PEGylation with dPEG® Products
PEGylation refers to the covalent addition of polyethylene glycol (PEG) to a compound or surface. PEGylated compounds include proteins, peptides, dyes or other labels, and small molecule drugs. Peptide synthesis frequently uses PEGylation to enhance a peptide’s water solubility. Moreover, peptide PEGylation prolongs the in vivo circulation of peptide conjugates by both increasing the peptide’s hydrodynamic volume and protecting the peptide from proteolysis. Additionally, PEGylation reduces or eliminates the conjugated peptide’s antigenicity.
However, traditional PEGs are dispersed polymers (Đ > 1.00). A traditional PEG consists of multiple chain lengths with different molecular weights. The stated molecular weight for conventional PEGs indicates an average of the distribution of chain lengths and molecular weights.
Quanta BioDesign’s single molecular weight PEG products (known as “discrete PEG” and sold under the dPEG® trademark) provide all of the benefits of traditional, dispersed PEG without the analytical headache that comes from having an intractable mixture of conjugates, each with different PEG chain lengths.
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Using Fmoc-amido-dPEG®24-amido-dPEG®24-acid
Fmoc-amido-dPEG®24-amido-dPEG®24-acid permits our customers to insert an extended (152 atoms, 197.9 – 198.9 Å) dPEG® spacer consisting of two conjugated amino-dPEG®24-acid units into a peptide chain using well-known, standard chemistry. Given its size, this product may work better in solution-phase rather than in solid-phase processes1.
The dPEG® can be inserted at either end of the peptide chain or in the middle of two peptides to provide a flexible spacer between distinct peptide chains. Also, the dPEG® spacer can be used to add distance in a synthetic construct where steric hindrance is a problem. The Fmoc protecting group removes easily with a solution of piperidine in N, N-dimethylformamide (DMF).
Numerous applications could benefit from using Fmoc-amido-dPEG®24-amido-dPEG®24-acid. Applications that might benefit from use of this product include:
- Antibody-Drug Conjugates (ADCs);
- PET/SPECT imaging applications;
- Making highly hydrophobic peptides and small molecules water-soluble;
- Shielding peptides and proteins from the immune system and proteolysis;
- PEG-functionalization of lipids for use in liposomes and micelles; and
- Supramolecular construction and functionalization of nanoparticles.
A Range of Different Fmoc-protected Amino-dPEG® Acids Is Available
To help our customers discover the optimum linker length necessary for a particular product or application, Fmoc-amido-dPEG®24-amido-dPEG®24-acid, product number 11301, is part of a line of Fmoc-protected amino-dPEG® acid products. Furthermore, we offer several Fmoc-protected amino acids activated with either N-hydroxysuccinimide (NHS) or 2,3,5,6-tetrafluorophenol (TFP). We invite you to consider our entire range of Fmoc-protected amino-dPEG®x-acid and active ester products whenever you need a single molecular weight PEG for your product.
Bulk Quantities Are Available
If you need bulk product in a larger package size than our standard sizes, please contact us for a quote. Our commercial capabilities permit us to manufacture this product at any scale that you need.
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Application Reference:
- Mäde, V.; Els-Heindl, S.; Beck-Sickinger, A. G. Automated Solid-Phase Peptide Synthesis to Obtain Therapeutic Peptides. Beilstein Journal of Organic Chemistry 2014, 10(1), 1197–1212. https://doi.org/10.3762/bjoc.10.118.
In the paper cited above, the authors were reporting on dispersed, not discrete, PEG; however, the caution may still apply to discrete PEG products.