Nature Communications (Nov 2017)

Dual protein kinase and nucleoside kinase modulators for rationally designed polypharmacology

  • Kahina Hammam,
  • Magali Saez-Ayala,
  • Etienne Rebuffet,
  • Laurent Gros,
  • Sophie Lopez,
  • Berengere Hajem,
  • Martine Humbert,
  • Emilie Baudelet,
  • Stephane Audebert,
  • Stephane Betzi,
  • Adrien Lugari,
  • Sebastien Combes,
  • Sebastien Letard,
  • Nathalie Casteran,
  • Colin Mansfield,
  • Alain Moussy,
  • Paulo De Sepulveda,
  • Xavier Morelli,
  • Patrice Dubreuil

DOI
https://doi.org/10.1038/s41467-017-01582-5
Journal volume & issue
Vol. 8, no. 1
pp. 1 – 11

Abstract

Read online

Masitinib is a protein kinase inhibitor that sensitises refractory pancreatic adenocarcinoma cells to treatment with the nucleoside analog gemcitabine. Here the authors show that Masitinib activates deoxycytidine kinase to enhance phosphorylation of nucleoside analogue pro-drugs, increasing their potency.