Diversity-oriented synthesis yields novel multistage antimalarial inhibitors

N Kato, E Comer, T Sakata-Kato, A Sharma, M Sharma… - Nature, 2016 - nature.com
Antimalarial drugs have thus far been chiefly derived from two sources—natural products
and synthetic drug-like compounds. Here we investigate whether antimalarial agents with …

Mapping the malaria parasite druggable genome by using in vitro evolution and chemogenomics

…, MG Gomez-Lorenzo, M Vanaerschot, T Sakata-Kato… - Science, 2018 - science.org
Chemogenetic characterization through in vitro evolution combined with whole-genome
analysis can identify antimalarial drug targets and drug-resistance genes. We performed a …

Open-source discovery of chemical leads for next-generation chemoprotective antimalarials

…, MR Luth, S Ottilie, AK Lukens, T Sakata-Kato… - Science, 2018 - science.org
INTRODUCTION Malaria remains a devastating disease, affecting 216 million people annually,
with 445,000 deaths occurring primarily in children under 5 years old. Malaria treatment …

[HTML][HTML] A broad analysis of resistance development in the malaria parasite

…, P Magistrado, O Coburn-Flynn, T Sakata-Kato… - Nature …, 2016 - nature.com
Microbial resistance to chemotherapy has caused countless deaths where malaria is
endemic. Chemotherapy may fail either due to pre-existing resistance or evolution of drug-resistant …

Control of inflammation by stromal Hedgehog pathway activation restrains colitis

…, WJ Lu, K Shin, T Sakata-Kato… - Proceedings of the …, 2016 - National Acad Sciences
Inflammation disrupts tissue architecture and function, thereby contributing to the
pathogenesis of diverse diseases; the signals that promote or restrict tissue inflammation thus …

Mutations in the P-type cation-transporter ATPase 4, PfATP4, mediate resistance to both aminopyrazole and spiroindolone antimalarials

EL Flannery, CW McNamara, SW Kim… - ACS chemical …, 2015 - ACS Publications
Aminopyrazoles are a new class of antimalarial compounds identified in a cellular antiparasitic
screen with potent activity against Plasmodium falciparum asexual and sexual stage …

[PDF][PDF] Structural basis for blocking sugar uptake into the malaria parasite Plasmodium falciparum

…, Q Tang, K Hirata, X Yang, Y Jiao, T Sakata-Kato… - Cell, 2020 - cell.com
Plasmodium species, the causative agent of malaria, rely on glucose for energy supply
during blood stage. Inhibition of glucose uptake thus represents a potential strategy for the …

Advances in malaria pharmacology and the online guide to MALARIA PHARMACOLOGY: IUPHAR review 38

…, M Rawat, F Rocamora, T SakataKato… - British Journal of …, 2023 - Wiley Online Library
Antimalarial drug discovery has until recently been driven by high‐throughput phenotypic
cellular screening, allowing millions of compounds to be assayed and delivering clinical drug …

[PDF][PDF] The Plasmodium falciparum ABC transporter ABCI3 confers parasite strain-dependent pleiotropic antimalarial drug resistance

…, O Coburn-Flynn, ES Istvan, T Sakata-Kato… - Cell chemical …, 2022 - cell.com
Widespread Plasmodium falciparum resistance to first-line antimalarials underscores the vital
need to develop compounds with novel modes of action and identify new druggable targets…

In vitro selection predicts malaria parasite resistance to dihydroorotate dehydrogenase inhibitors in a mouse infection model

…, MJ Lafuente-Monasterio, T Sakata-Kato… - Science translational …, 2019 - science.org
Resistance has developed in Plasmodium malaria parasites to every antimalarial drug in
clinical use, prompting the need to characterize the pathways mediating resistance. Here, we …