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Protein Modifications

Protein Modifications. -- to increase stability. Goal of protein modification. Improved bioavailability, including longer circulation time and slower clearance Optimized pharmacokinetics resulting in sustained duration

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Protein Modifications

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  1. Protein Modifications -- to increase stability

  2. Goal of protein modification • Improved bioavailability, including longer circulation time and slower clearance • Optimized pharmacokinetics resulting in sustained duration • Improved safety profile with lower toxicity, immunogenicity, and antigenicity • Increased efficacy • Decreased dosing frequency • Improved drug solubility and stability • Reduced proteolysis • Controlled drug release

  3. In an aqueous medium, the long, chain-like PEG molecule is heavily hydrated and in rapid motion. This rapid motion causes the PEG to sweep out a large volume and prevents the approach and interference of other molecules. As a result, when attached to a drug, PEG polymer chains can protect the drug molecules from immune response and other clearance mechanisms, sustaining drug bioavailability

  4. http://www.nektar.com/wt/page/advanced_pegylation http://www.peg-drug.com/index.html

  5. Comb-Shaped Copolymers

  6. Chemistry for peptide and protein PEGylation* M.J. Roberts , M.D. Bentley, J.M. HarrisAdvanced Drug Delivery Reviews 54 (2002) 459–476 PEG-proteins: Reaction engineering and separation issues Conan J. Feea,., James M. Van Alstineb Chemical Engineering Science 61 (2006) 924 – 939

  7. Neoglycosylation Alkoxyamine-mediated neoglycosylation

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