Peptide PEGylation

It has long been a dream in medicine and pharmacy to use peptides and proteins as drugs. The driving force for this interest is the ability of these compounds to eliminate toxic or overproduced compounds in the body and to mimic endogenous hormones, cytokines and antibodies. However, there is a serious challenge which is to deliver the molecules to the desired bodily target. Many approaches to enhancing protein delivery have been examined, including protein entrapment in insoluble matrices and liposomes and immobilization onto polymer resins for use with extracorporeal shunts through which blood could flow. By far the most successful approach has been to mask the protein surface by covalent coupling of soluble poly (ethylene glycol) (PEG) or, as it has been known, “PEGylation”.

PEGylation of peptides has proven to be useful for several applications:  
> PEGylation at cysteine residue
> Arginine modification
> Carboxyl group modification
> Hydroxyl group conjugation
> Active site protection from PEGylation
> PEG as flexible, hydrophilic moiety in bifunctional reagents
> Enzyme PEGylation for solubilization in organic solvents
> Reversible grafting of PEG to proteins or fatty acid

PEGylation of peptides often have the following advantages:  
> Increased solubility of hydrophobic peptides
> Masked antigenicity for minimum immune response in the host
> Prolonged half-life through reduced renal clearance

In addition, for PEG peptides, the PEG is usually attached to the peptide using standard amide bond formation but other linkage chemistry is possible as well (e.g. thiol-maleimide, oxime ligation, click chemistry). Thus, PEGylating peptide may overcome many of the challenges for peptide drug candidates.

Below is a list of our available modifications (include but not limited to the following):

1. PEG Carrier

1. PEG Spacer

1. Mini-PEG1

1. Mini-PEG2

1. Mini-PEG3

Creative Peptides specialized in the custom synthesis of PEGylating peptide, providing a confidential and efficient service at competitive prices. Every step of peptide synthesis is subject to Creative Peptides’ stringent quality control. Typical delivery specifications include:

1. HPLC chromatogram
2. Mass spec analysis
3. Synthesis report
4. Certificate of Analyses

References:
[1] Harris, J. M., Martin, N. E., & Modi, M. (2001). Pegylation. Clinical pharmacokinetics, 40(7), 539-551.
[2] Veronese, F. M. (2001). Peptide and protein PEGylation: a review of problems and solutions. Biomaterials, 22(5), 405-417.
[3] Veronese, F. M., & Pasut, G. (2005). PEGylation, successful approach to drug delivery. Drug discovery today, 10(21), 1451-1458.