| 摘要 |
A process is provided for coupling glycols to macromolecules through glycosylations on those macromolecules, rather than through amino or carboxyl groups on the macromolecule backbone. This produces macromolecules having decreased immunogenic response, and maintained activity. The present process for glycolation of a glycosylated macromolecule comprises activating a polyalkylene glycol; reacting the activated polyalkylene glycol with a diamino compound, whereby the activated polyalkylene glycol is coupled to the diamino compound through one of its amino groups; oxidizing the macromolecule to activate at least one glycosyl group therein; and reacting the polyalkylene glycol coupled to the diamino compound with the oxidized glycosyl group in the macromolecule. The result is a glycolated glycosylated macromolecule, wherein a glycol is bonded to the macromolecule through its glycosylations. |
