|国家预印本平台
首页|双功能抗体募集分子DNP-LHRH的合成

双功能抗体募集分子DNP-LHRH的合成

Synthesis of bifunctional molecules DNP-LHRH recruiting endogeous antibody

中文摘要英文摘要

促黄体激素释放激素(LHRH)是由10个氨基酸组成的多肽,可以特异性结合过表达LHRH受体的癌细胞,现已用于靶向性抗肿瘤药物的研发。本文首先通过多肽固相合成方法合成侧链带叠氮基团的LHRH多肽类似物;其次,通过化学方法设计并分别合成含有2、4和8个乙二醇重复单元连接臂的2,4-二硝基苯(DNP)衍生物;最后,通过点击化学反应,将DNP衍生物与LHRH类似物偶联成为抗体募集分子候选物DNP-LHRH。该双功能抗体募集分子有望招募血清中抗DNP抗体至过表达LHRH受体癌细胞表面,通过激发机体的免疫反应,对肿瘤细胞产生杀伤。

Luteinizing hormone releasing hormone (LHRH) is a polypeptide consisting of 10 amino acids that specifically binds onto cancer cells overexpressing LHRH receptors, and then it has been used in the development of targeted anti-tumor drugs. In this paper, the LHRH peptide analogue with azide group was synthesized by peptide solid phase synthesis method. Secondly, 2,4-dinitrobenzene (DNP) derivativescontaining 2, 4 and 8 ethylene glycol repeat unit linkerwere synthesized respectively.Finally, DNP derivatives were coupled to the LHRH analogto acquire antibody recruitment molecules DNP-LHRH. via a click chemical reaction. These bifunctional antibody recruiting moleculesare expected to combine with anti-DNP antibodies in serum and then deliver to overexpressing LHRH receptors cancer cells surface, which would be destroyedby exciting the immune response.

周志昉、吴志猛、王金凤

药学生物化学分子生物学

免疫治疗促黄体激素释放激素24-二硝基苯点击化学

Immunity therapyLHRHDNPClick reaction

周志昉,吴志猛,王金凤.双功能抗体募集分子DNP-LHRH的合成[EB/OL].(2020-01-21)[2025-08-18].http://www.paper.edu.cn/releasepaper/content/202001-110.点此复制

评论