Article
Plasmodium falciparum Resistance to a Lead Benzoxaborole Due to Blocked Compound Activation and Altered Ubiquitination or Sumoylation.
mBio - 28 Jan 2020
Sindhe Kirthana M V, Wu Wesley, Legac Jenny, Zhang Yong-Kang, Easom Eric E, Cooper Roland A, Plattner Jacob J, Freund Yvonne R, DeRisi Joseph L, Rosenthal Philip J
Abstract excerpt
New antimalarial drugs are needed. The benzoxaborole AN13762 showed excellent activity against cultured Plasmodium falciparum, against fresh Ugandan P. falciparum isolates, and in murine malaria models. To gain mechanistic insights, we selected in vitro for P. falciparum isolates resistant to AN13762. In all of 11 independent selections with 100 to 200 nM AN13762, the 50% inhibitory concentration (IC50) increased...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.
