抗體藥物偶聯(lián)物ADC-抗體與藥物連接位點的選擇
西安齊岳生物科技有限公司是科研材料供應(yīng)商,我們提供的產(chǎn)品性質(zhì)穩(wěn)定 、均有現(xiàn)貨,現(xiàn)我公司新上市一些小分子/ADC-抗體偶聯(lián)藥物/粒子液體可咨詢訂購
抗體藥物偶聯(lián)物(antibody-drug conjugate,ADC)是通過一個化學(xué)鏈接將具有生物活性的小分子藥物連接到單抗上,單抗作為載體將小分子藥物靶向運輸?shù)侥繕?biāo)細胞中,
抗體是一類具有特殊親和力的蛋白,利用其對靶細胞特異性的結(jié)合,有望作為藥物靶向遞送的載體,進而增強藥物的選擇性。
抗體與藥物連接位點的選擇:
對抗體進行藥物偶聯(lián)時,往往使用帶有特殊側(cè)鏈的氨基酸作為反應(yīng)位點。其中以半胱氨酸和賴氨酸為主。半胱氨酸在抗體中以二硫鍵的形式存在,因此需要對其進行還原為自由巰基進行下一步反應(yīng)。其中在抗體(IgG)鏈間有4對二硫鍵,比較容易被還原。而在抗體鏈內(nèi),有12對二硫鍵,較難被還原。賴氨酸則分布于抗體結(jié)構(gòu)域,大約有86個賴氨酸殘基,其中有大約20個賴氨酸殘基可作為連接位點。除選擇氨基酸殘基外,選取保守糖基化的多糖作為修飾位點也是可行的。
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