Natural products as LSD1 inhibitors for cancer therapy

Acta Pharmaceutica Sinica B

卷:11

Zhiqiang Yu¹  Bin Yu²  Chao Yang³  Yuan Fang⁴  Xiaochuan Li⁵  Guochao Liao⁶  Qingchun Mu⁶ 

[1] Application, Zhejiang Ocean University, Zhoushan 316022, China;

[2] Corresponding authors. Tel./fax: [phone].;

[3] Institute of Innovation &

[4] Joint Laboratory for Translational Cancer Research of Chinese Medicine of the Ministry of Education of the People's Republic of China, International Institute for Translational Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou 510006, China;

[5] School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China;

[6] The People's Hospital of Gaozhou, Gaozhou 525200, China;

关键词: Epigenetic regulation;    Histone demethylase;    Natural products;    LSD1 inhibitors;    Drug discovery;    Cancer therapy;   

DOI  :  

来源: DOAJ

【 摘 要 】

Natural products generally fall into the biologically relevant chemical space and always possess novel biological activities, thus making them a rich source of lead compounds for new drug discovery. With the recent technological advances, natural product-based drug discovery is now reaching a new era. Natural products have also shown promise in epigenetic drug discovery, some of them have advanced into clinical trials or are presently being used in clinic. The histone lysine specific demethylase 1 (LSD1), an important class of histone demethylases, has fundamental roles in the development of various pathological conditions. Targeting LSD1 has been recognized as a promising therapeutic option for cancer treatment. Notably, some natural products with different chemotypes including protoberberine alkaloids, flavones, polyphenols, and cyclic peptides have shown effectiveness against LSD1. These natural products provide novel scaffolds for developing new LSD1 inhibitors. In this review, we mainly discuss the identification of natural LSD1 inhibitors, analysis of the co-crystal structures of LSD1/natural product complex, antitumor activity and their modes of action. We also briefly discuss the challenges faced in this field. We believe this review will provide a landscape of natural LSD1 inhibitors.

【 授权许可】

Unknown