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HER2是一种具有酪氨酸激酶活性的跨膜糖蛋白 ,它的过表达与肿瘤形成、恶性程度及预后密切相关。根据HER2的结构及其介导的信号转导途径 ,已研制开发出一系列HER2受体抑制剂。抗HER2抗体通过加速受体内化 ,阻止HER2与其他表皮生长因子受体 (EGFR)家族成员形成异二聚体来阻断HER2的功能 ;一系列喹唑啉类小分子化合物能共价结合EGFR和HER2的ATP结合位点 ,阻断受体酪氨酸激酶活性 ;多瘤病毒增强子激活因子 3(PEA3)和人腺病毒 5型早期区 1A(E1A)蛋白在转录或翻译水平下调HER2的表达 ;细胞内表达的 6 8和 10 0kuHER2 胞外区结构域能干扰HER2异二聚体的形成及其信号转导。
HER2 is a transmembrane glycoprotein with tyrosine kinase activity. Its overexpression is closely related to tumor formation, malignancy and prognosis. According to the structure of HER2 and its signal transduction pathways, a series of HER2 receptor inhibitors have been developed. Anti-HER2 antibodies block the function of HER2 by accelerating receptor internalization and preventing HER2 from forming heterodimers with other members of the epidermal growth factor receptor (EGFR) family; a series of quinazoline-based small molecule compounds can covalently bind to EGFR And HER2 ATP-binding sites, blocking receptor tyrosine kinase activity; polyoma virus enhancer activator 3 (PEA3) and human adenovirus type 5 early region 1A (E1A) protein downregulate HER2 transcription or translation The expression of the extracellular domains of 68 and 100kuHER2 in cells can interfere with the formation of HER2 heterodimer and its signal transduction.