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Literature summary for 2.7.10.2 extracted from

  • Hill, Z.B.; Perera, B.G.; Maly, D.J.
    Bivalent inhibitors of the tyrosine kinases ABL and SRC: determinants of potency and selectivity (2011), Mol. Biosyst., 7, 447-456.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.10.2

Cloned(Commentary)

Cloned (Comment) Organism
expression of SH1, SH2, SH3 domains of isoform ABL, containing residues 65–534 Homo sapiens

Inhibitors

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

Organism UniProt Comment Textmining
Homo sapiens P00519 ABL1
-
Homo sapiens P12931 SRC
-

Synonyms

Synonyms Comment Organism
ABL1
-
 Homo sapiens
proto-oncogene tyrosine-protein kinase SRC
-
 Homo sapiens
Src
-
 Homo sapiens