Brand  (β version)

PDB ID: 3OXZ

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Ligands
Code Name Style Show Link
0LI 3-(imidazo[1,2-B]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzam ide PoSSuM
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Structure summary

Code : 3OXZ   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE/TRANSFERASE INHIBITOR
Title : Crystal structure of ABL kinase domain bound with a DFG-out inhibitor AP24534
Release Data : 2010-12-15
Compound :
mol_id molecule chains synonym
1 Tyrosine-protein kinase ABL1 A Abelson murine leukemia viral oncogene homolog 1, Proto-oncogene c-Abl, p150
ec: 2.7.10.2
fragment: UNP residues 229-511
Source :
mol_id organism_scientific organism_common expression_system
1 Mus musculus  (taxid:10090) Mouse Escherichia coli  (taxid:562)
gene: Abl1, Abl
Authors : Zhou, T., Huang, W.S., Wang, Y., Thomas, M., Keats, J., Xu, Q., Rivera, V., Shakespeare, W.C., Clackson, T., Dalgarno, D.C., Zhu, X.
Keywords : protein-inhibitor complex, protein kinase two-domain fold, phosphotransferase, ATP binding, phosphorylation, TRANSFERASE-TRANSFERASE INHIBITOR complex
Exp. method : X-RAY DIFFRACTION ( 2.2000 Å )
Citation :

Structural Mechanism of the Pan-BCR-ABL Inhibitor Ponatinib (AP24534): Lessons for Overcoming Kinase Inhibitor Resistance.

Zhou, T.,Commodore, L.,Huang, W.S.  et al.
(2011)  Chem.Biol.Drug Des.  77 : 1 - 11

PubMed: 21118377
DOI: 10.1111/j.1747-0285.2010.01054.x

Reaction

Chain : A
UniProt : P00520 (ABL1_MOUSE)
Reaction: EC: Evidence:
Physiological Direction:
ATP + L-tyrosyl-[protein] = ADP + H(+) + O-phospho-L-tyrosyl- [protein] 2.7.10.2 PROSITE-ProRule:PRU10028, PubMed:10988075, PubMed:12748290, PubMed:19878872, PubMed:20072125
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