Reagents and methods for functionalizing polypeptides with moieties (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalizing reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalizing reagent is covalently linked to a poly(alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly(alkylene glycol) molecule and/or the glycan group.
本文披露了一种功能化试剂和方法,用于将(烷基二醇)分子和糖基与
多肽功能化。该方法基于一种功能化试剂,该试剂包含一个含氮杂环芳香环,具有一个
乙烯基取代基,能够与
多肽中天然存在或已引入的一个或多个巯基反应,例如使用一个或多个半胱
氨酸残基的巯基。功能化试剂与多(烷基二醇)分子(例如聚
乙二醇(P
EG)分子)或糖基共价连接,因此,
多肽中
乙烯基和巯基之间的反应将
多肽共价连接到多(烷基二醇)分子和/或糖基上。