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Pharmacological Inhibition of LSD1 for Cancer Treatment

Guan-Jun Yang1, Pui-Man Lei2, Suk-Yu Wong3

  • 1State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao 999078, China. yb67509@connect.um.edu.mo.

Molecules (Basel, Switzerland)
|December 7, 2018
PubMed

Insights

Lysine-specific demethylase 1A (LSD1) is a cancer-driving enzyme. Inhibiting LSD1 shows promise in treating various cancers by blocking tumor progression and metastasis.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Lysine-specific demethylase 1A (LSD1/KDM1A) removes methyl groups from histone proteins.
  • Aberrant LSD1 expression is linked to impaired cell differentiation and increased cancer progression.
  • LSD1 activity is associated with poor prognosis in multiple cancer types.

Purpose of the Study:

  • To review the structural characteristics of LSD1.
  • To elucidate the role of LSD1 in carcinogenesis.
  • To compare screening methods for LSD1 inhibitors and classify existing inhibitors.

Main Methods:

  • Literature review of structural biology, cancer research, and drug discovery studies.
  • Analysis of published data on LSD1 function and inhibition.
  • Comparative assessment of LSD1 inhibitor screening assays.

Main Results:

  • LSD1's structural features facilitate its enzymatic activity.
  • LSD1 inhibition effectively reduces tumor progression in preclinical models.
  • Various classes of LSD1 inhibitors have been developed.

Conclusions:

  • LSD1 is a validated drug target for cancer therapy.
  • Targeting LSD1 offers a promising strategy for treating solid tumors and leukemia.
  • Further research into LSD1 inhibitors could lead to novel cancer treatments.
Keywords:
LSD1acute myeloid leukemiabreast cancercancer therapydemethylasehistoneprostate cancer

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