Yin Linglong, Dai Yi, Wang Yue, Liu Shiwen, Ye Yubing, Fu Yongming, Peng Yuchong, Tan Ruizheng, Fang Li, Suo Haoran, Qi Xuli, Yuan Bowen, Gao Yingxue, Liu Youhong, Li Xiong
Key Laboratory of Clinical Precision Pharmacy of Guangdong Higher Education Institutes, The First Affiliated Hospital, Guangdong Pharmaceutical University, Guangzhou, 510699, China.
Key Specialty of Clinical Pharmacy, The First Affiliated Hospital, Guangdong Pharmaceutical University, Guangzhou, 510699, China.
Oncogene. 2025 Jun;44(21):1567-1577. doi: 10.1038/s41388-025-03328-w. Epub 2025 Mar 6.
Prostate cancer (PCa) is an androgen-dependent malignancy, with HSP90 and HSP70 serving as classical molecular chaperones that maintain androgen receptor (AR) protein stability and regulate its transcriptional activation. Surprisingly, our study identified TOMM20, a mitochondrial outer membrane protein, as a potential molecular chaperone with similar roles to HSP90/HSP70. We found that TOMM20 expression is elevated in PCa tissues and cell lines and positively correlates with AR levels. RNA-seq analysis revealed that TOMM20 knockdown significantly reduced the mRNA levels of AR-regulated genes. Additionally, the protein level of KLK3 (PSA) decreased, and AR binding to the androgen response element (ARE) of the KLK3 promoter was diminished following TOMM20 knockdown, leading to decreased KLK3 gene transcription. Furthermore, TOMM20 depletion reduced both cytoplasmic and nuclear AR protein levels and facilitated AR degradation via an E3 ubiquitin ligase SKP2-mediated ubiquitin-proteasome pathway, independent of heat shock proteins (HSPs). To our knowledge, this is the first report demonstrating that TOMM20, a mitochondrial outer translocase protein, stabilizes AR protein and enhances its transcriptional activity, while its knockdown promotes AR degradation through the SKP2-mediated ubiquitin-proteasome pathway. These findings suggest that TOMM20 may serve as a potential biomarker for PCa progression and a promising therapeutic target for drug development.
前列腺癌(PCa)是一种雄激素依赖性恶性肿瘤,热休克蛋白90(HSP90)和热休克蛋白70(HSP70)作为经典分子伴侣,维持雄激素受体(AR)蛋白稳定性并调节其转录激活。令人惊讶的是,我们的研究发现线粒体外膜蛋白TOMM20是一种具有与HSP90/HSP70类似作用的潜在分子伴侣。我们发现TOMM20在PCa组织和细胞系中表达升高,且与AR水平呈正相关。RNA测序分析显示,敲低TOMM20可显著降低AR调控基因的mRNA水平。此外,敲低TOMM20后,激肽释放酶3(KLK3,前列腺特异性抗原)的蛋白水平降低,AR与KLK3启动子雄激素反应元件(ARE)的结合减少,导致KLK3基因转录减少。此外,TOMM20缺失降低了细胞质和细胞核中的AR蛋白水平,并通过E3泛素连接酶SKP2介导的泛素-蛋白酶体途径促进AR降解,这一过程独立于热休克蛋白(HSPs)。据我们所知,这是首次报道表明线粒体外转运酶蛋白TOMM20可稳定AR蛋白并增强其转录活性,而敲低TOMM20则通过SKP2介导的泛素-蛋白酶体途径促进AR降解。这些发现表明,TOMM20可能作为PCa进展的潜在生物标志物以及药物开发的有前景的治疗靶点。