發(fā)布時(shí)間：2018-03-10 18:55

  本文選題：抗體偶聯(lián)藥物　切入點(diǎn)：內(nèi)吞作用　出處：《中國新藥雜志》2017年10期 　論文類型：期刊論文

【摘要】：抗體偶聯(lián)藥物(antibody-drug conjugate,ADC)由單克隆抗體和小分子細(xì)胞毒藥物通過化學(xué)連接子連接,兼顧了單克隆抗體的選擇性和小分子藥物的細(xì)胞毒效力。ADC進(jìn)入體內(nèi)后,可通過單克隆抗體的靶向作用結(jié)合于腫瘤表面的靶抗原,經(jīng)內(nèi)吞作用進(jìn)入細(xì)胞內(nèi),在溶酶體的化學(xué)或酶促作用下釋放小分子細(xì)胞毒藥物導(dǎo)致靶細(xì)胞死亡。ADC的內(nèi)吞作用是ADC發(fā)揮藥效的關(guān)鍵,并且已經(jīng)成為ADC開發(fā)階段的重要部分。由于缺乏對于ADC內(nèi)吞作用的整體認(rèn)識,目前對于內(nèi)吞效率和內(nèi)吞機(jī)制的研究方法開發(fā)存在著諸多挑戰(zhàn)。本文對ADC的內(nèi)吞機(jī)制、影響因素和研究方法等方面的進(jìn)展進(jìn)行了綜合歸納和闡述。
[Abstract]:The antibody-drug conjugate drug (ADCC) was linked by monoclonal antibody and small molecular cytotoxic drug via chemical linker, which took into account the selectivity of monoclonal antibody and the cytotoxicity of small molecule drug. ADC entered the body. The target antigen that binds to the surface of the tumor through the targeting action of monoclonal antibody and enters the cell through endocytosis. The endocytosis of the target cell death caused by the release of small molecular cytotoxic drugs under the chemical or enzymatic action of lysosome is the key to the effect of ADC. And has become an important part of the ADC development stage. Due to the lack of overall understanding of the endocytosis of ADC, there are many challenges to the development of endocytosis efficiency and endocytosis mechanism. This paper discusses the endocytosis mechanism of ADC. The development of influencing factors and research methods are summarized and expounded.
【作者單位】： 中國藥科大學(xué)江蘇省藥物代謝動(dòng)力學(xué)重點(diǎn)實(shí)驗(yàn)室;天士力集團(tuán)研究院藥理毒理研究中心;
【分類號】：R945
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本文編號：1594629