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PEGylation
PEGylation (also often styled pegylation) is the process of both covalent and non-covalent attachment or amalgamation of polyethylene glycol (PEG) polymer chains to molecules and macrostructures, such as a drug, therapeutic protein or vesicle, which is then described as PEGylated (pegylated). PEGylation is routinely achieved by incubation of a reactive derivative of PEG with the target molecule. The covalent attachment of PEG to a drug or therapeutic protein can "mask" the agent from the host's immune system (reduced immunogenicity and antigenicity), and increase the hydrodynamic size (size in solution) of the agent which prolongs its circulatory time by reducing renal clearance. PEGylation can also provide water solubility to hydrophobic drugs and proteins.
==History==
Around 1970, Frank F. Davis, a professor of biochemistry at Rutgers University, became interested in developing a process to render usable bioactive proteins of potential medical value. After considerable study, he concluded that the attachment of an inert and hydrophilic polymer might extend blood life and control immunogenicity of the proteins. Polyethylene glycol was chosen as the polymer. A team of Davis, Theodorus Van Es and Nicholas C. Palczuk conducted animal studies and found that PEG attachment greatly extended blood life and controlled immunogenicity of the proteins. A patent application was filed in 1973 and patent issued in 1979.〔Davis, F. F., Van Es, T., and Palczuk, N. C. (1979) United States Patent . (Non-immunogenic polypeptides ). ''Originally filed in 1973''〕 The inventors and Abraham Abuchowski conducted extensive additional PEGylation studies on various enzymes.〔Abuchowski, A.; Van Es, T.; Palczuk, N.C.; Davis, F.F. (1977). '' J. Biol. Chem.'', 252, 3578-3581.〕〔Abuchowski, A.; McCoy, J. R.; Palczuk, N. C.; Van Es, T.; Davis, F.F. (1977). "Effect of Covalent Attachment of Polyethylene Glycol on Immunogenicity and Circulating Life of Bovine Liver Catalase". ''J. Biol. Chem.'' 252: 2582-3586.〕 In 1981 Davis and Abuchowski founded Enzon, Inc., which brought three PEGylated drugs to market. Abuchowski later founded and is CEO of Prolong Pharmaceuticals.
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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