Advances on clinical research of histone demethylase LSD1 inhibitors
10.16438/j.0513-4870.2022-0688
- VernacularTitle:组蛋白去甲基化酶LSD1抑制剂临床研究进展
- Author:
Yu-ting SHI
;
Xin-yu YANG
;
Bin YU
;
Yi-hui SONG
- Publication Type:Research Article
- Keywords:
epigenetics;
histone demethylase;
lysine-specific demethylase 1 inhibitor;
clinical trial;
rug discovery
- From:
Acta Pharmaceutica Sinica
2022;57(10):2949-2959
- CountryChina
- Language:Chinese
-
Abstract:
Lysine-specific demethylase 1 (LSD1) plays vital roles in cell stemness, differentiation, cell motility, metabolic control and epithelial-mesenchymal transition, which is closely associated with tumorigenesis processes including cell proliferation, invasive, metastasis and poor prognosis. Besides, LSD1 also contributes to the occurrence of other diseases such as neurodegenerative diseases and viral infections. Since 2013, the irreversible inhibitors including tranylcypromine, ORY-1001, ORY-2001, GSK-2879552, IMG-7289, INCB059872, TAK-418, LH-1802 and reversible inhibitors including CC-90011 and SP-2577 have been approved for clinical assessment. This review comprehensively summarizes the clinical research of LSD1 drug candidates and briefly discusses the prospects, opportunities and challenges of LSD1-targeted drug discovery, aiming to provide a landscape for the related drug development.
