The emergence of trophoblast cell-surface antigen 2 (TROP-2) as a novel cancer target.
The emergence of trophoblast cell-surface antigen 2 (TROP-2) as a novel cancer target.
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DOI：
10.18632/oncotarget.25615
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发表时间：
2018-06-22
期刊：
影响因子：
--
通讯作者：
Sharkey RM
中科院分区：
文献类型：
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作者：
Goldenberg DM;Stein R;Sharkey RM
TROP-2 是一种糖蛋白，最初被描述为滋养层细胞的表面标志物，但随后显示其在许多实体癌中表达增加，而在某些正常组织中表达较低。它通过多种信号通路调节癌症的生长、侵袭和扩散，并在干细胞生物学和其他疾病中发挥作用。这篇综述总结了 TROP-2 的特性，尤其是在癌症方面的特性，特别是它作为抗体药物偶联物 (ADC) 或免疫疗法靶标的作用。当伊立替康代谢物 SN-38 与人源化抗 TROP-2 抗体（sacituzumab govitecan）缀合时，它在人类癌症异种移植物以及晚期三阴性乳腺癌、非小细胞和小细胞肺癌以及尿路上皮癌患者中显示出有效的广泛抗癌活性。
TROP-2 is a glycoprotein first described as a surface marker of trophoblast cells, but subsequently shown to be increased in many solid cancers, with lower expression in certain normal tissues. It regulates cancer growth, invasion and spread by several signaling pathways, and has a role in stem cell biology and other diseases. This review summarizes TROP-2's properties, especially in cancer, and particularly its role as a target for antibody-drug conjugates (ADC) or immunotherapy. When the irinotecan metabolite, SN-38, is conjugated to a humanized anti-TROP-2 antibody (sacituzumab govitecan), it shows potent broad anticancer activity in human cancer xenografts and in patients with advanced triple-negative breast, non-small cell and small-cell lung, as well as urothelial cancers.