A Bioactive Trypanosoma cruzi Bromodomain Inhibitor from Chemically Engineered Extracts.

I Ayelen RamalloVictoria L AlonsoFederico RuaEsteban SerraRicardo Luis Eugenio Furlan

Published in: ACS combinatorial science (2018)

A set of chemically engineered extracts enriched in compounds including N-N and N-O fragments in their structures was prepared. Bromodomain binding screening and bioguided fractionation led to the identification of one oxime hit that interacts with TcBDF3 with affinity in the submicromolar range and that shows interesting antiparasitic properties against the different life cycle stages of T. cruzi.

Keyphrases

life cycle
trypanosoma cruzi
binding protein
dna binding
mass spectrometry