Search Results - "Alligood, K J"
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Assessment of epidermal growth factor receptor (EGFR, ErbB1) and HER2 (ErbB2) protein expression levels and response to lapatinib (Tykerb®, GW572016) in an expanded panel of human normal and tumour cell lines
Published in Cell proliferation (01-08-2007)“… Objective: Lapatinib (Tykerb®, GW572016), a potent inhibitor of the catalytic activities of epidermal growth factor receptor (EGFR) and human epidermal…”
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Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways
Published in Oncogene (12-09-2002)“…Dual EGFR/erbB2 inhibition is an attractive therapeutic strategy for epithelial tumors, as ligand-induced erbB2/EGFR heterodimerization triggers potent…”
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The Effects of the Novel, Reversible Epidermal Growth Factor Receptor/ErbB-2 Tyrosine Kinase Inhibitor, GW2016, on the Growth of Human Normal and Tumor-derived Cell Lines in Vitro and in Vivo
Published in Molecular cancer therapeutics (01-12-2001)“…The epidermal growth factor receptor (EGFR) and ErbB-2 transmembrane tyrosine kinases are currently being targeted by various mechanisms in the treatment of…”
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The characterization of novel, dual ErbB-2/EGFR, tyrosine kinase inhibitors: Potential therapy for cancer
Published in Cancer research (Chicago, Ill.) (01-10-2001)“…The type I receptor tyrosine kinases constitute a family of transmembrane proteins involved in various aspects of cell growth and survival and have been…”
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The formation of a covalent complex between a dipeptide ligand and the src SH2 domain
Published in Bioorganic & medicinal chemistry letters (19-05-1998)“…The X-ray crystal structure of the src SH2 domain revealed the presence of a thiol residue (Cys 188) located proximal to the phosphotyrosine portion of a…”
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Potent Dipeptide Inhibitors of the pp60c-src SH2 Domain
Published in Journal of medicinal chemistry (21-05-1998)“…The design, synthesis, and evaluation of dipeptide analogues as ligands for the pp60c-src SH2 domain are described. The critical binding interactions between…”
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A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): Relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells
Published in Cancer research (Chicago, Ill.) (15-09-2004)“…GW572016 (Lapatinib) is a tyrosine kinase inhibitor in clinical development for cancer that is a potent dual inhibitor of epidermal growth factor receptor…”
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Monoclonal antibodies generated against recombinant ATM support kinase activity
Published in Hybridoma (01-08-2000)“…We report on the rapid generation of two monoclonal antibodies, ATM A16.35 and ATM D16.11, that bind to the kinase domain of mutated ataxia telangiectasia…”
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Comparison of the biochemical and kinetic properties of the type 1 receptor tyrosine kinase intracellular domains. Demonstration of differential sensitivity to kinase inhibitors
Published in The Journal of biological chemistry (11-01-2002)“…Epidermal growth factor receptor (EGFR), ErbB-2, and ErbB-4 are members of the type 1 receptor tyrosine kinase family. Overexpression of these receptors,…”
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Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-05-2006)“…Anilinoalkynylpyrimidines were prepared and evaluated as dual EGFR/ErbB2 kinase inhibitors. A preference was found for substituted phenyl and heteroaromatic…”
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