The antimalarial drugs chloroquine and primaquine inhibit pyridoxal kinase, an essential enzyme for vitamin B6 production

FEBS Lett. 2014 Oct 16;588(20):3673-6. doi: 10.1016/j.febslet.2014.08.011. Epub 2014 Aug 23.


Quinoline derivatives such as chloroquine and primaquine are widely used for the treatment of malaria. These drugs are also used for the treatment of trypanosomiasis, and more recently for cancer therapy. However, molecular target(s) of these drugs remain unclear. In this study, we have identified human pyridoxal kinase as a binding protein of primaquine. Primaquine inhibited pyridoxal kinases of malaria, trypanosome and human, while chloroquine inhibited only malaria pyridoxal kinase. Thus, we have identified pyridoxal kinase as a possible target molecule of the antimalarial drugs chloroquine and primaquine.

Keywords: Chloroquine; Malaria; Primaquine; Pyridoxal kinase.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimalarials / pharmacology*
  • Chloroquine / pharmacology*
  • Enzyme Inhibitors / pharmacology*
  • HeLa Cells
  • Humans
  • Plasmodium vivax / enzymology
  • Primaquine / pharmacology*
  • Protein Binding
  • Protozoan Proteins / antagonists & inhibitors*
  • Protozoan Proteins / metabolism
  • Pyridoxal Kinase / antagonists & inhibitors*
  • Pyridoxal Kinase / metabolism
  • Substrate Specificity
  • Trypanosoma cruzi / enzymology


  • Antimalarials
  • Enzyme Inhibitors
  • Protozoan Proteins
  • Chloroquine
  • Pyridoxal Kinase
  • Primaquine