Introduction to polyethylene glycol (PEG) modifier

Polyethylene glycol (PEG) has good biological and blood compatibility, hydrophilicity, and no immunogenicity, while PEG with a molecular weight greater than 1000 Da has been proven to be non-toxic in the food, cosmetic, and pharmaceutical industries for many years. Often used to modify biochemical drugs and biomedical materials such as proteins, peptides, and enzymes. The main biological functions of the modified proteins and peptides remain unchanged and many advantageous properties are obtained.


Chemical drugs or protein drugs, etc., generally have problems that they cannot overcome at the same time; for example, a short period of action, large anti-immunogenicity and side effects. PEGylation technology is a technique that activates polyethylene glycol to link to a drug molecule or drug surface. Polyethylene glycol can increase the water solubility of drugs, reduce toxic side effects, reduce immunogenicity, improve the stability of drugs in the body, and prolong the cycle half-life of drugs.


Polyethylene glycol modification, also known as PEGylation of molecules, is a modification method developed in the late 1970s. Coupling activated polyethylene glycol with protein molecules affects the spatial structure of the protein, ultimately leading to changes in various biochemical properties of the protein: increased chemical stability, increased resistance to protease hydrolysis, reduced immunogenicity and toxicity, or Disappeared, the body half-life is prolonged, plasma clearance is reduced, and the like. The size, conformation, and binding sites of the polyethylene glycol have a critical impact on the pharmacokinetics and pharmacodynamics of the drug. Therefore, the specific protein must be PEGylated one by one in order to achieve the desired therapeutic effect.


The hydroxyl group at the end of polyethylene glycol is a functional group in the chemical modification reaction, but its reactivity is low, and it can react with other groups only under relatively strong conditions, and such conditions are usually unable to withstand proteins. Therefore, the polyethylene glycol must first be activated to couple it to the protein at a high reaction rate under mild reaction conditions. Polyethylene glycol derivatives can be classified according to the mode of activation, the electrical properties of the end groups, and the history of development.

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