Peptides, PEGylated

In this chapter, some methods for peptide-polymer conjugate synthesis are described and a number of examples are reviewed to illustrate the use of self-assembling peptide sequences to drive nanoscale organization. Conjugation of polymers with proteins or peptides for reasons other than self-assembly, for example, therapeutic protein or peptide PEGylation to prolong in vivo circulation half-lives, are not covered. 

Protein and peptide pegylation (conjugation to polymers of long-chain macrogol - or polyethylene glycol) improves the biopharmaceutical properties of active substances. The improvement encompasses increased stability, resistance to proteolytic inactivation and extension of the half-lives. By this the dehvery and efficacy of proteins is improved [31]. 

Lecolley, F., Tao, L., Mantovani, G., etal. (2005) A new approach to bioconjugates for proteins and peptides (pegylation) utilising living radical polymerisation, Chimica Oggi - Chemistry Today, 23, 45-51. 

Roberts MJ, Bentley MD, Harris JM (2002) Chemistry for peptide and protein PEGylation. Adv Drug Deliv Rev 54 459 -76... 

Liu et al. (2007) discovered that polyethylene glycol (PEG)ylated SWNTs are stable in vivo and demonstrate long blood circulation times and low uptake by the reticuloendothelial system. This group linked PEGylated SWNTs to an arginine-glycine-aspartic acid peptide, which was able to effectively target tumors in mice. 

Ashok, B., Rubinstein, I., Tsueshita, T. and Onyuksel, H. (2004), Effect of molecular mass and PEG chain length on the vasoreactivity of VIP and PACAPj 36 in PEGylated phospholipid micelles, Peptides, 25, 1253-1258. 

These polymers have been designed to achieve serum stability and sustained circulation with the PEGylated peptide, specific targeting to hepatocytes with... 

Rao GA, Tsai R, Roura D et al (2008) Evaluation of the transfection property of a peptide ligand for the fibroblast growth factor receptor as part of PEGylated polyethylenimine polyplex. J Drug Target 16 79-89... 

Conjugation of the peptide with polyethylene glycol (PEGylation) is quite powerful (23), increasing the peptides water solubility and reducing their immunogenecity (24). 

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