Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Infectious disease

Malaria

Plasmodium phosphatidylinositol 4-kinase IIIb (Plasmodium PI4KIIIb)

In vitro and in vivo studies suggest targeting Plasmodium PI4KIIIb could help treat malaria. In cell-, mouse- or rhesus macaque-based assays monitoring different stages of the Plasmodium life cycle, optimized imidazopyrazine compounds killed liver stage, asexual blood stage and sexual stage Plasmodium species. Genetic and biochemical analysis showed that the compounds inhibited Plasmodium PI4KIIIb but not related human proteins. Next steps include further improving the potency of Plasmodium PI4KIIIb inhibitors and testing them in rhesus macaques (see Lipid kinase enters the malaria stage, page 8).

SciBX 6(48); doi:10.1038/scibx.2013.1393
Published online Dec. 19, 2013

Patent application filed by Novartis AG covering the compounds; unavailable for licensing

McNamara, C.W. et al. Nature;
published online Nov. 27, 2013;
doi:10.1038/nature12782
Contact: Elizabeth A. Winzeler, University of California, San Diego,
La Jolla, Calif.
e-mail:
ewinzeler@ucsd.edu

Contact: Thierry T. Diagana, Novartis Institute for Tropical Diseases, Singapore

e-mail:
thierry.diagana@novartis.com