WATTS, Andrew Graham,KANTNER, Terrence,MACKENZIE, Amanda Barbara
申请号：
ES09795797
公开号：
ES2556328T3
申请日:
2009.12.21
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
A method for modifying a polypeptide that has at least one reactive thiol group, a method comprising contacting the polypeptide with a functionalizing reagent which comprises a nitrogen-containing heterocyclic aromatic ring having a vinyl substituent capable of reacting with the at least one thiol group of the polypeptide, where the functionalizing reagent is covalently linked to a glycan group, so that the vinyl substituent of the functionalizing reagent reacts with the thiol group of the polypeptide, thereby covalently linking the glycan group to the polypeptide, characterized in that the reagent Functionalizer is represented by one of the general formulas: ** Formula ** where: at least R1, and optionally R2, are covalently linked to a glycan group； and also where: R1, and optionally R2, are independently selected from: - (CH2) nZ- (CH2) oC (O) -R, where Z is S or NH, n is 0 to 10, or is 0 to 10 and wherein R is a hydrogen, a polyalkylene glycol molecule or a glycan group； or - (CH2) n-Z- (CH2) o-R, in which Z is S or NH, n is 0 to 10, or is 0 to 10 and in which R is a hydrogen, a polyalkylene glycol molecule or a glycan group； or - (CO) -Z- (CH2) or -R, in which Z is S or NH, or is 0 to 10 and in which R is a hydrogen, a polyalkylene glycol molecule or a glycan group； or - (CH2) nZC (O) - (CH2) oR, in which Z is S or NH, n is 0 to 10, or is 0 to 10 and in which R is a hydrogen, a polyalkylene glycol molecule or a glycan group； or -Y- (CH2) nZC (O) - (CH2) oR, in which Y is an aryl group, S or NH, Z is NH, n is 0 to 10, or is 0 to 10 and in which R it is a hydrogen, a polyalkylene glycol molecule or a glycan group； or -Y-R, where Y is S, R is a hydrogen, a glycan, a polyalkylene glycol, aryl or C1-10 alkyl molecule； with the proviso that when R2 is not linked to a polyalkylene glycol molecule or a glycan group, it can additionally be selected from hydrogen or from an electron acceptor group, such as halogen (F, Cl, or Br), -NO2, -CO2H , -CO2R4, COR4, -CHO, -CN, -C
