The present invention provides for a practical, universal and efficient method to ligate two large macromolecules (e.g., proteins) using the alkyne-azide 1,3-dipolar cycloaddition reaction to produce a conjugated macromolecule, such as a multivalent scFv. The present invention also provides for conjugate macromolecules comprising a plurality of macromolecule components cross-linked through at least one linking group comprising at least one 1,2,3-triazole moiety, wherein at least 50 percent of the macromolecule components in the conjugate macromolecule has only one site available for cross-linking.
本发明提供了一种实用、通用和高效的方法,利用炔基-偶氮1,3-双极环加成反应连接两种大分子(例如蛋白质),以产生共轭大分子,例如多价scFv。本发明还提供了一种共轭大分子,包括通过至少一个含有至少一个
1,2,3-三唑基团的连接基交联的多种分子组分,其中在共轭大分子中至少50%的分子组分仅具有一个可用于交联的位点。