含二硫键多肽药物在肿瘤治疗中的研究进展  

Progress of Chemically Synthesized Disulfide-containing Peptide Drugs in Tumor Therapy

作　　者：高冰 李凌木 程志刚 郭叶 GAO Bing;LI Ling-mu;CHENG Zhi-gang;GUO Ye(School of Pharmacy,Baotou Medical College,Baotou 014060,China)

机构地区：[1]包头医学院药学院,内蒙古包头014060

出　　处：《药物生物技术》2020年第3期269-273,共5页Pharmaceutical Biotechnology

基　　金：国家自然科学基金资助项目(No.21602121,No.21967017)。

摘　　要：含二硫键多肽药物是一类多肽序列中至少含有一对二硫键的药物,它们在治疗代谢性、消化系统等疾病中发挥着不可替代的作用。已有研究证实二硫键的存在对于维持多肽的结构和功能起着至关重要的作用。二硫键不仅赋予了多肽多种多样的生物活性,而且使多肽结构被锁定具有强的化学稳定性、酶稳定性、热稳定性。目前,已有数十种化学合成含二硫键多肽上市用于治疗肿瘤、糖尿病、中枢性尿崩症、肠道易激综合症等重大疾病,更多的含二硫键多肽也处于临床研究阶段。文章总结了近年来对治疗、诊断肿瘤起到重要作用的5个化学合成含二硫键多肽药物的发现、结构及活性优化、药用机制以及合成方法,希望为今后多肽类肿瘤药物的研发提供理论参考。Disulfide-containing peptide drugs represent a class of peptides containing at least one disulfide bond.They play a key role in the treatment of metabolic,digestive and other diseases.It had been demonstrated that disulfide bonds play an important role in maintaining the structure and function of the polypeptides.The disulfide bonds enable peptides to exhibit a wide variety of biological activity,high chemical stability,and enzyme and thermal stability.Nowadays,a good number of chemically synthesized disulfide-containing peptides have been approved for the treatment of tumors,diabetes,central diabetes insipidus,irritable bowel syndrome.More disulfide-containing peptides are in clinical research stage.The discovery,structure and activity optimization,medicinal mechanism and synthetic methods of 5 chemically synthesized disulfide-containing peptide drugs in the treatment and diagnosis of tumor were reviewed in recent years.It was hoped to provide theoretical reference for the research and development of anti-tumor peptide drugs.

关 键 词：含二硫键多肽 氧化折叠 化学合成 多肽药物 肿瘤治疗 生长抑制素 

分 类 号：R9[医药卫生—药学]