Watts, Andrew Graham,Kantner, Terrence,Mackenzie, Amanda
申请号：
ES15151649
公开号：
ES2674099T3
申请日:
2009.12.21
申请国别(地区):
ES
年份:
2018
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 bound to a poly (ethylene glycol) molecule, so that the vinyl substituent of the functionalizing reagent reacts with the thiol group of the polypeptide, thereby covalently linking the poly ( ethylene glycol) to the polypeptide, wherein the functionalizing reagent is represented by one of the general formulas: ** Formula ** wherein: at least R1, and optionally R2, are covalently linked to a poly (alkylene glycol) molecule； and also where: R1, and optionally R2, are independently selected from: - (CH2) nZ- (CH2) oC (O) R, where Z is O, S or NH, n is 0 to 10, or is 0 to 10 and where R is a hydrogen or a poly (alkylene glycol) molecule； or - (CH2) n-Z- (CH2) o-R, where Z is O, S or NH, n is 0 to 10, or is 0 to 10 and where R is a hydrogen or a poly (alkylene glycol) molecule； or - (CO) -Z- (CH2) or -R, where Z is O, S or NH, or is 0 to 10 and where R is a hydrogen or a poly (alkylene glycol) molecule； or - (CH2) nZC (O) - (CH2) oR, where Z is O, S or NH, n is 0 to 10, or is 0 to 10 and where R is a hydrogen or a poly (alkylene glycol molecule) ； or -Y- (CH2) nZC (O) - (CH2) oR, where Y is an aryl group, O, S or NH, Z is O or NH, n is 0 to 10, or is 0 to 10 and where R it is a hydrogen or a poly (alkylene glycol) molecule； or -Y-R, where Y is O or S, R is a hydrogen, a molecule of poly (alkylene glycol), aryl or C1-10 alkyl； or ** Formula ** wherein: at least R1, and optionally R2, are covalently linked to a poly (alkylene glycol) molecule； 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 where R is a hy
