Han Meng-Ting, Pei Hua, Sun Qi-Qi, Wang Cheng-Long, Li Peng, Xie Ya-Ya, Cao Li-Jun, Zhang Xing-Xing, Sun Zhen-Liang
Anhui University of Science and Technology Huainan 232001, Anhui, China.
Fengxian Hospital Affiliated to Anhui University of Science and Technology Shanghai 201499, China.
Am J Cancer Res. 2023 Apr 15;13(4):1533-1546. eCollection 2023.
Prostate cancer is one of the most lethal malignancies, and androgen deprivation therapy remains the mainstay of treatment for prostate cancer patients. Although androgen deprivation can initially come to remission, the disease often develops into castration-resistant prostate cancer (CRPC), which is still dependent on androgen receptor (AR) signaling and is related to a poor prognosis. Some success against CRPC has been achieved by drugs that target AR signaling, but secondary resistance uninterrupted emerges, and new therapies are urgently needed. In this study, we identified a potent small molecule compound, ZY-444, that suppressed PCa cells proliferation and metastasis, and inhibited tumor growth both in subcutaneous. Transcriptome sequencing analysis showed that TNFAIP3 was significantly elevated in prostate cancer cells after ZY-444 treatment. Further studies through overexpression of TNFAIP3 confirmed that TNFAIP3, as a direct target gene of ZY-444, contributes to the functions of ZY-444. In addition, we demonstrated the effects of TNFAIP3 on prostate cancer cell apoptosis, migration and proliferation to elucidate the mechanism of ZY-444. We found that TNFAIP3 inhibited the TNF signaling pathway, which could inhibit cell migration and proliferation and contribute to apoptosis. Overall, these findings highlighted TNFAIP3 as a tumor suppressor gene in the regulation of the progression and metastatic potential of prostate cancer and that targeting TNFAIP3 by ZY-444 might be a promising strategy for prostate cancer treatment.
前列腺癌是最致命的恶性肿瘤之一,雄激素剥夺疗法仍然是前列腺癌患者的主要治疗方法。虽然雄激素剥夺最初可以使病情缓解,但该疾病通常会发展为去势抵抗性前列腺癌(CRPC),其仍然依赖雄激素受体(AR)信号传导,且预后较差。针对CRPC,通过靶向AR信号传导的药物已取得了一些成效,但继发性耐药仍不断出现,因此迫切需要新的治疗方法。在本研究中,我们鉴定出一种有效的小分子化合物ZY-444,它能抑制前列腺癌细胞的增殖和转移,并在皮下抑制肿瘤生长。转录组测序分析表明,ZY-444处理后的前列腺癌细胞中TNFAIP3显著上调。通过过表达TNFAIP3的进一步研究证实,TNFAIP3作为ZY-444的直接靶基因,对ZY-444的功能起作用。此外,我们证明了TNFAIP3对前列腺癌细胞凋亡、迁移和增殖的影响,以阐明ZY-444的作用机制。我们发现TNFAIP3抑制TNF信号通路,这可以抑制细胞迁移和增殖并促进细胞凋亡。总体而言,这些发现突出了TNFAIP3作为前列腺癌进展和转移潜能调节中的肿瘤抑制基因,并且通过ZY-444靶向TNFAIP3可能是一种有前景的前列腺癌治疗策略。