New application of multi-arm polyethylene glycol modifier and its application in modification of asparaginase

A technology of asparaginase and polyethylene glycol succinimidyl acetate, which is applied in the application field of modifying asparaginase, can solve the problem of not involving the depolymerization of multi-subunit protein subunits, the presence of immunogens It can achieve the effect of low immunogenicity, maintaining biological activity and prolonging half-life.
CN104046600BActive Publication Date: 2019-04-05ZONHON BIOPHARMA INST
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZONHON BIOPHARMA INST
Publication Date
2019-04-05

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Abstract

The invention discloses a new application of a multi-arm polyethylene glycol modifier and its application in modifying asparaginase. The multi-arm PEG modifier provided by the present invention can be used to strengthen the inter-subunit interaction force of multi-subunit proteins, keep multi-subunit proteins in the form of aggregation, thereby increasing the stability of multi-subunit proteins, enhancing or maintaining multi-subunit proteins biological activity, while reducing the chance of exposure of antigenic sites after depolymerization of each subunit, reducing immunogenicity. In addition, compared with the commercially available PEGylated asparaginase product "pegaspargase", the PEG-modified asparaginase prepared in the present invention has low immunogenicity, high activity and high stability, and PEG does not It has the advantages of falling off and the like, and is more suitable for the preparation of antitumor drugs.
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Description

Technical field

[0001] The invention relates to a new use of a multi-arm polyethylene glycol modifier and its application in modifying asparaginase. Background technique

[0002] Polyethylene glycol (PEG) is a linear, uncharged polymer that can curl freely in solution. It has non-toxic, weak antigenicity and good biocompatibility. Using it to covalently modify proteins can increase the in vivo circulating half-life of the protein and reduce its antigenicity, increase the solubility of the protein and change the biological distribution of the protein in the human body. Since Abuchowski, Davis (J.Biol.Chem.1977,252:3578-3581.) et al. first reported the modification of proteins with PEG in 1977, PEG modification technology has been widely used in the fields of biomedicine and biotechnology. PEG has It is widely used in the modification of protein and peptide drugs. At present, protein PEGylation technology has become one of the most effective methods to reduce the immunogenicity o...

Claims

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