Small molecule targeting FOXM1 DNA binding domain exhibits anti-tumor activity in ovarian cancer.
Small molecule targeting FOXM1 DNA binding domain exhibits anti-tumor activity in ovarian cancer.
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DOI：
10.1038/s41420-022-01070-w
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发表时间：
2022-06-09
影响因子：
7
通讯作者：
Liu, Zhaojian
中科院分区：
文献类型：
--
作者：
Zhang, Zaixin;Xue, Si-Tu;Gao, Yan;Li, Yingwei;Zhou, Ziying;Wang, Jing;Li, Zhuorong;Liu, Zhaojian
FOXM1 is a potent oncogenic transcription factor essential for cancer initiation, progression, and drug resistance. FOXM1 regulatory network is a major predictor of adverse outcomes in various human cancers. Inhibition of FOXM1 transcription factor function is a potential strategy in cancer treatment. In this study, we performed structure-based in silico screening to discover small molecules targeting the FOXM1 DNA-binding domain (DBD). Compound XST-20 was identified to effectively suppress FOXM1 transcriptional activities and inhibit ovarian cancer cell proliferation. XST-20 directly interacts with the FOXM1 DNA-binding domain determined by SPR assay. Furthermore, XST-20 was found to significantly reduce the colony-forming efficiency and induce cell cycle arrest and apoptosis. Our study provides a lead compound of FOXM1 inhibitor which may serve as a potential targeted therapy agent for ovarian cancer.
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