Related Experiment Video
Updated: Jun 29, 2025

11:17
Direct Measurement of KDM1A Target Engagement Using Chemoprobe-based Immunoassays
Published on: June 13, 2019
7.3K
Strategies that regulate LSD1 for novel therapeutics
Meng Li1, Mengge Dai1, Bing Cheng1
1School of Pharmaceutical Sciences & Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou University, Zhengzhou 450001, China.
Acta Pharmaceutica Sinica. B
|April 4, 2024
Summary
Lysine-specific demethylase 1 (LSD1) regulates gene transcription and is a target for diseases. This review details how proteins, post-translational modifications, and metabolites dynamically regulate LSD1 activity.
Area of Science:
- Epigenetics
- Molecular Biology
- Biochemistry
Background:
- Histone methylation is key to chromatin structure and gene transcription.
- Lysine-specific demethylase 1 (LSD1) is overexpressed in diseases and is a therapeutic target.
- LSD1 regulates gene transcription by removing methyl groups from H3K4 and H3K9.
Purpose of the Study:
- To systematically review regulatory factors of LSD1 activity.
- To explore how transcriptional corepressor complexes influence LSD1.
- To summarize the impact of post-translational modifications and metabolites on LSD1.
Main Methods:
- Literature review of studies on LSD1 regulation.
- Analysis of protein interactions within corepressor complexes.
- Examination of post-translational modifications and metabolite effects on LSD1.
Main Results:
- LSD1 activity is dynamically regulated by multiple factors beyond its demethylase function.
- Proteins forming transcriptional corepressor complexes modulate LSD1.
- Post-translational modifications and cellular metabolites also influence LSD1 expression and activity.
Conclusions:
- Understanding LSD1 regulation is crucial for developing targeted therapies.
- LSD1's complex regulatory network involves protein interactions, PTMs, and metabolites.
- Further research into these regulatory mechanisms can uncover new therapeutic strategies for LSD1-associated diseases.

