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PDBsum entry 3eoc
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Transferase/cell cycle
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PDB id
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3eoc
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Contents |
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* Residue conservation analysis
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PDB id:
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| Name: |
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Transferase/cell cycle
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Title:
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Cdk2/cyclina complexed with a imidazo triazin-2-amine
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Structure:
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Cell division protein kinase 2. Chain: a, c. Synonym: p33 protein kinase. Engineered: yes. Cyclin-a2. Chain: b, d. Fragment: proteolytic fragment: residues 173-432. Synonym: cyclin-a. Engineered: yes
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Source:
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Homo sapiens. Organism_taxid: 9606. Gene: cdk2. Expressed in: spodoptera frugiperda. Gene: ccna2, ccn1, ccna. Expressed in: escherichia coli.
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Resolution:
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3.20Å
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R-factor:
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0.216
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R-free:
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0.238
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Authors:
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M.Cheung,K.Kuntz,M.Pobanz,J.Salovich,B.Wilson,W.Andrews,L.Shewchuk, A.Epperly,D.Hassler,M.Leesnitzer,J.Smith,G.Smith,T.Lansing,R.Mook
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Key ref:
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M.Cheung
et al.
(2008).
Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1.
Bioorg Med Chem Lett,
18,
6214-6217.
PubMed id:
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Date:
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26-Sep-08
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Release date:
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04-Nov-08
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PROCHECK
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Headers
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References
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Enzyme class:
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Chains A, C:
E.C.2.7.11.22
- cyclin-dependent kinase.
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Reaction:
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1.
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L-seryl-[protein] + ATP = O-phospho-L-seryl-[protein] + ADP + H+
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2.
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L-threonyl-[protein] + ATP = O-phospho-L-threonyl-[protein] + ADP + H+
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L-seryl-[protein]
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+
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ATP
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=
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O-phospho-L-seryl-[protein]
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+
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ADP
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+
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H(+)
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L-threonyl-[protein]
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+
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ATP
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=
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O-phospho-L-threonyl-[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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Bioorg Med Chem Lett
18:6214-6217
(2008)
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PubMed id:
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Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1.
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M.Cheung,
K.W.Kuntz,
M.Pobanz,
J.M.Salovich,
B.J.Wilson,
C.W.Andrews,
L.M.Shewchuk,
A.H.Epperly,
D.F.Hassler,
M.A.Leesnitzer,
J.L.Smith,
G.K.Smith,
T.J.Lansing,
R.A.Mook.
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ABSTRACT
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The synthesis and biological activities of imidazo[5,1-f][1,2,4]triazin-2-amines
(imidazotriazines) as novel polo-like kinase 1 inhibitors are reported.
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Links
