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New dimension in therapeutic targeting of BCL-2 family proteins
Proteins of the BCL-2 family control the mitochondrial pathway of apoptosis. Targeting these proteins proves to be an attractive strategy for anticancer therapy. The biological context is based on the fact that BH3-only members of the family are specific antagonists of prosurvival members. This prom...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Impact Journals LLC
2015
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4536985/ https://www.ncbi.nlm.nih.gov/pubmed/25970783 |
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author | Besbes, Samaher Mirshahi, Massoud Pocard, Marc Billard, Christian |
author_facet | Besbes, Samaher Mirshahi, Massoud Pocard, Marc Billard, Christian |
author_sort | Besbes, Samaher |
collection | PubMed |
description | Proteins of the BCL-2 family control the mitochondrial pathway of apoptosis. Targeting these proteins proves to be an attractive strategy for anticancer therapy. The biological context is based on the fact that BH3-only members of the family are specific antagonists of prosurvival members. This prompted the identification of “BH3 mimetic” compounds. These small peptides or organic molecules indeed mimic the BH3 domain of BH3-only proteins: by selectively binding and antagonizing prosurvival proteins, they can induce apoptosis in malignant cells. Some small-molecule inhibitors of prosurvival proteins have already entered clinical trials in cancer patients and two of them have shown significant therapeutic effects. The latest developments in the field of targeting BCL-2 family proteins highlight several new antagonists of prosurvival proteins as well as direct activators of proapoptotic proteins. These compounds open up novel prospects for the development of BH3 mimetic anticancer drugs. |
format | Online Article Text |
id | pubmed-4536985 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2015 |
publisher | Impact Journals LLC |
record_format | MEDLINE/PubMed |
spelling | pubmed-45369852015-08-26 New dimension in therapeutic targeting of BCL-2 family proteins Besbes, Samaher Mirshahi, Massoud Pocard, Marc Billard, Christian Oncotarget Review Proteins of the BCL-2 family control the mitochondrial pathway of apoptosis. Targeting these proteins proves to be an attractive strategy for anticancer therapy. The biological context is based on the fact that BH3-only members of the family are specific antagonists of prosurvival members. This prompted the identification of “BH3 mimetic” compounds. These small peptides or organic molecules indeed mimic the BH3 domain of BH3-only proteins: by selectively binding and antagonizing prosurvival proteins, they can induce apoptosis in malignant cells. Some small-molecule inhibitors of prosurvival proteins have already entered clinical trials in cancer patients and two of them have shown significant therapeutic effects. The latest developments in the field of targeting BCL-2 family proteins highlight several new antagonists of prosurvival proteins as well as direct activators of proapoptotic proteins. These compounds open up novel prospects for the development of BH3 mimetic anticancer drugs. Impact Journals LLC 2015-04-19 /pmc/articles/PMC4536985/ /pubmed/25970783 Text en Copyright: © 2015 Besbes et al. http://creativecommons.org/licenses/by/2.5/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. |
spellingShingle | Review Besbes, Samaher Mirshahi, Massoud Pocard, Marc Billard, Christian New dimension in therapeutic targeting of BCL-2 family proteins |
title | New dimension in therapeutic targeting of BCL-2 family proteins |
title_full | New dimension in therapeutic targeting of BCL-2 family proteins |
title_fullStr | New dimension in therapeutic targeting of BCL-2 family proteins |
title_full_unstemmed | New dimension in therapeutic targeting of BCL-2 family proteins |
title_short | New dimension in therapeutic targeting of BCL-2 family proteins |
title_sort | new dimension in therapeutic targeting of bcl-2 family proteins |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4536985/ https://www.ncbi.nlm.nih.gov/pubmed/25970783 |
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