Tomoyo Sakata

TL;DR: A targeted gene-disruption approach demonstrated that pfcdpk1 seems to be essential for parasite viability, and an in vitro biochemical screen using recombinant PfCDPK1 against a library of 20,000 compounds resulted in the identification of a series of structurally related 2,6,9-trisubstituted purines.

TL;DR: This review will concentrate on how genome-wide, systems biology approaches may be used following whole organism, cell-based screening to understand the mechanism of drug action or to identify biological targets of small molecules for chemotherapeutics of protozoan parasites.

TL;DR: A systematic SAR study resulted in the identification of compound 40 which exhibits good potency against both wild-type and drug resistant parasites and exhibits good in vivo pharmacokinetic properties.

TL;DR: In this paper, the authors used a cell-based Plasmodium falciparum proliferation assay to discover a pan-kinase inhibitor scaffold as a hit and further optimized this series led to a novel benzamide scaffold which was devoid of human kinase activity while retaining its antiplasmodial activity.