PDBsum entry 2vpp

Transferase

PDB id: 2vpp

Contents

Protein chains

189 a.a.

Ligands

GEO ×2

SO4 ×2

Waters ×239

References listed in PDB file

Key reference

• Title: Drosophila melanogaster deoxyribonucleoside kinase activates gemcitabine.
• Authors: W.Knecht, N.E.Mikkelsen, A.R.Clausen, M.Willer, H.Eklund, Z.Gojković, J.Piskur.
• Ref.: Biochem Biophys Res Commun, 2009, 382, 430-433.
• PubMed id: 19285960

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.