Pharmacological inhibition of LSD1 for cancer treatment

Guan Jun Yang, Pui Man Lei, Suk Yu Wong, Edmond Dik Lung MA*, Chung Hang Leung

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

96 Citations (Scopus)


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.

Original languageEnglish
Article number3194
Issue number12
Publication statusPublished - 4 Dec 2018

Scopus Subject Areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

User-Defined Keywords

  • Acute myeloid leukemia
  • Breast cancer
  • Cancer therapy
  • Demethylase
  • Histone
  • LSD1
  • Prostate cancer


Dive into the research topics of 'Pharmacological inhibition of LSD1 for cancer treatment'. Together they form a unique fingerprint.

Cite this