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Covalent Peptide LSD1 Inhibitor Specifically Recognizes Cys360 in the Enzyme-Active Region

J Med Chem . . 2023-11; 
Qinhong Luo , Yue Ma , Huiting Liang , Yuan Feng , Na Liu, Chenshan Lian , Lizhi Zhu , Yuxin Ye , Zhihong Liu , Zhanfeng Hou , Sijin Chen , Yaqi Wang , Chuan Dai , Chunli Song , Min Zhang , Zhipeng He , Yun Xing , Wanjin Zhong , Shuiming Li , Jianlong Wu , Fei Lu , Feng Yin , Zigang Li
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Lysine-specific demethylase 1 (LSD1) is a promising therapeutic target, especially in cancer treatment. Despite several LSD1 inhibitors being discovered for the cofactor pocket, none are FDA-approved. We aimed to develop stabilized peptides for irreversible LSD1 binding, focusing on unique cysteine residue Cys360 in LSD1 and SNAIL1. We created LSD1 C360-targeting peptides, like cyclic peptide S9-CMC1, using our Cysteine-Methionine cyclization strategy. S9-CMC1 effectively inhibited LSD1 at the protein level, as confirmed by MS analysis showing covalent bonding to Cys360. In cells, S9-CMC1 inhibited LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting... More