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G9a: An Emerging Epigenetic Target for Melanoma Therapy
Epigenetic regulation is a crucial component of DNA maintenance and cellular identity. As our understanding of the vast array of proteins that contribute to chromatin accessibility has advanced, the role of epigenetic remodelers in disease has become more apparent. G9a is a histone methyltransferase...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8536146/ https://www.ncbi.nlm.nih.gov/pubmed/34691767 http://dx.doi.org/10.3390/epigenomes5040023 |
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author | Flesher, Jessica L. Fisher, David E. |
author_facet | Flesher, Jessica L. Fisher, David E. |
author_sort | Flesher, Jessica L. |
collection | PubMed |
description | Epigenetic regulation is a crucial component of DNA maintenance and cellular identity. As our understanding of the vast array of proteins that contribute to chromatin accessibility has advanced, the role of epigenetic remodelers in disease has become more apparent. G9a is a histone methyltransferase that contributes to immune cell differentiation and function, neuronal development, and has been implicated in diseases, including cancer. In melanoma, recurrent mutations and amplifications of G9a have led to its identification as a therapeutic target. The pathways that are regulated by G9a provide an insight into relevant biomarkers for patient stratification. Future work is aided by the breadth of literature on G9a function during normal differentiation and development, along with similarities to EZH2, another histone methyltransferase that forms a synthetic lethal relationship with members of the SWI/SNF complex in certain cancers. Here, we review the literature on G9a, its role in melanoma, and lessons from EZH2 inhibitor studies. |
format | Online Article Text |
id | pubmed-8536146 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-85361462021-12-01 G9a: An Emerging Epigenetic Target for Melanoma Therapy Flesher, Jessica L. Fisher, David E. Epigenomes Review Epigenetic regulation is a crucial component of DNA maintenance and cellular identity. As our understanding of the vast array of proteins that contribute to chromatin accessibility has advanced, the role of epigenetic remodelers in disease has become more apparent. G9a is a histone methyltransferase that contributes to immune cell differentiation and function, neuronal development, and has been implicated in diseases, including cancer. In melanoma, recurrent mutations and amplifications of G9a have led to its identification as a therapeutic target. The pathways that are regulated by G9a provide an insight into relevant biomarkers for patient stratification. Future work is aided by the breadth of literature on G9a function during normal differentiation and development, along with similarities to EZH2, another histone methyltransferase that forms a synthetic lethal relationship with members of the SWI/SNF complex in certain cancers. Here, we review the literature on G9a, its role in melanoma, and lessons from EZH2 inhibitor studies. MDPI 2021-10-12 /pmc/articles/PMC8536146/ /pubmed/34691767 http://dx.doi.org/10.3390/epigenomes5040023 Text en © 2021 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 Flesher, Jessica L. Fisher, David E. G9a: An Emerging Epigenetic Target for Melanoma Therapy |
title | G9a: An Emerging Epigenetic Target for Melanoma Therapy |
title_full | G9a: An Emerging Epigenetic Target for Melanoma Therapy |
title_fullStr | G9a: An Emerging Epigenetic Target for Melanoma Therapy |
title_full_unstemmed | G9a: An Emerging Epigenetic Target for Melanoma Therapy |
title_short | G9a: An Emerging Epigenetic Target for Melanoma Therapy |
title_sort | g9a: an emerging epigenetic target for melanoma therapy |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8536146/ https://www.ncbi.nlm.nih.gov/pubmed/34691767 http://dx.doi.org/10.3390/epigenomes5040023 |
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