Search Results - "Dobrusin, E M"
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Structure-Based Design of a Potent, Selective, and Irreversible Inhibitor of the Catalytic Domain of the erbB Receptor Subfamily of Protein Tyrosine Kinases
Published in Journal of medicinal chemistry (28-03-1997)“…We report the use of structure-based drug design to create a selective erbB-1 (a.k.a. epidermal growth factor receptor) and erbB-2 (a.k.a. neu/her2 growth…”
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Substrate Specificity of the Protein Tyrosine Phosphatases
Published in Proceedings of the National Academy of Sciences - PNAS (15-05-1993)“…The substrate specificity of a recombinant protein tyrosine phosphatase (PTPase) was probed using synthetic phosphotyrosine-containing peptides corresponding…”
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Sequence specificity in recognition of the epidermal growth factor receptor by protein tyrosine phosphatase 1B
Published in The Journal of biological chemistry (05-11-1993)“…Protein tyrosine phosphatases all contain a conserved cysteine that forms an intermediate thiophosphate ester bond during tyrosine phosphate hydrolysis. A…”
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Tyrosine Kinase Inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(Phenylamino)pyrido[d]pyrimidine Acrylamides as Irreversible Inhibitors of the ATP Binding Site of the Epidermal Growth Factor Receptor
Published in Journal of medicinal chemistry (20-05-1999)“…A series of 6- and 7-acrylamide derivatives of the 4-(phenylamino)quinazoline and -pyridopyrimidine classes of epidermal growth factor receptor (EGFR)…”
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Specific, Irreversible Inactivation of the Epidermal Growth Factor Receptor and erbB2, by a New Class of Tyrosine Kinase Inhibitor
Published in Proceedings of the National Academy of Sciences - PNAS (29-09-1998)“…A class of high-affinity inhibitors is disclosed that selectively target and irreversibly inactivate the epidermal growth factor receptor tyrosine kinase…”
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Determinants of Substrate Recognition in the Protein-tyrosine Phosphatase, PTP1 (∗)
Published in The Journal of biological chemistry (08-03-1996)“…Photoaffinity labeling has been used to identify amino acids involved in recognition of protein substrates by the protein-tyrosine phosphatase PTP1. The…”
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Identification of amino acids in the N-terminal SH2 domain of phospholipase C gamma 1 important in the interaction with epidermal growth factor receptor
Published in Biochemistry (Easton) (13-12-1994)“…Photoaffinity labeling and site-directed mutagenesis have been used to identify amino acid residues of the phospholipase C gamma 1 (PLC gamma 1) N-terminal SH2…”
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Tyrosine Kinase Inhibitors. 3. Structure-Activity Relationships for Inhibition of Protein Tyrosine Kinases by Nuclear-Substituted Derivatives of 2,2'-Dithiobis(1-methyl-N-phenyl-1H-indole-3-carboxamide)
Published in Journal of medicinal chemistry (01-06-1994)“…A series of indole-substituted 2,2'-dithiobis(1-methyl-N-phenyl-1H-indole-3-carboxamides) were prepared and evaluated for their ability to inhibit the tyrosine…”
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Tyrosine kinase inhibitors. 1. Structure-activity relationships for inhibition of epidermal growth factor receptor tyrosine kinase activity by 2,3-dihydro-2-thioxo-1H-indole-3-alkanoic acids and 2,2'-dithiobis(1H-indole-3-alkanoic acids)
Published in Journal of medicinal chemistry (01-08-1993)“…A series of 2,3-dihydro-2-thioxo-1H-indole-3-alkanoic acids, and their methyl esters were prepared, the majority by oxidation of 1H-indole-3-alkanoic acids…”
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Differentiation of peptide molecular recognition by phospholipase Cγ‐1 Src homology‐2 domain and a mutant Tyr phosphatase PTP1bC215S
Published in Protein science (01-01-1995)“…Activated epidermal growth factor receptor (EGFR) undergoes autophosphorylation on several cytoplasmic tyrosine residues, which may then associate with the src…”
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Design of a potent peptide inhibitor of the epidermal growth factor receptor tyrosine kinase utilizing sequences based on the natural phosphorylation sites of phospholipase C-gamma 1
Published in Peptides (New York, N.Y. : 1980) (1994)“…Peptides that possess primary sequences identical to segments surrounding the natural phosphorylation sites of phospholipase C-gamma 1 (i.e., tyrosines 472,…”
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Pyrido[2,3-d]pyrimidin-7-ones as Specific Inhibitors of Cyclin-Dependent Kinase 4
Published in Journal of medicinal chemistry (07-04-2005)“…Inhibition of the cell cycle kinase, cyclin-dependent kinase-4 (Cdk4), is expected to provide an effective method for the treatment of proliferative diseases…”
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Structure–activity relationships for 2-anilino-6-phenylpyrido[2,3- d]pyrimidin-7(8 H)-ones as inhibitors of the cellular checkpoint kinase Wee1
Published in Bioorganic & medicinal chemistry letters (01-04-2005)“…2-Anilino-6-phenylpyrido[2,3- d]pyrimidin-7(8 H)-ones are inhibitors of c-Src and Wee1 kinases. Selectivity for c-Src was not markedly changed by 6-phenyl ring…”
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Inhibition of binding of phospholipase C gamma 1 SH2 domains to phosphorylated epidermal growth factor receptor by phosphorylated peptides
Published in International journal of peptide and protein research (01-09-1993)“…A series of tyrosine-containing peptides 1-12: [formula: see text] (six pairs with and without the tyrosine phosphorylated) has been synthesized. The peptides…”
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15
2-Aminoquinazoline inhibitors of cyclin-dependent kinases
Published in Bioorganic & medicinal chemistry letters (01-09-2005)“…The inhibition of cyclin-dependent kinase 4 (Cdk4) causes cell cycle arrest and restores a checkpoint that is absent in the majority of tumor cells. Compounds…”
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Tyrosine kinase inhibitors. I: Structure-activity relationships for inhibition of epidermal growth factor receptor tyrosine kinase activity by 2,3-dihydro-2-thioxo-1H-indole-3-alkanoic acids and 2,2'-dithiobis(1H-indole-3-alkanoic acids)
Published in Journal of medicinal chemistry (1993)Get full text
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Substrates specificity of the protein tyrosine phosphatases
Published in Proceedings of the National Academy of Sciences - PNAS (1993)Get full text
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