King T P, Weiner C
Int J Pept Protein Res. 1980 Aug;16(2):147-55. doi: 10.1111/j.1399-3011.1980.tb02948.x.
Alkoxypolyethylene glycols can be converted to O-alkoxypolyethyleneglycoxy-S-carboxamidomethyldithiocarbonates. These dithiocarbonates are useful for the preparation of protein conjugates with alkoxypolyethylene glycols. Studies with model compounds suggest that sites of reaction are primarily the amino groups of proteins and, to a lesser extent, the aliphatic and phenolic hydroxyl groups. Antigen E, which is an allergenic protein from ragweed pollen, was modified with different alkoxypolyethylene glycols by the above procedure. The size and the hydrophobicity of alkoxypolyethylene glycols used were found to influence the reduction in antigenic activity of conjugates.
烷氧基聚乙二醇可转化为O - 烷氧基聚乙二醇氧基 - S - 羧酰胺甲基二硫代碳酸酯。这些二硫代碳酸酯可用于制备与烷氧基聚乙二醇的蛋白质缀合物。对模型化合物的研究表明,反应位点主要是蛋白质的氨基,在较小程度上是脂肪族和酚羟基。通过上述方法用不同的烷氧基聚乙二醇对豚草花粉中的变应原蛋白抗原E进行了修饰。发现所用烷氧基聚乙二醇的大小和疏水性会影响缀合物抗原活性的降低。