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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...

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Autores principales: Yang, Guan-Jun, Lei, Pui-Man, Wong, Suk-Yu, Ma, Dik-Lung, Leung, Chung-Hang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
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.
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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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