发明名称 |
AMINE PEGYLATION METHODS FOR THE PREPARATION OF SITE-SPECIFIC PROTEIN CONJUGATES |
摘要 |
Examples include a method of making a protein-PEG conjugate. The method may include providing an aqueous protein solution. The aqueous protein solution may include a protein, a pH buffer, and a chelating agent. The chelating agent may be chosen from the group consisting of an aminopolycarboxylic acid, a hydroxyaminocarboxylic acid, an N-substituted glycine, 2-(2-amino-2-oxocthyl) aminoethane sulfonic acid (BES), and deferoxamine (DEF). The method may also include introducing sodium cyanoborohydride and a methoxy polyethylene glycol aldehyde to the aqueous protein solution. The sodium cyanoborohydride in the methoxy polyethylene glycol aldehyde may have a molar ratio ranging from about 5:1 to about 1.5:1. The method may further include reacting the methoxy polyethylene glycol aldehyde with the protein to form the protein-PEG conjugate. The pH buffer may maintain a pH of the aqueous protein solution ranging from 4.0 to 4.4 during the reaction. |
申请公布号 |
US2016354478(A1) |
申请公布日期 |
2016.12.08 |
申请号 |
US201615158898 |
申请日期 |
2016.05.19 |
申请人 |
AntriaBio, Inc. |
发明人 |
Rosendahl Mary S.;Mantripragada Sankaram B. |
分类号 |
A61K47/48;A61K38/26;A61K9/50;A61K38/27;A61K38/28;A61K38/29 |
主分类号 |
A61K47/48 |
代理机构 |
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代理人 |
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主权项 |
1. A method of making a protein-PEG conjugate, the method comprising:
providing an aqueous protein solution comprising a protein, a pH buffer, and a chelating agent, wherein the chelating agent is chosen from the group consisting of an aminopolycarboxylic acid, a hydroxyaminocarboxylic acid, an N-substituted glycine, 2-(2-amino-2-oxocthyl) aminoethane sulfonic acid (BES), and deferoxamine (DEF); introducing boron-containing reducing agent and a methoxy polyethylene glycol aldehyde to the aqueous protein solution, wherein the boron-containing reducing agent and methoxy polyethylene glycol aldehyde have a molar ratio ranging from about 25:1 to about 1.5:1; and reacting the methoxy polyethylene glycol aldehyde with the protein to form the protein-PEG conjugate, wherein the pH buffer maintains a pH of the aqueous protein solution ranging from 4.0 to 6.0 during the reaction. |
地址 |
Louisville CO US |