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

Proceedings of the National Academy of Sciences of the United States of America

Volumn 111, Issue 1, 2014, Pages 173-178

  Schwartz, Phillip A ^a   Kuzmic, Petr ^b   Solowiej, James ^a   Bergqvist, Simon ^a   Bolanos, Ben ^a   Almaden, Chau ^a   Nagata, Asako ^a   Ryan, Kevin ^a   Feng, Junli ^a   Dalvie, Deepak ^a   Kath, John C ^a   Xu, Meirong ^a   Wani, Revati ^a   Murray, Brion William ^a  

^a PFIZER INC   (United States)

^b BioKin Ltd   (United States)

Author keywords

Capture period; Cysteine oxidation; Protein kinase; Signaling; Warhead interactions

Indexed keywords

AFATINIB; CANERTINIB; CYSTEINE; DACOMITINIB; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; GEFITINIB; GLUTATHIONE; HYDROGEN PEROXIDE; LAPATINIB; NERATINIB; NUCLEOPHILE;

ARTICLE; AUTOPHOSPHORYLATION; BINDING AFFINITY; CATALYSIS; CHEMICAL REACTION; COVALENT BOND; DISSOCIATION; DISSOCIATION CONSTANT; DRUG DESIGN; DRUG MECHANISM; DRUG POTENCY; DRUG RESISTANCE; ENZYME ACTIVITY; EXPERIMENTAL DESIGN; MOLECULAR MODEL; NUCLEOPHILICITY; OXIDATION; PRIORITY JOURNAL; QUALITY CONTROL; SURFACE PLASMON RESONANCE;

CAPTURE PERIOD; CYSTEINE OXIDATION; PROTEIN KINASE; SIGNALING; WARHEAD INTERACTIONS;

ANTINEOPLASTIC AGENTS; CATALYSIS; CELL LINE, TUMOR; CHEMISTRY, PHARMACEUTICAL; CYSTEINE; DRUG DESIGN; DRUG RESISTANCE; ENZYME INHIBITORS; ENZYME-LINKED IMMUNOSORBENT ASSAY; HUMANS; INHIBITORY CONCENTRATION 50; MASS SPECTROMETRY; OXYGEN; PHOSPHORYLATION; PROTEIN BINDING; PROTEIN CONFORMATION; QUINAZOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR; SIGNAL TRANSDUCTION;

EID: 84891946419     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.1313733111     Document Type: Article

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