Next Article in Journal
Intracellular Accumulation of Linezolid and Florfenicol in OptrA-Producing Enterococcus faecalis and Staphylococcus aureus
Previous Article in Journal
Adverse Drug Reaction Predictions Using Stacking Deep Heterogeneous Information Network Embedding Approach
Previous Article in Special Issue
Cloning, Characterization and Anion Inhibition Studies of a β-Carbonic Anhydrase from the Pathogenic Protozoan Entamoeba histolytica
Article Menu

Export Article

Open AccessReview
Molecules 2018, 23(12), 3194;

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
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]   |  


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

Graphical abstract

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).

Share & Cite This Article

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.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top