N-terminal derivatisation of proteins with polysaccharides
AssigneeLipoxen Technologies Limited
InventorsSanjay Jain, Peter Laing, Gregory Gregoriadis
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Abstract
The present invention relates to methods for producing N-terminal derivatives of proteins in which a polysaccharide, preferably having at least terminal sialic units, and preferably consisting essentially only of sialic acid units, is reacted at the N-terminus of a protein or peptide under controlled conditions to produce an N-terminal derivative. The controlled conditions include use of acidic pH for the derivatization step and a higher pH for purification. The derivatives are useful for improving pharmacokinetics and pharmacodynamics of proteins and peptides.
Claims6
A method for producing a purified N-terminal derivative of a DNase protein, comprising reacting (i) a Polysialic acid (PSA) with DNase at the amine group of the N-terminus of the DNase in aqueous acidic solution to produce the N-terminal derivative;
- and (ii) purifying the N-terminal derivative in an aqueous solution of higher pH than in step (i) to obtain a population of derivatives comprising between 2 and 200 sialic acid units and wherein at least 85% of the population is derivatised with polysialic acid at the N-Terminal amine only.
Dependencies are inferred from the claim text.