2. Academic Validation
  3. A comprehensive review of lysine-specific demethylase 1 and its roles in cancer

A comprehensive review of lysine-specific demethylase 1 and its roles in cancer

  • Epigenomics. 2017 Aug;9(8):1123-1142. doi: 10.2217/epi-2017-0022.
Amir Hosseini 1,  Saverio Minucci 1 2
Affiliations

Affiliations

  • 1 Department of Experimental Oncology, European Institute of Oncology, Milan, Italy.
  • 2 Department of Biosciences, University of Milan, Milan, Italy.
PMID: 28699367 DOI: 10.2217/epi-2017-0022
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.

Keywords

GSK2879552; KDM1A; LSD1; MC2580; NCD38; OG86; ORY-1001; SP2509; cancer; epigenetic therapy; histone demethylases.

Figures