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In-SiteTM PEGylation |
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In-SiteTM is a novel site-selective PEGylation platform, using a proprietary efficient and cost-effective PEGylation chemistry, which is suitable to a large variety of proteins.
Common limits for therapeutic application of peptides and proteins are their chemical instability, their short residence time in blood and their tendency to promote an immunological response. Most of these problems may be solved by linking one or more PEG molecules to these peptides and proteins (PEGylation). This is achieved due to the combination of increased molecular weight and coverage of epitopes or blockage of sequences prone to enzymatic degradation. In addition, PEGylation enhances protein solubility in aqueous solutions.
The chemistry used for PEGylation of native proteins has been thoroughly investigated and is mainly focused on modification of reactive amino acids (e.g. lysine, histidine, N-terminal amine and cysteine). However, only few new chemical and enzymatic approaches for PEGylation of native proteins have been developed in the last decade. Due to the difficulty in the discovery of new PEGylation chemistries more and more recent approaches utilize engineered proteins for obtaining innovative PEGylation.
InSight's scientists have developed a new proprietary PEGylation platform, based on a unique strategy for PEGylation of native proteins. A novel PEG derivative has been developed which allows PEGylation of proteins by conjugation to an amino acid that has never been previously conjugated to PEG. A selective PEGylation process has been developed by exploiting the difference in pKa between the different amino acids.
This novel, selective and efficient PEGylation technology, termed In-SiteTM PEGylation is applicable to a large variety of important therapeutic proteins and is especially suitable for the development of novel, second generation, long-lasting versions of off-patent therapeutic proteins.
In-SiteTM PEGylation platform is patent pending worldwide.
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