Forschungsverbund Berlin E.v.

Ludwig-Maximilians-Universitat München

Freie Universitaet Berlin

Ludwig-Mavimilians-Universität München

Freie Universitat Berlin

Christian Hackenberger

Heinrich Leonhardt

Dominik Schumacher

Jonas Helma-Smets

Jonas Helma

Andreas Stengl

Maria Glanz

Marc André Kasper

Tom Sauer

Stephen Byrne

Giuseppe Del Signore

Tina Stoscheck

Remigiusz Serwa

Ina Wilkening

Robert Vallee

Marc-André Kasper

Marcus Gerlach

Alice Leonie Baumann

Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene-or alkyne-phosohonothiolates and -phosphonates comprises the step of: reacting a compound of formula (I) with a thiol-containing molecule of formula (II) wherein represents an amino acid, a peptide, a protein, an antibody, a nucleotide, an oligonucleotide, a saccharide, a polysaccharide, a polymer, an optionally substituted C-C-alkyl, an optionally substituted phenyl, or an optionally substituted aromatic 5- or 6-membered heterocyclic system; resulting in a compound of formula (III).

Chemoselective thiol-conjugation with alkene or alkyne-phosphonothiolates and -phosphonates

Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene- or alkyne-phosphonamidates comprises the steps of

Chemoselective thiol-conjugation with alkene or alkyne-phosphonamidates

The present invention provides means and methods for equipping a polypeptide of interest at its C-terminus with a versatile adaptor amino acid that allows the functionalization of the polypeptide of interest.

Means and methods for site-specific functionalization of polypeptides

The present invention provides means and methods for functionalizing a polypeptide of interest at its C-terminus with an amino acid derivative.

Unusual substrates of tubulin tyrosine ligase

Disclosed are novel conjugates and processes for the preparation thereof. A process tor the preparation of alkene- or alkyne-phosphonamidates comprises the steps of (I) reacting a compound of formula (III), with an azide of formula (IV), to prepare a compound of formula (V), reacting a compound of formula (V) with a thiol-containing molecule of formula (VI), resulting in a compound of formula (VII). 

A modified compound that has at least one further functional group, in particular a bio- or macromolecule, comprising at least one x-fold (x&#x2267;1) chemoselectively incorporated phosphoramidate group of general formula (I), NPO(OR)(OR), and/or at least one x-fold (x&#x2267;1) chemoselectively incorporated phosphonamide group of general formula (Ia), NPO(R)(OR). Rand Ris selected from the group containing glycerol, polyglycerol, PEG polymers of the general empirical formula CHOwith n&#x2267;1, C-alkyl chains with n&#x2267;1; functionalized C-alkyl chains with n&#x2267;1, aryls, heteroaryl, silyl, lipids, fluorophores, saccharides, peptides, crown ethers, or a linker, which links the aforementioned groups. Rand Rcan be identical to or different from one another.

Compound modified by a phosphoramidate and/or phosphonamide group and use thereof

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Berlin, Germany

Christian Hackenberger