Drosophila melanogaster deoxyribonucleoside kinase activates gemcitabine
Author
Summary, in English
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 2.2 angstrom resolution structure of DmdNK 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(. (C) 2009 Elsevier Inc. All rights reserved.
Department/s
Publishing year
2009
Language
English
Pages
430-433
Publication/Series
Biochemical and Biophysical Research Communications
Volume
382
Issue
2
Document type
Journal article
Publisher
Elsevier
Topic
- Biological Sciences
Keywords
- Structure-function relationship
- Salvage pathway
- Cancer
- Gene-therapy
- Nucleoside analogs
- Deoxyribonucleoside kinase
Status
Published
ISBN/ISSN/Other
- ISSN: 1090-2104