N-terminal derivatisation of proteins with polysaccharides
First Claim
1. A composition comprising a population of polysialic acid derivatives of a DNase protein, wherein the derivatives comprise 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.
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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.
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Citations
19 Claims
- 1. A composition comprising a population of polysialic acid derivatives of a DNase protein, wherein the derivatives comprise 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.
- 8. A polysialic derivative according to formula (I)
Specification