| 摘要 |
The present invention describes a linkage for use in the conjugation of compounds (e.g. peptides) to carrier vehicles (e.g. macromolecules, polymers, dendrimers, proteins etc.), producing constructs of biological and immunological relevance. The ability to link an Epitope (such as a peptide) to a carrier (such as a protein) in a controlled and specific manner is of a paramount importance in the development of a potent, pharmaceutically relevant, immunogenic hapten-carrier construct, such as a vaccine. The invention provides a reversible linkage technology for controlled conjugation of compounds such as peptides or peptidic Epitopes to carriers such as proteins. It utilises an aryl aldehyde moiety to introduce an aldehyde functionality on to a carrier molecule (e.g. on to the surface of a protein carrier molecule). It uses a 2-hydroxy-4-alkoxy linker based on an aryl aldehyde to provide protection in the conjugation of a peptide to a carrier, by virtue of imine formation. |
