| abstract |
Method for conjugating peptides, said method including the steps of i) reacting in one or more steps a Gln residue with peptide represented by the formula with a nitrogen with nucleophile (first compound) represented by the formula H2N-DRX which includes one or more groups functional or functional latent groups, which are not accessible in any of the amino acid residues constituting said peptide, in the presence of transglutaminase capable of catalyzing the incorporation of said first compound into said peptide to form a transaminated peptide of the formula and ii) optionally activating the latent group functional X; and iii) reacting in one or more steps said transaminated peptide with a second compound of the formula Y-EZ that includes one or more functional groups, where said functional group (s) does not react with accessible functional groups in the amino acid residues constituting said peptide, and where said functional group (s) in said second compound is capable of reacting with said functional group (s) in said first compound so that a covalent bond between said transaminated peptide and said second compound is formed as a result of a conjugated peptide of the formula where D represents a bond or oxygen; R represents a linker or link; X represents a radical comprising a functional group or a functional latent group not accessible in the amino acid residues constituting the P-C (O) -NH2 peptide; Y represents a radical comprising one or more functional groups these groups reacting with functional groups present in X, and these functional groups not reacting with functional groups accessible in the P-C (O) -NH2 peptide; E represents a linker or link; A represents a fraction of oxime, hydrazone, phenylhydrazone, semicarbazone, triazole or isooxazolidine, the fraction formed by the reaction between the functional groups comprised in X and Y; and Z is the fraction that must be conjugated to the peptide. |