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Updated: Oct 15, 2025

Direct Measurement of KDM1A Target Engagement Using Chemoprobe-based Immunoassays
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Direct Measurement of KDM1A Target Engagement Using Chemoprobe-based Immunoassays

Published on: June 13, 2019

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Therapeutic potential of targeting LSD1/ KDM1A in cancers

Xiangyu Zhang1, Xinran Wang2, Tianxiao Wu1

  • 1Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, Liaoning, China.

Pharmacological Research
|October 31, 2021
PubMed

Insights

Lysine-specific demethylase 1 (LSD1) is a key driver in various cancers. Inhibiting LSD1 shows promise for effective cancer therapy, with numerous inhibitors in development.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Lysine-specific demethylase 1 (LSD1), identified in 2004, is a crucial enzyme utilizing FAD as a cofactor.
  • LSD1 catalyzes the demethylation of H3K4 and H3K9, epigenetic modifications linked to cancer progression.
  • Aberrant LSD1 overexpression correlates with enhanced tumor growth, invasion, and metastasis in various cancers.

Purpose of the Study:

  • To provide a comprehensive review of recent advancements in LSD1 inhibitors for cancer therapy.
  • To summarize the role of LSD1 in tumor cells and its structural characteristics.
  • To compare inhibitor screening methods and propose future research directions.

Main Methods:

  • Extensive literature review from electronic databases (PubMed, Web of Science, PDB, ClinicalTrials.gov).
  • Focus on research published between January 2015 and June 2021.
  • Analysis of Homo sapiens LSD1 crystal structures and inhibitor characteristics.

Main Results:

  • LSD1 inhibition effectively suppresses tumor development, making it a significant therapeutic target.
  • Numerous LSD1 inhibitors are undergoing preclinical and clinical trials for solid tumors and hematological malignancies.
  • Detailed review of LSD1 inhibitor structures and screening methodologies.

Conclusions:

  • LSD1 inhibitors represent a promising therapeutic strategy for various cancers.
  • Understanding LSD1 structure and inhibitor characteristics is vital for drug development.
  • Further research is needed to optimize LSD1 inhibitor efficacy and clinical application.
Keywords:
CancerDemethylationInhibitorLSD1Therapeutic target

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