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Raloxifene, identified as a novel LSD1 inhibitor, suppresses the migration of renal cell carcinoma
Yuan Ma1, Yan Zheng2, Yanli Ji3
1Institute of Clinical Medicine, Urodynamic Center and Department of Urology, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China.
Abstract:
Aim: As an important epigenetic modulator, histone lysine-specific demethylase 1 (LSD1) has been proved to be associated with the progression of renal cell carcinoma (RCC). Discovering novel LSD1 inhibitors offers therapeutic potential for RCC treatment. Methods & Results: We identified raloxifene as a novel LSD1 inhibitor (IC50 = 2.08 μM) through small compound library screening. Molecular docking indicated raloxifene might bind LSD1 in the flavin adenine dinucleotide (FAD) binding cavity in a reversible manner. Cell viability and migration assays showed raloxifene could suppress the proliferation and migration of RCC cells bearing overexpressed LSD1. Conclusion: Our findings indicated that LSD1 might be a promising therapeutic target for RCC and that raloxifene could serve as a lead compound for further anti-RCC metastasis drug discovery.
Insights
Raloxifene inhibits histone lysine-specific demethylase 1 (LSD1), a key factor in renal cell carcinoma (RCC) progression. This compound suppressed RCC cell proliferation and migration, offering potential for new anti-cancer therapies.
Area of Science:
- Epigenetics
- Oncology
- Pharmacology
Background:
- Histone lysine-specific demethylase 1 (LSD1) is an epigenetic modulator implicated in renal cell carcinoma (RCC) progression.
- Targeting LSD1 presents a therapeutic strategy for RCC treatment.
Purpose of the Study:
- To identify novel inhibitors of LSD1.
- To evaluate the potential of identified inhibitors as anti-RCC agents.
Main Methods:
- Screening of a small compound library to identify LSD1 inhibitors.
- Molecular docking to predict binding interactions.
- Cell viability and migration assays in RCC cell lines.
Main Results:
- Raloxifene identified as a novel LSD1 inhibitor with an IC50 of 2.08 μM.
- Molecular docking suggests reversible binding of raloxifene to the LSD1 flavin adenine dinucleotide (FAD) binding cavity.
- Raloxifene demonstrated suppression of proliferation and migration in RCC cells with overexpressed LSD1.
Conclusions:
- LSD1 is a promising therapeutic target for renal cell carcinoma.
- Raloxifene serves as a potential lead compound for developing novel anti-RCC metastasis drugs.
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