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PDBsum entry 4ap7
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PDB id:
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Transferase
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Title:
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Crystal structure of c-met kinase domain in complex with 4-((6-(4- fluorophenyl)-(1,2,4)triazolo(4,3-b)(1,2,4)triazin-3-yl)methyl)phenol
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Structure:
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Hepatocyte growth factor receptor. Chain: a. Fragment: tyrosine kinase domain, unp residues 1051-1348. Synonym: hgf receptor, hgf/sf receptor, proto-oncogenE C-met, scatter factor receptor, sf receptor, tyrosine-protein kinase met. Engineered: yes
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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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1.80Å
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R-factor:
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0.191
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R-free:
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0.214
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Authors:
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M.Mctigue,J.Wickersham
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Key ref:
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J.J.Cui
et al.
(2012).
Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of cancer.
J Med Chem,
55,
8091-8109.
PubMed id:
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Date:
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30-Mar-12
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Release date:
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26-Sep-12
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PROCHECK
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Headers
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References
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P08581
(MET_HUMAN) -
Hepatocyte growth factor receptor from Homo sapiens
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Seq:
Struc:
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1390 a.a.
290 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
55:8091-8109
(2012)
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PubMed id:
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Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of cancer.
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J.J.Cui,
M.McTigue,
M.Nambu,
M.Tran-Dubé,
M.Pairish,
H.Shen,
L.Jia,
H.Cheng,
J.Hoffman,
P.Le,
M.Jalaie,
G.H.Goetz,
K.Ryan,
N.Grodsky,
Y.L.Deng,
M.Parker,
S.Timofeevski,
B.W.Murray,
S.Yamazaki,
S.Aguirre,
Q.Li,
H.Zou,
J.Christensen.
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ABSTRACT
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