Activity Comparison of Epigenetic Modulators against the Hemoprotozoan Parasites Babesia divergens and Plasmodium falciparum. Academic Article uri icon

Overview

abstract

  • 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 Babesia infections. As epigenetic regulation is a promising target for new antiparasitic drugs, we screened 324 epigenetic inhibitors against Babesia divergens 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 Babesia divergens and Plasmodium falciparum 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.

publication date

  • February 18, 2021

Research

keywords

  • Babesia
  • Babesiosis
  • Parasites

Identity

PubMed Central ID

  • PMC9022219

Scopus Document Identifier

  • 85102039109

Digital Object Identifier (DOI)

  • 10.1021/acsinfecdis.0c00853

PubMed ID

  • 33599488

Additional Document Info

volume

  • 7

issue

  • 8