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=2.08μM) throughsmall compound library screening. Molecular docking indicated raloxifene might bind LSD1 in the flavin adenine dinucleotide (FAD) bindingcavity ina reversible manner. Cell viability and migration assays showed raloxifene could suppress the proliferation and migration of RCC cellsbearing overexpressed LSD1. Conclusion: Our findings indicated thatLSD1 might be a promising therapeutic target for RCCand thatraloxifene could serve as a lead compound for further anti-RCC metastasis drug discovery.
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