State Key Laboratory of Medicinal Chemical Biology and College of Pharmacy, The Haihe Laboratory of Cell Ecosystem, Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin, 300350, China.
Department of Pharmacology, Second Military Medical University/Naval Medical University, Shanghai, 200433, China.
Biol Res. 2024 Nov 24;57(1):90. doi: 10.1186/s40659-024-00566-2.
The establishment of apicobasal polarity in epithelial cells is of critical importance in morphogenesis of mammary gland and other secretive gland tissues. The demise of the polarity is a critical step in early stages of tumorigenesis such as in breast ductal carcinoma in situ. The underlying molecular mechanism thus warrants in-depth investigations.
Protein kinase C isoform ζ (PKCζ), which is highly expressed in breast cancer cells, accumulates in the nuclei of human mammary epithelial cells overexpressing human rhomboid family-1 (RHBDF1), an endoplasmic reticulum membrane protein. Nuclear translocation of PKCζ results in the failure of the formation of the cytosolic apicobasal polarity complex Par, of which PKCζ is an essential component. Additionally, enhanced nuclear translocation of PKCζ is accompanied by an inhibition of the expression of cell tight junction and adherens junction proteins and an increase of cell mobility. Mechanistically, RHBDF1 is able to interact with importin β1 and PKCζ and promote PKCζ phosphorylation. Consistently, treatment of RHBDF1-overexpressing cells with an inhibitor of PKCζ phosphorylation leads to restoration of apicobasal polarity and cell-cell junctions, as well as suppressed cell mobility.
RHBDF1-facilitated nuclear translocation of PKCζ is critically responsible for the dismantlement of epithelial cell apicobasal polarity, and thus may serve as a target in the development of therapeutic approaches against early stages of breast cancer.
上皮细胞中顶端-基底极性的建立对于乳腺和其他分泌腺组织的形态发生至关重要。极性的丧失是肿瘤发生早期的关键步骤,如乳腺导管原位癌。因此,其潜在的分子机制值得深入研究。
蛋白激酶 C 同工型 ζ(PKCζ)在乳腺癌细胞中高度表达,在过表达人菱形家族 1(RHBDF1)的人乳腺上皮细胞中积累在核内,RHBDF1 是内质网膜蛋白。PKCζ 的核易位导致细胞质顶端-基底极性复合物 Par 的形成失败,PKCζ 是其必不可少的组成部分。此外,PKCζ 核易位增强伴随着细胞紧密连接和黏着连接蛋白表达的抑制以及细胞迁移性的增加。在机制上,RHBDF1 能够与输入蛋白β1 和 PKCζ 相互作用并促进 PKCζ 的磷酸化。一致地,用 PKCζ 磷酸化抑制剂处理过表达 RHBDF1 的细胞导致顶端-基底极性和细胞-细胞连接的恢复,以及抑制细胞迁移性。
RHBDF1 促进 PKCζ 的核易位对于上皮细胞顶端-基底极性的解体至关重要,因此可能成为针对乳腺癌早期阶段的治疗方法开发的靶点。