The site-directed modification of e.g. biomolecules is often time consuming and laborious. This invention provides a high yielding and highly specific method to link nearly any molecule to nearly any other molecule. The Click reaction used is the well known Diels-Alder reaction with inverse electron demand. In this fast reaction an appropriate, easily functionalized dien (e.g. Tetrazin) is reacted with an appropriate functionalized dienophil (e.g. Olefin) to yield the conjugate. The release of nitrogen makes the reaction irreversible. No side reactions occur. Further the Intellectual Property covers specific information regarding the ligation of a diagnostic marker AND a therapeutic agent AND a biomolecule. Convincing synthetic data are available for the ligation of peptide with peptide, peptide with marker molecule, peptide with therapeutic agent, peptide with oligo nucleotide, dendritic structure and specific surface modification by means of this technology.
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DKFZ (German Cancer Research Center, Deutsches Krebsforschungszentrum)
Phone: +49-6221-42 2955
Dr. Ruth Herzog
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