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Pharmacological Inhibition of LSD1 for Cancer Treatment
Lysine-specific demethylase 1A (LSD1, also named KDM1A) is a demethylase that can remove methyl groups from histones H3K4me1/2 and H3K9me1/2. It is aberrantly expressed in many cancers, where it impedes differentiation and contributes to cancer cell proliferation, cell metastasis and invasiveness, a...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6320820/ https://www.ncbi.nlm.nih.gov/pubmed/30518104 http://dx.doi.org/10.3390/molecules23123194 |
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author | Yang, Guan-Jun Lei, Pui-Man Wong, Suk-Yu Ma, Dik-Lung Leung, Chung-Hang |
author_facet | Yang, Guan-Jun Lei, Pui-Man Wong, Suk-Yu Ma, Dik-Lung Leung, Chung-Hang |
author_sort | Yang, Guan-Jun |
collection | PubMed |
description | Lysine-specific demethylase 1A (LSD1, also named KDM1A) is a demethylase that can remove methyl groups from histones H3K4me1/2 and H3K9me1/2. It is aberrantly expressed in many cancers, where it impedes differentiation and contributes to cancer cell proliferation, cell metastasis and invasiveness, and is associated with inferior prognosis. Pharmacological inhibition of LSD1 has been reported to significantly attenuate tumor progression in vitro and in vivo in a range of solid tumors and acute myeloid leukemia. This review will present the structural aspects of LSD1, its role in carcinogenesis, a comparison of currently available approaches for screening LSD1 inhibitors, a classification of LSD1 inhibitors, and its potential as a drug target in cancer therapy. |
format | Online Article Text |
id | pubmed-6320820 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-63208202019-01-14 Pharmacological Inhibition of LSD1 for Cancer Treatment Yang, Guan-Jun Lei, Pui-Man Wong, Suk-Yu Ma, Dik-Lung Leung, Chung-Hang Molecules Review Lysine-specific demethylase 1A (LSD1, also named KDM1A) is a demethylase that can remove methyl groups from histones H3K4me1/2 and H3K9me1/2. It is aberrantly expressed in many cancers, where it impedes differentiation and contributes to cancer cell proliferation, cell metastasis and invasiveness, and is associated with inferior prognosis. Pharmacological inhibition of LSD1 has been reported to significantly attenuate tumor progression in vitro and in vivo in a range of solid tumors and acute myeloid leukemia. This review will present the structural aspects of LSD1, its role in carcinogenesis, a comparison of currently available approaches for screening LSD1 inhibitors, a classification of LSD1 inhibitors, and its potential as a drug target in cancer therapy. MDPI 2018-12-04 /pmc/articles/PMC6320820/ /pubmed/30518104 http://dx.doi.org/10.3390/molecules23123194 Text en © 2018 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Yang, Guan-Jun Lei, Pui-Man Wong, Suk-Yu Ma, Dik-Lung Leung, Chung-Hang Pharmacological Inhibition of LSD1 for Cancer Treatment |
title | Pharmacological Inhibition of LSD1 for Cancer Treatment |
title_full | Pharmacological Inhibition of LSD1 for Cancer Treatment |
title_fullStr | Pharmacological Inhibition of LSD1 for Cancer Treatment |
title_full_unstemmed | Pharmacological Inhibition of LSD1 for Cancer Treatment |
title_short | Pharmacological Inhibition of LSD1 for Cancer Treatment |
title_sort | pharmacological inhibition of lsd1 for cancer treatment |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6320820/ https://www.ncbi.nlm.nih.gov/pubmed/30518104 http://dx.doi.org/10.3390/molecules23123194 |
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