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A comprehensive comparative study on LSD1 in different cancers and tumor specific LSD1 inhibitors.

Authors :
Dong, Jianshu
Pervaiz, Waqar
Tayyab, Bilal
Li, Dié
Kang, Lei
Zhang, Huimin
Gong, Huimin
Ma, Xinli
Li, Jian
Agboyibor, Clement
Bi, Yuefeng
Liu, Hongmin
Source :
European Journal of Medicinal Chemistry. Oct2022, Vol. 240, pN.PAG-N.PAG. 1p.
Publication Year :
2022

Abstract

LSD1 was significantly over-expressed in several cancer types, and its aberrant overexpression was revealed to play a crucial role in the initiation and progression of cancer. Several LSD1 inhibitors that were discovered and developed so far were found to be effective in attenuating tumor growth in both in vivo and in vitro studies. However, the major challenge associated with the development of cancer therapies is personalized treatment. Therefore, it is essential to look in detail at how LSD1 plays its part in carcinogenesis and whether there are any different expression levels of LSD1 in different tumors. Here in this review, fresh insight into a list of function correlated LSD1 binding proteins are provided, and we tried to figure out the role of LSD1 in different cancer types, including hematological malignancies and solid tumors. A critical description of mutation preference for LSD1 in different tumors was also discussed. Recent research findings clearly showed that the abrogation of LSD1 demethylase activity via LSD1 inhibitors markedly reduced the growth of cancer cells. But there are still many ambiguities regarding the role of LSD1 in different cancers. Therefore, targeting LSD1 for treating different cancers is still reductionist, and many challenges need to be met to improve the therapeutic outcomes of LSD1 inhibitors. [Display omitted] • LSD1 overexpression is linked with the invasion and migration of cancer cells. • LSD1's critical role in regulating EMT is one of the primary causes of cancer. • Mutations in LSD1 or its effector molecules can cause variety of cancers in humans. • Diverse binding interactions of LSD1 control the fate of target genes in cancer cells. • LSD1 and its partners can serve as potential targets for precision cancer therapy. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
02235234
Volume :
240
Database :
Academic Search Index
Journal :
European Journal of Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
158424154
Full Text :
https://doi.org/10.1016/j.ejmech.2022.114564