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肝半乳糖基受体存在于哺乳动物肝细胞内和膜上,特异性识别结合血浆去唾液酸糖蛋白的末端半乳糖基。利用这种受体与其配体相互识别结合的机制,可以把连接到配体上的药物定向转运到肝细胞内,进行肝病的导向诊断和治疗。人工半合成的糖化白蛋白和合成糖肽同样被肝半乳糖受体所识别结合,在体内具有一定的肝脏选择性,可用于药物的导向转运。本文报道从游离乳糖和L-赖氨酸出发,经保护、接肽、糖化等十几步反应,制备肝半乳糖受体的配体糖肽——三-(3-S-硫代乳糖基丙酰)二聚赖氨酸甲酯。应用了新的HOEC活性酯方法,进行二肽糖化,产物和中间体的化学结构经光谱、比色和元素分析等证实,配体糖肽的受体亲和力待测。
Hepatic galactosyl receptors are present in mammalian hepatocytes and on membranes and specifically recognize terminal galactosyl groups that bind to plasma asialoglycoprotein. Using this receptor and its ligand mutual recognition of the binding mechanism, can be connected to the ligand drug delivery to liver cells oriented, diagnosis and treatment of liver disease-oriented. Artificial semi-synthetic glycated albumin and synthetic glycopeptide are also recognized by the liver galactose receptor recognition, in the liver has a certain degree of selectivity, can be used for drug delivery. In this paper, starting from free lactose and L-lysine, glycopeptide-tris- (3-S-thiogalactosyl Propionyl) dimer-lysine methyl ester. The new HOEC active ester method was applied to the dipeptide saccharification. The chemical structures of the products and the intermediates were confirmed by spectroscopic, colorimetric and elemental analysis, and the acceptor affinity of the ligand glycopeptide was tested.