Glycopeptide dendrimers. Part II.

Glycopeptide dendrimers are regularly branched structures containing both carbohydrates and peptides. Various types of these compounds differing in composition and structure are mentioned, together with their practical use spanning from catalysis, transport vehicles to synthetic vaccines. This Part II (for Part I see JeZek J, et al., J. Pept. Sci. 2008; 14: 2-43) covers linear oligomers with variable valency (brush dendrimers, comb dendrimers), sequential oligopeptide carriers SOCn-I and SOCn-II, chitosan-based dendrimers, and brush dendrimers. Other types of glycopeptide dendrimers are self-immolative dendrimers (cascade release dendrimers, domino dendrimers), dendrimers containing omega-amino acids (Gly, beta-Ala, gamma-Abu and epsilon-aminohexanoic acid), etc. Microwave-assisted synthesis of dendrimers and libraries of glycopeptides and glycopeptide dendrimers are also included. Characterization of dendrimers by electromigration methods, mass spectrometry, and time-resolved and nonlinear optical spectroscopy, etc. plays an important role in purity assessment and structure characterization. Physicochemical properties of dendrimers including chirality are given. Stability of dendrimers, their biocompatibility and toxicity are reviewed. Finally, biomedical applications of dendrimers including imaging agents (contrast agents), site-specific drug delivery systems, artificial viruses, synthetic antibacterial, antiviral, and anticancer vaccines, inhibitors of cell surface protein-carbohydrate interactions, intervention with bacterial adhesion, etc. are given. Glycopeptide dendrimers were used also for studying recognition processes, as diagnostics and mimetics, for complexation of different cations, for therapeutic purposes, as immunodiagnostics, and in drug design.     

Glycopeptide dendrimers. Part I.

Glycopeptide dendrimers are branched structures containing both carbohydrates and peptides. Various classes of these compounds differing in composition and structure are mentioned, together with their practical use spanning from catalysis, transport vehicles to synthetic vaccines. The main stress is given to glycopeptide dendrimers, namely multiple antigen glycopeptides (MAGs). In MAGs, the core, branches or both are composed of amino acids or peptides. Other classes of glycodendrimers (PAMAM, polypropylene imine, cyclodextrin, calixarene, etc.) are mentioned too, but to a smaller extent. Their syntheses, physicochemical properties and biological activities are given with many examples. Glycopeptide dendrimers can be used as inhibitors of cell surface protein-carbohydrate interactions, intervention with bacterial adhesion, for studying of recognition processes, diagnostics, imaging and contrast agents, mimetics, for complexation of different cationts, as site-specific molecular delivery systems, for therapeutic purposes, as immunodiagnostics and in drug design. Biomedical applications of glycopeptide dendrimers as drug and gene delivery systems are also given.     

Peptide and glycopeptide dendrimers. Part II

Recent progress in peptide and glycopeptide chemistry make the preparation of peptide and glycopeptide dendrimers of acceptable purity, with designed structural and immunochemical properties reliable. New methodologies using unprotected peptide building blocks have been developed to further increase the possibilities of their design and improve their preparation and separation. The sophisticated design of peptide and glycopeptide dendrimers has led to their use as antigens and immunogens, for serodiagnosis and other biochemical uses including drug delivery. Dendrimers bearing peptide with predetermined secondary structures are useful tools in protein de novo design. This article covers synthesis and applications of multiple antigen peptides (MAPs), multiple antigen glycopeptides (MAGs), multiple antigen peptides based on sequential oligopeptide carriers (MAP‐SOCs), glycodendrimers and template‐assembled synthetic proteins (TASPs). In part II the preparation of MAPs, and the utility of glycodendrimers and TASPs are discussed. Copyright © 1999 European Peptide Society and John Wiley & Sons, Ltd.     

Peptide and glycopeptide dendrimers. Part I

Recent progress in peptide and glycopeptide chemistry make the preparation of peptide and glycopeptide dendrimers of acceptable purity, with designed structural and immunochemical properties reliable. New methodologies using unprotected peptide building blocks have been developed to further increase possibilities of their design and improve their preparation and separation. Sophisticated design of peptide and glycopeptide dendrimers has led to their use as antigens and immunogens, for serodiagnosis and other biochemical uses including drug delivery. Dendrimers bearing peptide with predetermined secondary structures are useful tools in protein de novo design. This article covers synthesis and applications of multiple antigen peptides (MAPs), multiple antigen glycopeptides (MAGs), multiple antigen peptides based on sequential oligopeptide carriers (MAP‐SOCs), glycodendrimers and template‐assembled synthetic proteins (TASPs). Part I deals with the development of various structural forms of MAPs as well as their application as antigens, immunogens, and for immunodiagnostic and biochemical purposes. Copyright © 1999 European Peptide Society and John Wiley & Sons, Ltd.     

Solid phase synthesis of glycopeptide dendrimers with Tn antigenic structure and their biological activities. Part I

Multiple antigenic peptides containing dimeric Tn antigen [Ac‐(Tn)₂‐γ‐Abu]₄‐(Lys‐X)₂‐Lys‐β‐Ala ( V : X=0; VIII : X=γ‐Abu) and [Ac‐(Tn)₂‐γ‐Abu]₈‐(Lys‐X)₄‐(Lys‐X)₂‐Lys‐β‐Ala ( XI : X=0; XIV : X=γ‐Abu), immobilized on biocompatible Tenta Gel S NH₂ support were prepared by SPPS. Rosetting tests of V , VIII , XI and XIV showed positive reactions with anti‐Tn (DAKO) and Tn+ erythrocytes, with anti‐Tn/A (BRIC 66) and Tn+ and A erythrocytes, other combinations were negative. In all the animals immunized with XIV , we found a remarkable increase in the level of anti‐Tn (titre 2000–64 000, score 105–167) and no change of anti‐A levels (titre 8, score 13–17). Neither non‐immune nor immune sera showed any reactivity with T⁺, Cad⁺ and blood group O erythrocytes. Immunized mice did not exhibit any sign of adverse reaction to the administered conjugates. Biological activities were correlated with molecular modelling and molecular dynamic calculations. The biological activities of these synthetic Tn antigen conjugates (good availability for the immunological interactions, highly specific immunogenicity, good biological tolerance) together with their precise chemical characterization seem to be a promising approach to preparation of anti‐tumour vaccine and affinity purification of anti‐Tn antibodies. Copyright © 1999 European Peptide Society and John Wiley & Sons, Ltd.     

功能化量子点在肿瘤诊治中的应用

量子点是一种半导体纳米晶体,它可发出激发荧光,具有亮度高、稳定时间长和发射光谱可调节等特性,是同时检测多信号的良好材料.这些独特性质使得它们在肿瘤诊治领域中的应用日益受到人们的重视.对量子点进行功能化修饰,如偶联抗体等活性物质后,可以对肿瘤细胞进行特异性识别及示踪,以实现对肿瘤的诊断和治疗.文中分别从分子靶向识别、淋巴结定位和药物传递等方面探讨了功能化量子点在肿瘤诊断和治疗中的最新进展.此外,还讨论了量子点的毒性以及用于肿瘤检测和治疗的多功能量子点的设计方法,并提出了其实际应用的潜在方向.