Annual review of LSD1/KDM1A inhibitors in 2020

Eur J Med Chem. 2021 Mar 15:214:113254. doi: 10.1016/j.ejmech.2021.113254.

Dong-Jun Fu ¹, Jun Li ², Bin Yu ³

Affiliations

1 Modern Research Center for Traditional Chinese Medicine, School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 100029, China.
2 Modern Research Center for Traditional Chinese Medicine, School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 100029, China. Electronic address: drlj666@163.com.
3 School of Pharmaceutical Sciences & Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou University, Zhengzhou, 450001, China. Electronic address: zzuyubin@hotmail.com.

PMID: 33581557 DOI: 10.1016/j.ejmech.2021.113254

Abstract

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.

Keywords

Cancer therapy; Histone demethylase; LSD1 inhibitor.

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