A Bioactive Trypanosoma cruzi Bromodomain Inhibitor from Chemically Engineered Extracts

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.

Palabras clave: bromodomain inhibitor , Chagas disease , chemically engineered extracts , oxime

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Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution-NonCommercial-ShareAlike 2.5 Unported (CC BY-NC-SA 2.5)

Identificadores

URI: http://hdl.handle.net/11336/94033

DOI: http://dx.doi.org/10.1021/acscombsci.7b00172

URL: https://pubs.acs.org/doi/10.1021/acscombsci.7b00172

Colecciones

Articulos (IIDEFAR)
Articulos de INSTITUTO DE INVESTIGACIONES PARA EL DESCUBRIMIENTO DE FARMACOS DE ROSARIO

Articulos(IBR)
Articulos de INST.DE BIOLOGIA MOLECULAR Y CELULAR DE ROSARIO

Articulos(IICAR)
Articulos de INST. DE INVESTIGACIONES EN CIENCIAS AGRARIAS DE ROSARIO

Citación

Ramallo, Ivana Ayelen; Alonso, Victoria Lucia; Rúa, Federico; Serra, Esteban Carlos; Furlan, Ricardo Luis Eugenio; A Bioactive Trypanosoma cruzi Bromodomain Inhibitor from Chemically Engineered Extracts; American Chemical Society; ACS Combinatorial Science; 20; 4; 4-2018; 220-228

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