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PDBsum entry 4c7t
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PDB id:
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Transferase
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Title:
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Focal adhesion kinase catalytic domain in complex with a diarylamino- 1,3,5-triazine inhibitor
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Structure:
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Focal adhesion kinase 1. Chain: a. Fragment: kinase domain, residues 411-686. Synonym: fadk 1, focal adhesion kinase-related nonkinase, frnk, p41/p43frnk, protein-tyrosine kinase 2, p125fak, pp125fak, focal adhesion kinase. Engineered: yes
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Source:
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Gallus gallus. Chicken. Organism_taxid: 9031. Expressed in: trichoplusia ni. Expression_system_taxid: 7111. Expression_system_cell_line: high five.
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Resolution:
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2.05Å
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R-factor:
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0.220
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R-free:
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0.246
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Authors:
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J.Le Coq,D.Lietha
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Key ref:
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P.Dao
et al.
(2014).
Inhibition of both focal adhesion kinase and fibroblast growth factor receptor 2 pathways induces anti-tumor and anti-angiogenic activities.
Cancer Lett,
348,
88-99.
PubMed id:
DOI:
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Date:
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25-Sep-13
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Release date:
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02-Apr-14
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PROCHECK
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Headers
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References
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Q00944
(FAK1_CHICK) -
Focal adhesion kinase 1 from Gallus gallus
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Seq:
Struc:
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1053 a.a.
259 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.2.7.10.2
- 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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DOI no:
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Cancer Lett
348:88-99
(2014)
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PubMed id:
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Inhibition of both focal adhesion kinase and fibroblast growth factor receptor 2 pathways induces anti-tumor and anti-angiogenic activities.
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P.Dao,
R.Jarray,
N.Smith,
Y.Lepelletier,
J.Le Coq,
D.Lietha,
R.Hadj-Slimane,
J.P.Herbeuval,
C.Garbay,
F.Raynaud,
H.Chen.
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ABSTRACT
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FAK and FGFR2 signaling pathways play important roles in cancer development,
progression and tumor angiogenesis. PHM16 is a novel ATP competitive inhibitor
of FAK and FGFR2. To evaluate the therapeutic efficacy of this agent, we
examined its anti-angiogenic effect in HUVEC and its anti-tumor effect in
different cancer cell lines. We showed PHM16 inhibited endothelial cell
viability, adherence and tube formation along with the added ability to induce
endothelial cell apoptosis. This compound significantly delayed tumor cell
growth. Together, these data showed that inhibition of both FAK and FGFR2
signaling pathways can enhance anti-tumor and anti-angiogenic activities.
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