含聚[Lys]的支链多肽

F. Hudecz
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引用次数: 1

摘要

本章概述了一组结构相关的具有聚[Lys]骨架的支链聚合多肽的设计、合成、化学和功能表征。已有文献表明,该分支的组成和氨基酸序列可以显著地决定其物理化学特性,包括溶液构象、磷脂单层或双层相互作用以及化合物的生物学特性,如细胞毒性、血液清除率、生物分布、免疫反应性,甚至与化疗药物、肽表位或报告实体的相关生物偶联物。偶联物的合成、结构和功能表征,其中(i)各种抗肿瘤、抗寄生虫化合物(如道诺霉素、甲氨蝶呤、GnRH类似物),(ii)显像剂(如放射性核素、荧光团)或(iii)来自病毒(如单纯疱疹病毒)、细菌(如结核分枝杆菌)和各种疾病(如肿瘤)的B细胞和/或t细胞表位肽;讨论了与阿尔茨海默病(Alzheimer disease)相关的蛋白共价连接到选定的聚[Lys]支链聚合物多肽。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Branched polymeric polypeptides with poly[Lys]
This chapter is to outline the design, synthesis, chemical and functional characterization of a set of structurally related branched polymeric polypeptides with poly[Lys] backbone. It has been documented that the composition and amino acid sequence of the branch could markedly determine the physico-chemical characteristics including solution conformation, the interaction phospholipid mono- or bilayers as well as the biological properties, like cytotoxicity, blood clearance, biodistribution, immunoreactivity of the compound and even related bioconjugates with chemotherapeutic agent, peptide epitope or reporter entity. The synthesis, structural and functional characterization of conjugates, in which (i) various antitumour, antiparasitic compounds (e.g. daunomycin, methotrexate, GnRH analogue), (ii) imaging agents (e.g. radionuclides, fluorophores) or (iii) B- and/or T-cell epitope peptides from viral (e.g. Herpes simplex virus), bacterial (e.g. M. tuberculosis) and various disease (e.g. tumour, Alzheimer disease) related proteins are attached covalently to selected poly[Lys] branched polymeric polypeptides are discussed.
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