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Versatile Method to Link Diagnostics and/or Therapeutics to Biomolecules

Ref-Nr: TA-P-687


Kurzfassung

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.


Hintergrund

The “Click reaction” used is the well known DielsAlder reaction with inverse electron demand (DARinv). In this fast reaction an appropriate, easily functionalized dien (e.g. Tetrazin 1) is reacted with an appropriate functionalized dienophil (e.g. Olefin 2) to yield the product 3. The release of nitrogen 4 makes the reaction irreversible. No side reactions occur (Scheme). Transient protection of functional groups of the molecules to be linked with this method is obsolete. Further no activation of the reacting compounds is necessary and thus there are no restrictions to the solvents to be used for the reaction, i.e. organic solvents, alcohols and even water are appropriate solvents. The invention discloses several applications for this reaction:

  • ligation of diagnostics or therapeutics to peptides, oligo nucleotides or saccharides
  • Modification of surfaces and solid phases
  • Preparation of dendritic structures and quantum dots

Further the Intellectual Property covers specific information regarding the combination of above mentioned applications e.g. the ligation of a diagnostic marker AND a therapeutic agent AND a biomolecule. 


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Lösung

  • Simple synthetic pathways
  • Versatile starting materials
  • High yielding, easy to monitor reactions without side reactions
  • Re-formulation of “old fashioned” drugs & diagnostics
  • Applicable to surface modifications 

Anwendungsbereiche

  1. Improvement of production processes (higher yield) in particular for biomolecules.
  2. Chip production: DNA, Protein or Carbon hydrate (i.e. Saccharide) Chips

DKFZ is currently seeking a commercial partner to develop this technology under an exclusive licence and/or collaboration agreement. Exclusive licensing for specific applications/indications is possible.


Deutsches Krebsforschungszentrum DKFZ

Dr. Christian Kliem
+49-6221-42-2948
c.kliem@dkfz.de
www.dkfz.de
Adresse
Im Neuenheimer Feld 280
69120 Heidelberg



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Kontakt | Geschäftsstelle

TechnologieAllianz e. V.
Christiane Bach-Kaienburg
(Geschäftsstellenleiterin)

c/o PROvendis GmbH
Schloßstr. 11-15
D-45468 Mülheim an der Ruhr