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Open AccessReview

Pharmacological Inhibition of LSD1 for Cancer Treatment

State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao 999078, China
Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong 999077, China
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Tiziano Tuccinardi
Molecules 2018, 23(12), 3194;
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)
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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MDPI and ACS Style

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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