Activity Comparison of Epigenetic Modulators against the Hemoprotozoan Parasites and .

ACS Infect Dis

Department of Microbiology & Immunology, Weill Cornell Medicine, New York, New York 10065, United States.

Published: August 2021

Babesiosis is a tick-borne parasitic disease of humans and livestock that has dramatically increased in frequency and geographical range over the past few decades. Infection of cattle often causes large economic losses, and human infection can be fatal in immunocompromised patients. Unlike for malaria, another disease caused by hemoprotozoan parasites, limited treatment options exist for infections. As epigenetic regulation is a promising target for new antiparasitic drugs, we screened 324 epigenetic inhibitors against blood stages and identified 75 (23%) and 17 (5%) compounds that displayed ≥90% inhibition at 10 and 1 μM, respectively, including over a dozen compounds with activity in the low nanomolar range. We observed differential activity of some inhibitor classes against and parasites and identified pairs of compounds with a high difference in activity despite a high similarity in chemical structure, highlighting new insights into the development of epigenetic inhibitors as antiparasitic drugs.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9022219PMC
http://dx.doi.org/10.1021/acsinfecdis.0c00853DOI Listing

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