您的当前位置：首页 > 行业数据 > TROP-2-ECD二聚体特征（A-顺式，B-反式）

TROP-2-ECD二聚体特征（A-顺式，B-反式）

行业数据

下载图片

原图定位

同报告图片

/ 4

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

所属报告：

医药生物行业：TROP2 ADC行业专题-241226（26页）.pdf

打包全文图表

聚体机制可能限制Trop2裸抗的开发，ADC药物开发更有潜力。基于TROP2在多种实体瘤中差异化高表达的特点，TROP2成为药物开发的潜力靶点。目前全球仅有Trodelvy和SKB264两款TROP2靶向药上市，均为ADC药物。与一般的ADC药物开发相比，Trop2 ADC的开发有其特殊性。一般ADC的开发都是基于已上市的成熟单抗，如HER2 ADC常用的曲妥珠单抗早已于1999年上市，而全球尚未有Trop2单抗上市。既往研究发现，Trop2裸抗在体内模型中并未表现出明显的抗肿瘤活性。这可能与TROP2的聚体机制有关：Trop2分子可以通过低聚物形式参与细胞连接或黏附，并增强介导的信号通路。Trop2可以形成顺式二聚体、反式二聚体，两个二聚体可以形成四聚体。顺式二聚体的形成主要是通过TY和CPD区域相互作用，反式二聚体主要通过CPD区域的β片相互作用，四聚体的形成是通过CRD区域的N端相互作用。研究发现，Trodelvy的抗体部分sacituzumab在Trop2上的结合位点主要是CPD的结构域，并且主要是Q237-Q252 区域的线性表位，该表位的结合可能不会阻碍顺式或者反式二聚体的形成。另一方面，考虑到TROP2的功能十分复杂，在不同瘤种中的作用机制并未完全清楚，直接开发具有抑制功能的单抗或小分子抑制剂风险可能较大，而结合抗体靶向性和小分子杀伤作用的ADC药物或许识别风险，发现价值请务必阅读末页的免责声明是更有潜力的方向（来源：Struc tural insights into the cis and trans assembly of human trophoblast cell surface antigen 2（Meng Sun，iScience）。

行业数据原图定位