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Review

A Comprehensive Review of Lysine-Specific Demethylase 1 and its Roles in Cancer

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Pages 1123-1142 | Received 05 Feb 2017, Accepted 15 Jun 2017, Published online: 12 Jul 2017
 

Abstract

Histone methylation plays a key role in the regulation of chromatin structure, and its dynamics regulates important cellular processes. The investigation of the role of alterations in histone methylation in cancer has led to the identification of histone methyltransferases and demethylases as promising novel targets for therapy. Lysine-specific demethylase 1(LSD1, also known as KDM1A) is the first discovered histone lysine demethylase, with the ability to demethylase H3K4me1/2 and H3K9me1/2 at target loci in a context-dependent manner. LSD1 regulates the balance between self-renewal and differentiation of stem cells, and is highly expressed in various cancers, playing an important role in differentiation and self-renewal of tumor cells. In this review, we summarize recent studies about the LSD1, its role in normal and tumor cells, and the potential use of small molecule LSD1 inhibitors in therapy.

Financial & competing interests disclosure

Work in S Minucci’s lab was supported by EC (4D Cell Fate), AIRC (IG13) and CNR (Epigen Flagship Project). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.

Additional information

Funding

Work in S Minucci’s lab was supported by EC (4D Cell Fate), AIRC (IG13) and CNR (Epigen Flagship Project). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed. No writing assistance was utilized in the production of this manuscript.

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