Hu Yixuan, Zhu Yinxing, Qi Dan, Tang Cuiju, Zhang Wenwen
Department of Oncology, Nanjing First Hospital, Nanjing Medical University, Nanjing, 210006, China.
Department of Radiation Oncology, The Affiliated Huaian No. 1 People's Hospital of Nanjing Medical University, Huai'an, China.
Biomark Res. 2024 Aug 13;12(1):82. doi: 10.1186/s40364-024-00633-6.
Human trophoblastic cell surface antigen 2 (Trop2) is a glycoprotein, a cellular marker of trophoblastic and stem cells, and a calcium signaling transducer involved in several signaling pathways, leading to the proliferation, invasion, and metastasis of tumors. It is expressed at a low level in normal epithelial cells, but at a high level in many tumors, making it an ideal target for cancer therapy. According to previous literature, Trop2 is broadly expressed in all breast cancer subtypes, especially in triple negative breast cancer (TNBC). Several clinical trials have demonstrated the effectiveness of Trop2-targeted therapy in breast cancer. Sacituzumab govitecan (SG) is a Trop2-targeted antibody-drug conjugate (ADC) that has been approved for the treatment of metastatic TNBC and hormone receptor-positive (HR+) and human epidermal growth factor receptor 2-negative (HER2-) breast cancer. This article reviews the structure and function of Trop2, several major Trop2-targeted ADCs, other appealing novel Trop2-targeted agents and relevant clinical trials to provide a landscape of how Trop2-targeted treatments will develop in the future.
人滋养层细胞表面抗原2（Trop2）是一种糖蛋白，是滋养层细胞和干细胞的细胞标志物，也是一种参与多种信号通路的钙信号转导分子，可导致肿瘤的增殖、侵袭和转移。它在正常上皮细胞中低表达，但在许多肿瘤中高表达，使其成为癌症治疗的理想靶点。根据以往文献，Trop2在所有乳腺癌亚型中广泛表达，尤其是在三阴性乳腺癌（TNBC）中。多项临床试验已证明Trop2靶向治疗在乳腺癌中的有效性。戈沙妥珠单抗（SG）是一种Trop2靶向抗体药物偶联物（ADC），已被批准用于治疗转移性TNBC以及激素受体阳性（HR+）和人表皮生长因子受体2阴性（HER2-）乳腺癌。本文综述了Trop2的结构和功能、几种主要的Trop2靶向ADC、其他有吸引力的新型Trop2靶向药物以及相关临床试验，以展现Trop2靶向治疗未来的发展前景。
