Annual review of LSD1/KDM1A inhibitors in 2020.

Dong-Jun Fu, Jun Li, Bin Yu

European journal of medicinal chemistry 2021 Mar 15

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Lysine-specific demethylase 1 (LSD1/KDM1A) has emerged as a promising target for the discovery of specific inhibitors as antitumor drugs. Based on the source of compounds, all LSD1 inhibitors in this review are divided into two categories: natural LSD1 inhibitors and synthetic LSD1 inhibitors. This review highlights the research progress of LSD1 inhibitors with the potential to treat cancer covering articles published in 2020. Design strategies, structure-activity relationships, co-crystal structure analysis and action mechanisms are also highlighted. Copyright © 2021 Elsevier Masson SAS. All rights reserved.