Researchers report the development of a small molecule that treated visceral leishmaniasis, a neglected parasitic tropical disease that kills 20,000¬-40,000 people annually, in a mouse model, with pharmacokinetic properties favorable to oral dosing and no significant safety or tolerability issues; the compound, which is currently advancing toward human clinical trials, selectively inhibited the chymotrypsin-like activity of the proteasome, the cellular protein recycling machine, by binding to a previously undiscovered inhibitor site.
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Article #18-20175: "Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition," by Susan Wyllie et al.
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Journal
Proceedings of the National Academy of Sciences