BioCentury
ARTICLE | Discovery & Translation

Killing malaria at any life cycle stage; plus GSK’s primate plague data and more

BioCentury’s roundup of translational news

June 4, 2022 12:22 AM UTC

University of Melbourne-led team published a molecule in Science that inhibited growth of the malaria parasite Plasmodium falciparum at all stages of its life cycle, a feat that has eluded most therapeutic programs. The compound works by blocking protein translation, a process fundamental to all life cycle stages, and it led to no apparent toxicity in mammalian cell lines or mice engrafted with P. falciparum–infected human red blood cells, potentially due to structural differences in its target, tyrosine–transfer RNA synthetase, between species. The compound, named ML901, is a covalent, nucleophilic sulfamate that inhibits the parasite with an IC50_72h of 2.0 ± 0.1 nM.

ML901 was discovered by screening 2,314 sulfamates from a  Takeda Pharmaceutical Co. Ltd. (Tokyo:4502; NYSE:TAK) compound library. ML901 is patented by Millennium Pharmaceuticals Inc., which Takeda acquired in 2008...