Details

Autor(en) / Beteiligte

• Zhang, Yawen
• Wang, Mengmeng
• Meng, Fanyi
• Yang, Man
• Chen, Yinshuang
• Guo, Xuqin
• Wang, Weiwei
• Zhu, Yifan
• Guo, Yundi
• Feng, Chunlai
• Tian, Shen
• Zhang, Hongjian
• Li, Huanqiu
• Sun, Jing
• Wang, Weipeng

Titel

A novel SRSF3 inhibitor, SFI003, exerts anticancer activity against colorectal cancer by modulating the SRSF3/DHCR24/ROS axis

Ist Teil von

• Cell death discovery, 2022-05, Vol.8 (1), p.238-238, Article 238

Ort / Verlag

London: Nature Publishing Group UK

Erscheinungsjahr

2022

Quelle

EZB-FREE-00999 freely available EZB journals

Beschreibungen/Notizen

• As the modulation of serine/arginine-rich splicing factor 3 (SRSF3) may be therapeutically beneficial to colorectal cancer (CRC) treatment, the identification of novel SRSF3 inhibitors is highly anticipated. However, pharmaceutical agents targeting SRSF3 have not yet been discovered. Here, we propose a functional SRSF3 inhibitor for CRC therapy and elucidate its antitumor mechanisms. We found high expression of SRSF3 in 70.6% CRC tissues. Silencing SRSF3 markedly inhibits the proliferation and migration of CRC cells through suppression of its target gene 24-dehydrocholesterol reductase (DHCR24). This is evidenced by the links between SRSF3 and DHCR24 in CRC tissues. The novel SRSF3 inhibitor SFI003 exhibits potent antitumor efficacy in vitro and in vivo, which drives apoptosis of CRC cells via the SRSF3/DHCR24/reactive oxygen species (ROS) axis. Moreover, SFI003 is druggable with suitable pharmacokinetic properties, bioavailability, and tumor distribution. Thus, SRSF3 is a novel potential therapeutic target for CRC. Its inhibitor SFI003 may be developed as an anticancer therapeutic.