2VPP

Drosophila melanogaster deoxyribonucleoside kinase successfully activates gemcitabine in transduced cancer cell lines

2VPP の概要

• エントリーDOI: 10.2210/pdb2vpp/pdb
• 関連するPDBエントリー: 1J90 1OE0 1OT3 1ZM7 1ZMX 2JCS 2VP0 2VP2 2VP4 2VP5 2VP6 2VP9
• 分子名称: DEOXYNUCLEOSIDE KINASE, GEMCITABINE, SULFATE ION, ... (4 entities in total)
• 機能のキーワード: kinase, cancer, transferase, atp-binding, phosphoprotein, nucleoside analogs, nucleotide-binding, structure-function relationship, gemcitabine, gene therapy, dna synthesis
• 由来する生物種: DROSOPHILA MELANOGASTER (FRUIT FLY)
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 54531.94

構造登録者

Knecht, W.,Mikkelsen, N.E.,Clausen, A.,Willer, M.,Gojkovic, Z.,Piskur, J. (登録日: 2008-03-03, 公開日: 2009-03-24, 最終更新日: 2023-12-13)

主引用文献

Knecht, W.,Mikkelsen, N.E.,Clausen, A.,Willer, M.,Eklund, H.,Gojkovic, Z.,Piskur, J.
Drosophila Melanogaster Deoxyribonucleoside Kinase Activates Gemcitabine.
Biochem.Biophys.Res.Commun., 382:430-, 2009

PubMed Abstract: 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.

PubMed: 19285960
DOI: 10.1016/J.BBRC.2009.03.041

実験手法

X-RAY DIFFRACTION (2.2 Å)