Pepscan Systems B.v.

Syngenta Corporation

Robbert Hans Meloen

Wouter Cornelis Puijk

Peter Timmerman

Joris Beld

Jelle Wouter Slootstra

Evert Van Dijk

Willem F Broekaert

Sarah Bronwen Rees

Franky Fant

Aart Van Amerongen

Frans Borremans

Genoveva Wivina De Samblanx

Wilhelmus Martinus Maria Schaaper

Lolke Sijtsma

Pieter Van Dijken

Wilhelmus Martinus Josef Van Gelder

The disclosure relates to the field of candidate drug testing and drug development. A method is provided for providing a compound composed of at least one molecule attached via at least two linkages to a molecular scaffold, the method comprising providing a scaffold comprising at least a first and a second reactive group; providing at least one molecule capable of reacting with the at least first and second reactive group; contacting the scaffold with at least one molecule to form at least two linkages between the scaffold and the at least one molecule in a coupling reaction, wherein the formation of a linkage accelerates the formation of a consecutive linkage, preferably wherein the coupling reaction is performed in solution, more preferably in an aqueous solution. Furthermore, a method is provided for selecting a candidate drug compound comprising providing a library of compounds hereof and determining the binding of a target molecule to the compounds.

Method for selecting a candidate drug compound

The invention relates to the field of candidate drug testing and drug development. A method is provided for providing a compound composed of at least one molecule attached via at least two linkages to a molecular scaffold, the method comprising providing a scaffold comprising at least a first and a second reactive group; providing at least one molecule capable of reacting with the at least first and second reactive group; contacting the scaffold with at least one molecule to form at least two linkages between the scaffold and the at least one molecule in a coupling reaction, wherein the formation of a linkage accelerates the formation of a consecutive linkage, preferably wherein the coupling reaction is performed in solution, more preferably in an aqueous solution. Furthermore, a method is provided for selecting a candidate drug compound comprising providing a library of compounds according to the invention and determining the binding of a target molecule to the compounds.

The disclosure relates to the field of candidate drug testing and drug development. Described are methods for providing a compound composed of at least one molecule attached via at least two linkages to a molecular scaffold, the method comprising providing a scaffold comprising at least a first and a second reactive group; providing at least one molecule able to react with the at least first and second reactive group; and contacting the scaffold with at least one molecule to form at least two linkages between the scaffold and the molecule in a coupling reaction, wherein the formation of a linkage accelerates the formation of a consecutive linkage. The coupling reaction may be performed in solution, such as an aqueous solution. Furthermore, described is a method for selecting a candidate drug compound comprising providing a library of the compounds and determining the binding of a target molecule to the compounds.

The invention relates to the field of molecular recognition or detection of discontinuous or conformational binding sites or epitopes corresponding to a binding molecule, in particular, in relation to protein-protein, protein-nucleic acid, nucleic acid-nucleic acid or biomolecule-ligand interactions. The invention provides a synthetic molecular library allowing testing for, identification, characterization or detection of a discontinuous binding site capable of interacting with a binding molecule, the library having been provided with a plurality of test entities, each test entity comprising at least one first segment spotted next to a second segment, each segment having the capacity of being a potential single part of a discontinuous binding site.

Identification of protein binding sites

The invention provides means and methods for producing compounds suitable for testing for the presence and/or identification of an immunogenic compound and/or a binding compound of interest. Immunogenic compounds and compositions are also herewith provided, as well as peptidomimetics of members of the cystine-knot family.

Binding compounds, immunogenic compounds and peptidomimetics

Antifungal peptides which comprise at least six amino acid residues identical to a run of amino acid residues found between position 21 and position 51 of the Rs-AFP2 antifungal protein sequence or of substantially homologous protein sequences. The peptides are useful for combating fungal diseases in agricultural, pharmaceutical or preservative applications.

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Lelystad, Netherlands

Robbert Hans Meloen