Tools for PEGylation

By: Matthias Junkers, Aldrich ChemFiles 2008, 8.7, 26.

Aldrich ChemFiles 2008, 8.7, 26.

Polyethylene glycol (PEG) reagents offer numerous favorable characteristics, including high water solubility, high mobility in solution, lack of toxicity and immunogenicity, and ready clearance from the body. Thus, the chemical modification of biologically active compounds, such as peptides, antibody fragments, enzymes, or small molecules with polyethylene glycol chains (referred to as PEGylation), is an effective method to tailor molecular properties to particular applications (Figure 1).

Figure 1

Drugs can especially benefit from PEGylation as has been proved by a continuously growing number of PEG conjugated drugs on the market. By increasing the molecular mass of proteins and peptides and shielding them from proteolytic enzymes, PEGylation improves pharmacokinetics.1 The judicious choice of PEG size and linkers enhance a potential drug’s solubility and its distribution within an organism.2

Numerous review articles concerning the application of PEG polymers in drug delivery are available.3 In some recent reports PEGylation is discussed as a tool to facilitate the drug delivery of nanocarrier systems and microparticles.4,5

In this issue of ChemFiles, Sigma-Aldrich® is proud to further expand its offer of tools for PEGylation with new bifunctional, small and medium-sized ethylene glycol building blocks. For a complete list of PEGylation products, please visit our online product catalog at and browse through the peptide synthesis category.

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  1. Harris, J.M.; Chess, R.B. Nature Rev. Drug. Disc. 2003, 2, 214.
  2. Fee, C. Biotechn. and Bioeng. 2007, 98, 725.
  3. (a) “Peptide and Protein PEGylation, a Review of Problems and Solutions”, Veronese, F.M. Biomaterials 2001, 5,405.(b) “Chemistry for Peptide and Protein PEGylation”, Roberts, M.J.; Bentley, M.D.;Jarris, J.M. Adv. Drug Del. Rev. 2002, 4, 459.(c) “PEGylation, Successful Approach to Drug Delivery”, Veronese, F.M.; Pasut, G. Drug Disc. Today 2005, 10, 1451.(d) “Advances in PEGylation of Important Biotech Molecules: Delivery Aspects”, Ryan,S.M.; Mantovani, G.; Wang, X.; Haddleton, D.M.; Brayden, D.J. Exp. Op. on Drug Del. 2008, 5, 371.
  4. Howard, M.D.; Jay, M.; Dziubla, T.D.; Lu, X. Biomed. Nanotechn. 2008,4, 133.
  5. Wattendorf, U.; Merkle, H.P. J. Pharm. Sci. 2008, 97, 4655.

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