Mimicking phosphorylation of Ser-74 on human deoxycytidine kinase selectively increases catalytic activity for dC and dC analogues

FEBS Lett. 2008 Mar 5;582(5):720-4. doi: 10.1016/j.febslet.2008.01.048. Epub 2008 Feb 5.

Abstract

Intracellular phosphorylation of dCK on Ser-74 results in increased nucleoside kinase activity. We mimicked this phosphorylation by a Ser-74-Glu mutation in bacterially produced dCK and investigated kinetic parameters using various nucleoside substrates. The S74E mutation increases the k(cat) values 11-fold for dC, and 3-fold for the anti-cancer analogues dFdC and AraC. In contrast, the rate is decreased for the purine substrates. In HEK293 cells, we found that by comparing transiently transfected dCK(S74E)-GFP and wild-type dCK-GFP, mimicking the phosphorylation of Ser-74 has no effect on cellular localisation. We note that phosphorylation may represent a mechanism to enhance the catalytic activity of the relatively slow dCK enzyme.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Active Transport, Cell Nucleus
  • Catalysis
  • Cell Line
  • Cell Nucleus / enzymology
  • Deoxycytidine / analogs & derivatives*
  • Deoxycytidine / metabolism*
  • Deoxycytidine Kinase / chemistry
  • Deoxycytidine Kinase / metabolism*
  • Humans
  • Intracellular Space / enzymology
  • Kinetics
  • Molecular Mimicry*
  • Mutant Proteins / metabolism
  • Phosphorylation
  • Phosphoserine / metabolism*
  • Protein Structure, Secondary
  • Protein Transport
  • Substrate Specificity

Substances

  • Mutant Proteins
  • Deoxycytidine
  • Phosphoserine
  • Deoxycytidine Kinase