EC Number |
Application |
Reference |
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2.7.10.2 | analysis |
development of a protein chip consisting of a silicone elastomer microwell array with recombinant enzyme covalently attached to the wells via a 3-glycidoxypropyltrimethoxysilane crosslinker for large scale activity assay, overview |
662926 |
2.7.10.2 | analysis |
peptide photoaffinity probe GAPEVIYA-4-azidophenylalanyl-PGAKKKGK(biotin) based on consensus substrate GAPEVIYATPGAKKK. Incubation of purified recombinant isoform Abl results in covalent incorporation of biotin. The label crosslinks to Abl specifically through binding to the active site cleft into the kinase. Abl activity is enhanced by phosphorylation at multiple sites, the extent of labeling increases with increasing catalytic activity |
722050 |
2.7.10.2 | analysis |
SH2 domain-based tyrosine kinase assay using biotin ligase modified with a terbium(III) complex. An SH2 domain from lymphocyte-specific tyrosine kinase is genetically fused to a truncated biotin carboxyl carrier protein, and the resulting fusion protein is labeled through biotinylation with biotin protein ligase carrying multiple copies of a luminescent Tb3+ complex. The labeled SH2 fusion proteins are employed to detect a phosphorylated peptide immobilized on the surface of the microtiter plate, where the phosphorylated peptide is produced by phosphorylation to the substrate peptide by Src tyrosine kinase. The assay allows for a reliable determination of the activity of Src kinase lower than 10 ng/mL |
723946 |
2.7.10.2 | analysis |
the fluorescence properties of bosutinib and related compounds allow inhibitor binding to be measured quantitatively, and the infrared absorption of the nitrile group reveals a different electrostatic environment in the conserved ATP-binding sites of Abl and Src kinases |
723547 |
2.7.10.2 | drug development |
JAK2 is a target for drug development, specific inhibitors are of tremendous clinical relevance |
661392 |
2.7.10.2 | drug development |
non-receptor PTKs are targets for design by computational chemistry of therapeutic agents based on plant-derived inhibitors from ethnopharmaceutical knowledge, high-throughput screening, tyrosine kinase inhibitors can target the ATP or the substrate binding sites, respectively, strategies, detailed overview |
661540 |
2.7.10.2 | drug development |
PTKS are key targets for anticancer drug discovery |
661396 |
2.7.10.2 | drug development |
the enzyme is a target for development and evaluation of tyrosine kinase inhibitors |
672787 |
2.7.10.2 | drug development |
tyrosine kinase Src is a key enzyme in mammalian signal transduction and an important target for anticancer drug discovery |
672104 |
2.7.10.2 | medicine |
aberrant Src kinase activity is associated with the invasive phenotype in both early and advanced solid tumors |
691297 |