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2020 ; 11
(3
): 621-31
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Natural products as LSD1 inhibitors for cancer therapy
#MMPMID32837872
Fang Y
; Yang C
; Yu Z
; Li X
; Mu Q
; Liao G
; Yu B
Acta Pharm Sin B
2020[Jun]; 11
(3
): 621-31
PMID32837872
show ga
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.
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