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A new quinoxaline-containing peptide induces apoptosis in cancer cells by autophagy modulation
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 accumulat...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Royal Society of Chemistry
2015
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5666514/ https://www.ncbi.nlm.nih.gov/pubmed/29142702 http://dx.doi.org/10.1039/c5sc00125k |
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author | Zamudio-Vázquez, Rubí Ivanova, Saška Moreno, Miguel Hernandez-Alvarez, Maria Isabel Giralt, Ernest Bidon-Chanal, Axel Zorzano, Antonio Albericio, Fernando Tulla-Puche, Judit |
author_facet | Zamudio-Vázquez, Rubí Ivanova, Saška Moreno, Miguel Hernandez-Alvarez, Maria Isabel Giralt, Ernest Bidon-Chanal, Axel Zorzano, Antonio Albericio, Fernando Tulla-Puche, Judit |
author_sort | Zamudio-Vázquez, Rubí |
collection | PubMed |
description | 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. |
format | Online Article Text |
id | pubmed-5666514 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2015 |
publisher | Royal Society of Chemistry |
record_format | MEDLINE/PubMed |
spelling | pubmed-56665142017-11-15 A new quinoxaline-containing peptide induces apoptosis in cancer cells by autophagy modulation Zamudio-Vázquez, Rubí Ivanova, Saška Moreno, Miguel Hernandez-Alvarez, Maria Isabel Giralt, Ernest Bidon-Chanal, Axel Zorzano, Antonio Albericio, Fernando Tulla-Puche, Judit Chem Sci Chemistry 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. Royal Society of Chemistry 2015-08-01 2015-05-20 /pmc/articles/PMC5666514/ /pubmed/29142702 http://dx.doi.org/10.1039/c5sc00125k Text en This journal is © The Royal Society of Chemistry 2015 https://creativecommons.org/licenses/by/3.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution 3.0 Unported License (http://creativecommons.org/licenses/by/3.0/ (https://creativecommons.org/licenses/by/3.0/) ) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Chemistry Zamudio-Vázquez, Rubí Ivanova, Saška Moreno, Miguel Hernandez-Alvarez, Maria Isabel Giralt, Ernest Bidon-Chanal, Axel Zorzano, Antonio Albericio, Fernando Tulla-Puche, Judit A new quinoxaline-containing peptide induces apoptosis in cancer cells by autophagy modulation |
title | A new quinoxaline-containing peptide induces apoptosis in cancer cells by autophagy modulation
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title_full | A new quinoxaline-containing peptide induces apoptosis in cancer cells by autophagy modulation
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title_fullStr | A new quinoxaline-containing peptide induces apoptosis in cancer cells by autophagy modulation
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title_full_unstemmed | A new quinoxaline-containing peptide induces apoptosis in cancer cells by autophagy modulation
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title_short | A new quinoxaline-containing peptide induces apoptosis in cancer cells by autophagy modulation
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title_sort | new quinoxaline-containing peptide induces apoptosis in cancer cells by autophagy modulation |
topic | Chemistry |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5666514/ https://www.ncbi.nlm.nih.gov/pubmed/29142702 http://dx.doi.org/10.1039/c5sc00125k |
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