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Title: A new quinoxaline-containing peptide induces apoptosis in cancer cells by autophagy modulation
Author: Zamudio Vázquez, Rubí
Ivanova, Saska
Moreno, Miguel
Hernández-Alvarez, María Isabel
Giralt Lledó, Ernest
Bidon-Chanal Badia, Axel
Zorzano Olarte, Antonio
Albericio Palomera, Fernando
Tulla-Puche, Judit
Keywords: Quinoxalina
Ressonància magnètica nuclear
Síntesi en fase sólida
Química combinatòria
Nuclear magnetic resonance
Solid-phase synthesis
Combinatorial chemistry
Issue Date: 20-May-2015
Publisher: Royal Society of Chemistry
Abstract: The synthesis of a new small library of quinoxaline-containing peptides is described. After cytotoxic evaluation in four human cancer cell lines, as well as detailed biological studies, it was found that the most active compound, RZ2, promotes the formation of acidic compartments, where it accumulates, blocking the progression of autophagy. Further disruption of the mitochondrial membrane potential and an increase in mitochondrial ROS was observed, causing cells to undergo apoptosis. Given its cytotoxic activity and protease-resistant features, RZ2 could be a potential drug candidate for cancer treatment and provide a basis for future research into the crosstalk between autophagy and apoptosis and its relevance in cancer therapy.
Note: Reproducció del document publicat a:
It is part of: Chemical Science, 2015, num. 6, p. 4537-4549
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ISSN: 2041-6520
Appears in Collections:Articles publicats en revistes (Química Inorgànica i Orgànica)
Articles publicats en revistes (Nutrició, Ciències de l'Alimentació i Gastronomia)

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