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Molecules 2018, 23(12), 3194; https://doi.org/10.3390/molecules23123194

Pharmacological Inhibition of LSD1 for Cancer Treatment

1
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao 999078, China
2
Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong 999077, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Tiziano Tuccinardi
Received: 15 November 2018 / Revised: 30 November 2018 / Accepted: 30 November 2018 / Published: 4 December 2018
(This article belongs to the Special Issue Trends in the Development of Enzyme Inhibitors)
Full-Text   |   PDF [2676 KB, uploaded 4 December 2018]   |  

Abstract

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. View Full-Text
Keywords: LSD1; demethylase; histone; breast cancer; prostate cancer; acute myeloid leukemia; cancer therapy LSD1; demethylase; histone; breast cancer; prostate cancer; acute myeloid leukemia; cancer therapy
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Yang, G.-J.; Lei, P.-M.; Wong, S.-Y.; Ma, D.-L.; Leung, C.-H. Pharmacological Inhibition of LSD1 for Cancer Treatment. Molecules 2018, 23, 3194.

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