摘要
肿瘤靶向肽偶联药物是一类由线性或环状多肽组成的新型靶向偶联药物,具有不良反应少、靶向特异性高及疗效显著等特点,已成为近年来抗肿瘤药物研发的新热点。但其在体内代谢快、药物稳定性差,因此合理的药物设计与合成至关重要。本文总结了噬菌体展示技术、化学合成肽库筛选和计算机模拟设计等最新肿瘤靶向肽的筛选方法,同时讨论了细胞毒性载荷种类及连接基团特征等关键问题,并对肿瘤靶向肽偶联药物的设计原则和最新进展进行介绍。
Tumor targeting peptide-drug conjugates, which are usually composed of linear or cyclic peptides, has become hotspot in recent years for its characteristics of less adverse reactions, increased specificity and improved efficacy. However, due to the instability of peptides and short effective half-life in vivo, rational drug design and synthesis become the key point. The lasted selection methods of tumor targeting peptides which include phage display technology, screening of synthetic peptide library and computer simulation design were summerized, the types of cytotoxic loading and the characteristics of ligand groups were discussed, and the principles of design and the recent developments of tumor targeting peptide-drug conjugates were introduced in this article.
作者
刘巾玮
魏敏杰
LIU Jin-wei;WEI Min-jie(Department of Pharmacology,College of Pharmacy,China Medical University,Shenyang LIAONING 110122,China;Department of Pharmacy,Chifeng Municipal Hospital,Chifeng INNER MONGOLIA 024000,China)
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2020年第3期129-134,共6页
Chinese Journal of New Drugs and Clinical Remedies
关键词
药物设计
药物释放系统
抗肿瘤药
肿瘤靶向肽
多肽偶联药物
drug design
drug delivery systems
antineoplastic agents
tumor targeting peptides
peptide-drug conjugates
