HDAC Inhibitors for the Therapy of Triple Negative Breast Cancer

Triple negative breast cancer (TNBC) is an urgent as well as huge medical challenge, which is associated with poor prognosis and responsiveness to chemotherapies. Since epigenetic changes are highly implicated in TNBC tumorigenesis and development, inhibitors of histone deacetylases (HDACIs) could r...

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Autores principales: Maccallini, Cristina, Ammazzalorso, Alessandra, De Filippis, Barbara, Fantacuzzi, Marialuigia, Giampietro, Letizia, Amoroso, Rosa
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Review
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9230362/
https://www.ncbi.nlm.nih.gov/pubmed/35745586
http://dx.doi.org/10.3390/ph15060667
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author Maccallini, Cristina
Ammazzalorso, Alessandra
De Filippis, Barbara
Fantacuzzi, Marialuigia
Giampietro, Letizia
Amoroso, Rosa
author_facet Maccallini, Cristina
Ammazzalorso, Alessandra
De Filippis, Barbara
Fantacuzzi, Marialuigia
Giampietro, Letizia
Amoroso, Rosa
author_sort Maccallini, Cristina
collection PubMed
description Triple negative breast cancer (TNBC) is an urgent as well as huge medical challenge, which is associated with poor prognosis and responsiveness to chemotherapies. Since epigenetic changes are highly implicated in TNBC tumorigenesis and development, inhibitors of histone deacetylases (HDACIs) could represent a promising therapeutic strategy. Although clinical trials involving single HDACIs showed disappointing results against TNBC, recent studies emphasize the high potential impact of HDACIs in controlling TNBC. In addition, encouraging results stem from new compounds designed to obtain isoform selectivity and/or polypharmacological HDAC approach. The present review provides a discussion of the HDACIs pharmacophoric models and of the structural modifications, leading to compounds with a potent activity against TNBC progression.
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spelling pubmed-92303622022-06-25 HDAC Inhibitors for the Therapy of Triple Negative Breast Cancer Maccallini, Cristina Ammazzalorso, Alessandra De Filippis, Barbara Fantacuzzi, Marialuigia Giampietro, Letizia Amoroso, Rosa Pharmaceuticals (Basel) Review Triple negative breast cancer (TNBC) is an urgent as well as huge medical challenge, which is associated with poor prognosis and responsiveness to chemotherapies. Since epigenetic changes are highly implicated in TNBC tumorigenesis and development, inhibitors of histone deacetylases (HDACIs) could represent a promising therapeutic strategy. Although clinical trials involving single HDACIs showed disappointing results against TNBC, recent studies emphasize the high potential impact of HDACIs in controlling TNBC. In addition, encouraging results stem from new compounds designed to obtain isoform selectivity and/or polypharmacological HDAC approach. The present review provides a discussion of the HDACIs pharmacophoric models and of the structural modifications, leading to compounds with a potent activity against TNBC progression. MDPI 2022-05-26 /pmc/articles/PMC9230362/ /pubmed/35745586 http://dx.doi.org/10.3390/ph15060667 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Maccallini, Cristina
Ammazzalorso, Alessandra
De Filippis, Barbara
Fantacuzzi, Marialuigia
Giampietro, Letizia
Amoroso, Rosa
HDAC Inhibitors for the Therapy of Triple Negative Breast Cancer
title HDAC Inhibitors for the Therapy of Triple Negative Breast Cancer
title_full HDAC Inhibitors for the Therapy of Triple Negative Breast Cancer
title_fullStr HDAC Inhibitors for the Therapy of Triple Negative Breast Cancer
title_full_unstemmed HDAC Inhibitors for the Therapy of Triple Negative Breast Cancer
title_short HDAC Inhibitors for the Therapy of Triple Negative Breast Cancer
title_sort hdac inhibitors for the therapy of triple negative breast cancer
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9230362/
https://www.ncbi.nlm.nih.gov/pubmed/35745586
http://dx.doi.org/10.3390/ph15060667
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