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Updated: Jul 9, 2025

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Published on: May 16, 2021
LSD1 in drug discovery: From biological function to clinical application
Hui-Min Liu1, Ying Zhou1, He-Xiang Chen1
1State Key Laboratory of Esophageal Cancer Prevention & Treatment, Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education of China, Key Laboratory of Henan Province for Drug Quality and Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan, China.
Lysine-specific demethylase 1 (LSD1) regulates gene transcription and is upregulated in cancers. Inhibitors targeting LSD1 are in clinical trials, offering potential therapeutic strategies.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Lysine-specific demethylase 1 (LSD1) is an FAD-dependent enzyme that demethylates histone and nonhistone substrates.
- LSD1 regulates gene transcription by erasing H3K4 methylation, impacting cellular functions.
- Upregulation of LSD1 is implicated in the progression of various cancers.
Conclusions:
- LSD1 is a promising therapeutic target in oncology.
- Targeting LSD1 offers a potential strategy for cancer treatment.
- Further research into LSD1 inhibitors could benefit cancer therapy.
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