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A comprehensive comparative study on LSD1 in different cancers and tumor specific LSD1 inhibitors
被引:18
|作者:
Dong, Jianshu
[1
,2
,3
,5
]
Pervaiz, Waqar
[1
,2
,3
,5
]
Tayyab, Bilal
[1
,2
,3
,5
]
Li, Die
[1
,2
,3
,5
]
Kang, Lei
[1
,2
,3
,5
]
Zhang, Huimin
[1
,2
,3
,4
,5
]
Gong, Huimin
[1
,2
,3
,5
]
Ma, Xinli
[6
]
Li, Jian
[6
]
Agboyibor, Clement
[3
,4
,5
]
Bi, Yuefeng
[1
,2
,3
,4
,5
,7
]
Liu, Hongmin
[3
,5
,7
]
机构:
[1] Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Peoples R China
[2] Zhengzhou Univ, Key Lab Adv Drug Preparat Technol, Minist Educ, Zhengzhou 450001, Peoples R China
[3] Zhengzhou Univ, Key Lab Henan Prov Drug Qual Control & Evaluat, Zhengzhou 450001, Peoples R China
[4] Zhengzhou Univ, Collaborat Innovat Ctr New Drug Res & Safety Evalu, Zhengzhou 450001, Peoples R China
[5] Zhengzhou Univ, Inst Drug Discovery & Dev, Zhengzhou 450001, Peoples R China
[6] China US Henan Hormel Canc Inst, 127,Dongming Rd,Jinshui Dist, Zhengzhou 450008, Henan, Peoples R China
[7] Zhengzhou Univ, Sch Pharmaceut Sci, 100 Kexue Dadao,Gaoxin Dist, Zhengzhou 450001, Peoples R China
基金:
中国国家自然科学基金;
关键词:
LSD1;
Epigenetics;
Cancer;
Leukemia;
Histonedemethylase;
EMT;
EPITHELIAL-MESENCHYMAL TRANSITION;
DEMETHYLASE;
LSD1;
HISTONE DEMETHYLASE;
BIOLOGICAL-ACTIVITY;
GENE-EXPRESSION;
CYCLOPROPYLAMINE DERIVATIVES;
CELL-PROLIFERATION;
STRUCTURAL BASIS;
PHASE-I;
TRANYLCYPROMINE;
D O I:
10.1016/j.ejmech.2022.114564
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
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.
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页数:17
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