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PDBsum entry 2vpp
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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
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Title:
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Drosophila melanogaster deoxyribonucleoside kinase successfully activates gemcitabine in transduced cancer cell lines
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Structure:
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Deoxynucleoside kinase. Chain: a, b. Fragment: residues 1-230. Synonym: deoxyribonucleoside kinase, dm-dnk, multispecific deoxynucleoside kinase. Engineered: yes
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Source:
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Drosophila melanogaster. Fruit fly. Organism_taxid: 7227. Expressed in: escherichia coli. Expression_system_taxid: 511693.
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Resolution:
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2.20Å
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R-factor:
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0.209
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R-free:
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0.253
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Authors:
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W.Knecht,N.E.Mikkelsen,A.Clausen,M.Willer,Z.Gojkovic,J.Piskur
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Key ref:
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W.Knecht
et al.
(2009).
Drosophila melanogaster deoxyribonucleoside kinase activates gemcitabine.
Biochem Biophys Res Commun,
382,
430-433.
PubMed id:
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Date:
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03-Mar-08
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Release date:
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24-Mar-09
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PROCHECK
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Headers
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References
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Q9XZT6
(DNK_DROME) -
Deoxynucleoside kinase from Drosophila melanogaster
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Seq:
Struc:
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250 a.a.
189 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.2.7.1.145
- deoxynucleoside kinase.
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Reaction:
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a 2'-deoxyribonucleoside + ATP = a 2'-deoxyribonucleoside 5'-phosphate + ADP + H+
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2'-deoxyribonucleoside
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+
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ATP
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=
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2'-deoxyribonucleoside 5'-phosphate
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+
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ADP
Bound ligand (Het Group name = )
matches with 45.16% similarity
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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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Biochem Biophys Res Commun
382:430-433
(2009)
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PubMed id:
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Drosophila melanogaster deoxyribonucleoside kinase activates gemcitabine.
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W.Knecht,
N.E.Mikkelsen,
A.R.Clausen,
M.Willer,
H.Eklund,
Z.Gojković,
J.Piskur.
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ABSTRACT
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Drosophila melanogaster multisubstrate deoxyribonucleoside kinase (Dm-dNK) can
additionally sensitize human cancer cell lines towards the anti-cancer drug
gemcitabine. We show that this property is based on the Dm-dNK ability to
efficiently phosphorylate gemcitabine. The 2.2A resolution structure of Dm-dNK
in complex with gemcitabine shows that the residues Tyr70 and Arg105 play a
crucial role in the firm positioning of gemcitabine by extra interactions made
by the fluoride atoms. This explains why gemcitabine is a good substrate for
Dm-dNK.
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Links
