Brand  (β version)

PDB ID: 3IK3

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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 : 3IK3   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE
Title : AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance
Release Data : 2009-11-03
Compound :
mol_id molecule chains synonym
1 Proto-oncogene tyrosine-protein kinase ABL1 A,B Abelson murine leukemia viral oncogene homolog 1, c-ABL, p150
ec: 2.7.10.2
mutation: T315I
Source :
mol_id organism_scientific organism_common expression_system
1 Mus musculus  (taxid:10090) Mouse Escherichia coli BL21(DE3)  (taxid:469008)
gene: Abl1, Abl
expression_system_strain: BL21DE3
expression_system_vector_type: Plasmid
Authors : Zhou, T.
Keywords : Bcr-Abl, CML, T315I, inhibitor, mutation, drug resistance, Alternative splicing, ATP-binding, Cell adhesion, Chromosomal rearrangement, Cytoplasm, Cytoskeleton, Kinase, Lipoprotein, Magnesium, Manganese, Metal-binding, Myristate, Nucleotide-binding, Nucleus, Phosphoprotein, Proto-oncogene, SH2 domain, SH3 domain, Transferase
Exp. method : X-RAY DIFFRACTION ( 1.900 Å )
Citation :

AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance.

O'Hare, T.,Shakespeare, W.C.,Zhu, X.  et al.
(2009)  Cancer Cell  16 : 401 - 412

PubMed: 19878872
DOI: 10.1016/j.ccr.2009.09.028

Reaction

Chain : A, B
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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