Home Journals Articles Updates About
CN
image
收藏切换
Screening novel inhibitors of squalene epoxidase and their effects on hepatocellular carcinoma
收藏切换
PDF
Liang-qi GUO1, Ya-li LIU1, Xiao TAN1, Ting ZHAI2, De-qiao SHENG1, *, Ya-yun LIU1, 2, *
Acta Pharmaceutica Sinica | 2023, 58(9) : 2707 - 2714
Less
收藏切换
Acta Pharmaceutica Sinica | 2023, 58(9): 2707-2714
Screening novel inhibitors of squalene epoxidase and their effects on hepatocellular carcinoma
Full
Liang-qi GUO1, Ya-li LIU1, Xiao TAN1, Ting ZHAI2, De-qiao SHENG1, *, Ya-yun LIU1, 2, *
Affiliations
  • 1. Hubei Key Laboratory of Tumor Microenvironment and Immunotherapy, College of Basic Medical Science, China Three Gorges University, Yichang 443002, China
  • 2. Hubei Province Key Laboratory of Biotechnology of Chinese Traditional Medicine, National & Local Joint Engineering Research Center of High Throughput Drug Screening Technology, Hubei University, Wuhan 430062, China
Published: 2023-09-12 doi: 10.16438/j.0513-4870.2023-0788
Outline
收藏切换

Squalene epoxidase (SQLE) is a potential target for the treatment of liver cancer. Bioinformatics analysis indicated that the high expression of SQLE was closely related to the clinical stage and poor prognosis of patients with liver cancer. However, the existing inhibitors against SQLE 195 tyrosine residue (Y195) cannot be used clinically due to severe side effects. In this study, 35 small-molecule compounds targeting SQLE 335 tyrosine residue (Y335) were selected by computer virtual screening. Combined with MTT assay, 3 candidate compounds (19#, 31# and 35#) with significant inhibitory effects on the proliferation of Huh7 cell line were obtained. Further studies showed that these 3 compounds could inhibit the migration of Huh7 cells, reduce the contents of total and free cholesterol, up-regulate the expression of tumor suppressor gene PTEN, and down-regulate the expression of PI3K and AKT proteins. The results showed that the novel inhibitors 19#, 31# and 35# targeting SQLE Y335 could reduce cholesterol content, inhibit the proliferation and migration of Huh7, thus playing an anti-liver cancer role.

squalene epoxidase  /  novel inhibitor  /  liver cancer  /  cholesterol  /  proliferation  /  migration
Liang-qi GUO, Ya-li LIU, Xiao TAN, Ting ZHAI, De-qiao SHENG, Ya-yun LIU. Screening novel inhibitors of squalene epoxidase and their effects on hepatocellular carcinoma[J]. Acta Pharmaceutica Sinica, 2023 , 58 (9) : 2707 -2714 . DOI: 10.16438/j.0513-4870.2023-0788
Appendix
Less
Year 2023 volume 58 Issue 9
PDF
245
109
Cite this Article
BibTeX
Article Info
doi: 10.16438/j.0513-4870.2023-0788
  • Receive Date：2023-06-26
  • Online Date：2025-11-21
  • Published：2023-09-12
Article Data
Affiliations
History
  • Received：2023-06-26
  • Revised：2023-07-27
Funding
Affiliations
    1. Hubei Key Laboratory of Tumor Microenvironment and Immunotherapy, College of Basic Medical Science, China Three Gorges University, Yichang 443002, China
    2. Hubei Province Key Laboratory of Biotechnology of Chinese Traditional Medicine, National & Local Joint Engineering Research Center of High Throughput Drug Screening Technology, Hubei University, Wuhan 430062, China
References
Share
https://castjournals.cast.org.cn/joweb/yxxb/EN/10.16438/j.0513-4870.2023-0788
Share to
QR

Scan QR to access full text

Cite this article
BibTeX
Citations
表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
关闭全屏
  • BibTeX
  • EndNote
  • RefWorks
  • TxT
Links
Articles
Latest Articles
Most Read
Collections
Updates
Events
News
Multimedia
About
About Us
Contact
No. 86 Xueyuan South Road, Haidian District, Beijing
100081
010-62199257
qkjq@cast.org.cn

Copyright © 2025 China Association for Science and Technology. All rights reserved. For all open access content, the relevant licensing terms apply.
Sponsored by the Office of the Leading Group for Cybersecurity and Informatization of CAST, and supported by Science and Technology Review Publishing House