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          抗體藥物偶聯(lián)物ADC-抗體與藥物連接位點(diǎn)的選擇
          發(fā)布時(shí)間:2020-10-26     作者:axc   分享到:

          抗體藥物偶聯(lián)物ADC-抗體與藥物連接位點(diǎn)的選擇

          西安pg電子官方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(gòu)

          抗體藥物偶聯(lián)物(antibody-drug conjugate,ADC)是通過(guò)一個(gè)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(yùn)輸?shù)侥繕?biāo)細(xì)胞中,

          抗體是一類具有特殊親和力的蛋白,利用其對(duì)靶細(xì)胞特異性的結(jié)合,有望作為藥物靶向遞送的載體,進(jìn)而增強(qiáng)藥物的選擇性。

          image.png

          抗體與藥物連接位點(diǎn)的選擇:

          對(duì)抗體進(jìn)行藥物偶聯(lián)時(shí),往往使用帶有特殊側(cè)鏈的氨基酸作為反應(yīng)位點(diǎn)。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(duì)其進(jìn)行還原為自由巰基進(jìn)行下一步反應(yīng)。其中在抗體(IgG)鏈間有4對(duì)二硫鍵,比較容易被還原。而在抗體鏈內(nèi),有12對(duì)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(gè)賴氨酸殘基,其中有大約20個(gè)賴氨酸殘基可作為連接位點(diǎn)。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(diǎn)也是可行的。

          image.png

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