Cloned (Comment) | Organism |
---|---|
expression of SH1, SH2, SH3 domains of isoform ABL, containing residues 65534 | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
additional information | use of the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase AGT to display an ATP-competitive inhibitor and a ligand that targets a secondary binding domain. Systematic analysis of ATP-competitive inhibitors with varying linker lengths reveals that isoforms SRC and ABL have differential sensitivities to ligand presentation. Generation of bivalent constructs that contain ligands with differential affinities for the ATP-binding sites and SH3 domains of SRC and ABL demonstrates the modular nature of inhibitors based on the O6-alkylguanine-DNA alkyltransferase scaffold. The interaction between the SH3 domain ligand and the kinase SH3 domain is the major selectivity determinant amongst closely-related tyrosine kinases; use of the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase AGT to display an ATP-competitive inhibitor and a ligand that targets a secondary binding domain. Systematic analysis of ATP-competitive inhibitors with varying linker lengths reveals that isoforms SRC and ABL have differential sensitivities to ligand presentation. Generation of bivalent constructs that contain ligands with differential affinities for the ATP-binding sites and SH3 domains of SRC and ABL demonstrates the modular nature of inhibitors based on the O6-alkylguanine-DNA alkyltransferase scaffold. The interaction between the SH3 domain ligand and the kinase SH3 domain is the major selectivity determinant amongst closely-related tyrosine kinases | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P00519 | ABL1 | - |
Homo sapiens | P12931 | SRC | - |
Synonyms | Comment | Organism |
---|---|---|
ABL1 | - |
Homo sapiens |
proto-oncogene tyrosine-protein kinase SRC | - |
Homo sapiens |
Src | - |
Homo sapiens |