[EN] A METHOD FOR MODIFICATION OF PEPTIDES IMMOBILIZED ON A SOLID SUPPORT BY TRACELESS REDUCTIVELY CLEAVABLE LINKER MOLECULES [FR] PROCÉDÉ DE MODIFICATION DE PEPTIDES IMMOBILISÉS SUR UN SUPPORT SOLIDE PAR DES MOLÉCULES DE LIAISON POUVANT ÊTRE CLIVÉES PAR RÉDUCTION SANS TRACE
[EN] A METHOD FOR MODIFICATION OF PEPTIDES IMMOBILIZED ON A SOLID SUPPORT BY TRACELESS REDUCTIVELY CLEAVABLE LINKER MOLECULES<br/>[FR] PROCÉDÉ DE MODIFICATION DE PEPTIDES IMMOBILISÉS SUR UN SUPPORT SOLIDE PAR DES MOLÉCULES DE LIAISON POUVANT ÊTRE CLIVÉES PAR RÉDUCTION SANS TRACE
申请人:BELYNTIC GMBH
公开号:WO2021023892A1
公开(公告)日:2021-02-11
The present invention relates to a method for modifying and purifying peptides comprising an immobilizing step, a modification step and a releasing step. In the immobilizing step, a crude linker-tagged peptide L-P is coupled to a solid support yielding an immobilized linker-tagged peptide S-L-P. Subsequently, the immobilized linker-tagged peptide S-L-P is modified with one or more organic molecules yielding an immobilized linker-tagged peptide S-L-mP. Finally, the modified peptide is released via a reduced intermediate RI. The linker molecule is a compound of formula 1, X-Tb-Va-U-Y-Z (1), which can be coupled to a purification resin via the moiety X and to a peptide via the moiety Y under the release of the leaving group Z. T is an optional spacer moiety and V is an optional electron withdrawing moiety. U is an aryl or 5- or 6-membered heteroaryl moiety bound to at least one electron withdrawing moiety V, W or E. The linker is stable under acidic conditions and releases the peptide upon addition of a reducing agent.