phillip A. Schwartz et al.   BIOORGANIC CHEMISTRY

Phase I Dose-Escalation Study of the Pan-HER Inhibitor, PF299804, in Patients with Advanced Malignant Solid Tumors

(2011) P. A. Janne et al.   CLINICAL CANCER RESEARCH

Irreversible Protein Kinase Inhibitors

(2011) L. Garuti et al.   CURRENT MEDICINAL CHEMISTRY

Cysteine Mapping in Conformationally Distinct Kinase Nucleotide Binding Sites: Application to the Design of Selective Covalent Inhibitors

(2011) Emeline Leproult et al.   JOURNAL OF MEDICINAL CHEMISTRY

Peroxide-dependent sulfenylation of the EGFR catalytic site enhances kinase activity

(2011) Candice E Paulsen et al.   Nature Chemical Biology

The resurgence of covalent drugs

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

The Role of Irreversible HER Family Inhibition in the Treatment of Patients with Non-Small Cell Lung Cancer

(2011) E. Kwak   ONCOLOGIST

EGF Receptor Exposed to Oxidative Stress Acquires Abnormal Phosphorylation and Aberrant Activated Conformation That Impairs Canonical Dimerization

(2011) Simone Filosto et al.   PLoS One

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

Orchestrating Redox Signaling Networks through Regulatory Cysteine Switches

(2009) Candice E. Paulsen et al.   ACS Chemical Biology

A randomized, phase II, dose-finding study of the pan-ErbB receptor tyrosine-kinase inhibitor CI-1033 in patients with pretreated metastatic breast cancer

(2009) Olivier Rixe et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

A Zone Classification System for Risk Assessment of Idiosyncratic Drug Toxicity Using Daily Dose and Covalent Binding

(2009) S. Nakayama et al.   DRUG METABOLISM AND DISPOSITION

Activating and resistance mutations of EGFR in non-small-cell lung cancer: role in clinical response to EGFR tyrosine kinase inhibitors

(2009) A F Gazdar   ONCOGENE

Endosomes: A legitimate platform for the signaling train

(2009) J. E. Murphy et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Development of HKI‐272 and Related Compounds for the Treatment of Cancer

(2008) Allan Wissner et al.   ARCHIV DER PHARMAZIE

Comparison of the EGFR resistance mutation profiles generated by EGFR-targeted tyrosine kinase inhibitors and the impact of drug combinations

(2008) Egle Avizienyte et al.   BIOCHEMICAL JOURNAL

Discovering mechanisms of signaling-mediated cysteine oxidation

(2008) Leslie B Poole et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Trafficking of receptor tyrosine kinases to the nucleus

(2008) Graham Carpenter et al.   EXPERIMENTAL CELL RESEARCH

Recognition-Domain Focused Chemosensors: Versatile and Efficient Reporters of Protein Kinase Activity

(2008) Elvedin Luković et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY