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PDBsum entry 2xp2
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Contents |
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* Residue conservation analysis
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PDB id:
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Transferase
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Title:
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Structure of the human anaplastic lymphoma kinase in complex with crizotinib (pf-02341066)
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Structure:
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Tyrosine-protein kinase receptor. Chain: a. Fragment: tyrosine kinase domain, residues 105-423. Synonym: anaplastic lymphoma kinase. Engineered: yes. Other_details: nonphosphorylated
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Source:
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Homo sapiens. Human. Organism_taxid: 9606. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108. Expression_system_cell_line: sf9.
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Resolution:
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1.90Å
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R-factor:
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0.207
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R-free:
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0.252
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Authors:
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M.Mctigue,Y.Deng,W.Liu,A.Brooun,S.Timofeevski,T.Marrone,J.J.Cui
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Key ref:
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J.J.Cui
et al.
(2011).
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).
J Med Chem,
54,
6342-6363.
PubMed id:
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Date:
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24-Aug-10
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Release date:
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15-Sep-10
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PROCHECK
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Headers
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References
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Q9UM73
(ALK_HUMAN) -
ALK tyrosine kinase receptor from Homo sapiens
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Seq:
Struc:
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1620 a.a.
289 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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Enzyme class:
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E.C.2.7.10.1
- receptor 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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J Med Chem
54:6342-6363
(2011)
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PubMed id:
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Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).
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J.J.Cui,
M.Tran-Dubé,
H.Shen,
M.Nambu,
P.P.Kung,
M.Pairish,
L.Jia,
J.Meng,
L.Funk,
I.Botrous,
M.McTigue,
N.Grodsky,
K.Ryan,
E.Padrique,
G.Alton,
S.Timofeevski,
S.Yamazaki,
Q.Li,
H.Zou,
J.Christensen,
B.Mroczkowski,
S.Bender,
R.S.Kania,
M.P.Edwards.
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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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D.R.Camidge,
and
R.C.Doebele
(2012).
Treating ALK-positive lung cancer--early successes and future challenges.
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Nat Rev Clin Oncol,
9,
268-277.
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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
