Inclusion of transmission-blocking agents in combination therapies for malaria could help eliminate the disease. Through a screen of compounds from the Novartis-GNF Malaria Box, Vanaerschot et al. identify hexahydroquinolines (HHQs) as potent Plasmodium falciparum (Pf) gametocyte (GAM) and asexual blood stage inhibitors. Transmission-blocking activity of HHQs was confirmed in in vitro assays using Pf GAMs and gametes. In Plasmodium berghei-infected mice, HHQs suppressed blood-stage parasite proliferation. In vitro HHQ resistance selection studies identified mutations in Pf multidrug resistance gene-1, which sensitized parasites to first-line antimalarial drugs.
References
Vanaerschot, M. et al. Hexahydroquinolines are antimalarial candidates with potent blood-stage and transmission-blocking activity. Nat. Microbiol. http://dx.doi.org/10.1038/s41564-017-0007-4 (2017)
Rights and permissions
About this article
Cite this article
Crunkhorn, S. Blocking malaria transmission. Nat Rev Drug Discov 16, 680 (2017). https://doi.org/10.1038/nrd.2017.184
Published:
Issue Date:
DOI: https://doi.org/10.1038/nrd.2017.184