RT Journal Article
T1 Functional screening of selective mitochondrial inhibitors of Plasmodium
A1 Gómez Lorenzo, María G.
A1 Rodríguez Alejandre, Ane
A1 Moliner Cubel, Sonia
A1 Martínez Hoyos, María
A1 Bahamontes Rosa, Noemí
A1 González Del Río, Rubén
A1 Ródenas, Carolina
A1 De La Fuente, Jesús
A1 Lavandera, José Luis
A1 García Bustos, José F.
A1 Mendoza Losana, Alfonso
AB Phenotypic screening has produced most of the new chemical entities currently in clinical development for malaria, plus many lead compounds active against Plasmodium falciparum asexual stages. However, lack of knowledge about the mode of action of these compounds delays and may even hamper their future development. Identifying the mode of action of the inhibitors greatly helps to prioritise compounds for further development as novel antimalarials. Here we describe a whole-cell method to detect inhibitors of the mitochondrial electron transport chain, using oxygen consumption as high throughput readout in 384-well plate format. The usefulness of the method has been confirmed with the Tres Cantos Antimalarial Compound Set (TCAMS). The assay identified 124 respiratory inhibitors in TCAMS, seven of which were novel anti-plasmodial chemical structures never before described as mitochondrial inhibitors.
PB Elsevier BV
SN 2211-3207
YR 2018
FD 2018-05-15
LK https://hdl.handle.net/10016/39559
UL https://hdl.handle.net/10016/39559
LA eng
DS e-Archivo
RD 1 sept. 2024