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PDBsum entry 3qri
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Transferase/transferase inhibitor
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PDB id
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3qri
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PDB id:
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Transferase/transferase inhibitor
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Title:
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The crystal structure of human abl1 kinase domain in complex with dcc- 2036
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Structure:
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Tyrosine-protein kinase abl1. Chain: a, b. Fragment: kinase domain, unp residues 229-499. Synonym: abelson murine leukemia viral oncogene homolog 1, proto- oncogenE C-abl, p150. Engineered: yes
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Source:
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Homo sapiens. Human. Organism_taxid: 9606. Gene: abl1, abl, jtk7. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108. Expression_system_cell_line: sf9.
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Resolution:
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2.10Å
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R-factor:
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0.216
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R-free:
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0.272
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Authors:
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W.W.Chan,S.C.Wise,M.D.Kaufman,Y.M.Ahn,C.L.Ensinger,T.Haack,M.M.Hood, J.Jones,J.W.Lord,W.P.Lu,D.Miller,W.C.Patt,B.D.Smith,P.A.Petillo, T.J.Rutkoski,H.Telikepalli,L.Vogeti,T.Yao,L.Chun,R.Clark, P.Evangelista,L.C.Gavrilescu,K.Lazarides,V.M.Zaleskas,L.J.Stewart, R.A.Van Etten,D.L.Flynn
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Key ref:
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W.W.Chan
et al.
(2011).
Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036.
Cancer Cell,
19,
556-568.
PubMed id:
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Date:
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18-Feb-11
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Release date:
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01-Jun-11
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PROCHECK
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Headers
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References
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P00519
(ABL1_HUMAN) -
Tyrosine-protein kinase ABL1 from Homo sapiens
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Seq:
Struc:
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1130 a.a.
275 a.a.*
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Key: |
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PfamA domain |
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Secondary structure |
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CATH domain |
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*
PDB and UniProt seqs differ
at 5 residue positions (black
crosses)
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Enzyme class:
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E.C.2.7.10.2
- non-specific protein-tyrosine kinase.
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Reaction:
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L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H+
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L-tyrosyl-[protein]
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+
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ATP
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=
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O-phospho-L-tyrosyl-[protein]
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+
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ADP
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+
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H(+)
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Molecule diagrams generated from .mol files obtained from the
KEGG ftp site
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Cancer Cell
19:556-568
(2011)
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PubMed id:
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Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036.
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W.W.Chan,
S.C.Wise,
M.D.Kaufman,
Y.M.Ahn,
C.L.Ensinger,
T.Haack,
M.M.Hood,
J.Jones,
J.W.Lord,
W.P.Lu,
D.Miller,
W.C.Patt,
B.D.Smith,
P.A.Petillo,
T.J.Rutkoski,
H.Telikepalli,
L.Vogeti,
T.Yao,
L.Chun,
R.Clark,
P.Evangelista,
L.C.Gavrilescu,
K.Lazarides,
V.M.Zaleskas,
L.J.Stewart,
R.A.Van Etten,
D.L.Flynn.
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ABSTRACT
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Literature references that cite this PDB file's key reference
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PubMed id
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Reference
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L.Packer,
and
R.Marais
(2011).
Unswitch-ABL drugs overcome resistance in chronic myeloid leukemia.
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Cancer Cell,
19,
435-437.
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The most recent references are shown first.
Citation data come partly from CiteXplore and partly
from an automated harvesting procedure. Note that this is likely to be
only a partial list as not all journals are covered by
either method. However, we are continually building up the citation data
so more and more references will be included with time.
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Links
