Matsubara Teruhiko
Department of Biosciences and Informatics, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kouhoku, Yokohama 223-8522, Japan.
J Nucleic Acids. 2012;2012:740982. doi: 10.1155/2012/740982. Epub 2012 Oct 10.
Glycoconjugates play various roles in biological processes. In particular, oligosaccharides on the surface of animal cells are involved in virus infection and cell-cell communication. Inhibitors of carbohydrate-protein interactions are potential antiviral drugs. Several anti-influenza drugs such as oseltamivir and zanamivir are derivatives of sialic acid, which inhibits neuraminidase. However, it is very difficult to prepare a diverse range of sugar derivatives by chemical synthesis or by the isolation of natural products. In addition, the pathogenic capsular polysaccharides of bacteria are carbohydrate antigens, for which a safe and efficacious method of vaccination is required. Phage-display technology has been improved to enable the identification of peptides that bind to carbohydrate-binding proteins, such as lectins and antibodies, from a large repertoire of peptide sequences. These peptides are known as "carbohydrate-mimetic peptides (CMPs)" because they mimic carbohydrate structures. Compared to carbohydrate derivatives, it is easy to prepare mono- and multivalent peptides and then to modify them to create various derivatives. Such mimetic peptides are available as peptide inhibitors of carbohydrate-protein interactions and peptide mimotopes that are conjugated with adjuvant for vaccination.
糖缀合物在生物过程中发挥着多种作用。特别是，动物细胞表面的寡糖参与病毒感染和细胞间通讯。碳水化合物 - 蛋白质相互作用的抑制剂是潜在的抗病毒药物。几种抗流感药物，如奥司他韦和扎那米韦，都是唾液酸的衍生物，可抑制神经氨酸酶。然而，通过化学合成或天然产物分离来制备多种糖衍生物非常困难。此外，细菌的致病荚膜多糖是碳水化合物抗原，需要一种安全有效的疫苗接种方法。噬菌体展示技术已经得到改进，能够从大量肽序列中鉴定出与碳水化合物结合蛋白（如凝集素和抗体）结合 的肽。这些肽被称为“碳水化合物模拟肽（CMP）”，因为它们模拟碳水化合物结构。与碳水化合物衍生物相比，制备单价和多价肽然后对其进行修饰以产生各种衍生物很容易。这种模拟肽可作为碳水化合物 - 蛋白质相互作用的肽抑制剂以及与佐剂缀合用于疫苗接种的肽模拟表位。
