Biosciences Laboratory, IRCCS Istituto Romagnolo per lo Studio dei Tumori (IRST) "Dino Amadori", Meldola, Italy.
Department of Medical Oncology, IRCCS Istituto Romagnolo per lo Studio dei Tumori (IRST) "Dino Amadori", Meldola, Italy.
Expert Opin Ther Targets. 2022 Jul;26(7):593-602. doi: 10.1080/14728222.2022.2113513. Epub 2022 Aug 19.
Breast cancer (BC) is the most common diagnosed cancer and the second leading cause of cancer-associated death in women, with the triple negative (TNBC) subtype being characterized by the poorest prognosis. New therapeutic targets are urgently needed to overcome the high metastatic potential, aggressiveness and poor survival of these tumors. Trop2 transmembrane glycoprotein, acting as an intracellular calcium signal transducer, recently emerged as a new potential target in epithelial cancers, in particular in breast cancer.
We summarize the key features of Trop2 structure and function, describing the therapeutic strategies targeting this protein in cancer. Particular attention is paid to antibody-drug conjugates (ADCs), actually representing the most successful strategy.
ADCs targeting Trop2 recently received an accelerated FDA approval for the therapy of metastatic TNBC. The prospects for these novel ADCs in BC subtypes other than TNBC are discussed, taking into account the main pitfalls relative to Trop2 structure and function.
乳腺癌（BC）是最常见的诊断癌症，也是女性癌症相关死亡的第二大主要原因，三阴性（TNBC）亚型的特点是预后最差。迫切需要新的治疗靶点来克服这些肿瘤的高转移潜力、侵袭性和不良生存率。Trop2 跨膜糖蛋白作为细胞内钙信号转导器，最近作为上皮癌特别是乳腺癌的一个新的潜在靶点出现。
我们总结了 Trop2 结构和功能的关键特征，描述了针对该蛋白的癌症治疗策略。特别关注针对 Trop2 的抗体药物偶联物（ADC），这实际上是最成功的策略。
针对 Trop2 的 ADC 最近获得了 FDA 对转移性 TNBC 治疗的加速批准。讨论了这些新型 ADC 在除 TNBC 以外的 BC 亚型中的应用前景，同时考虑了与 Trop2 结构和功能相关的主要缺陷。
