Next Article in Journal
Aminolevulinic Acid-Based Tumor Detection and Therapy: Molecular Mechanisms and Strategies for Enhancement
Next Article in Special Issue
TriFabs—Trivalent IgG-Shaped Bispecific Antibody Derivatives: Design, Generation, Characterization and Application for Targeted Payload Delivery
Previous Article in Journal
Interleukins 6 and 15 Levels Are Higher in Subcutaneous Adipose Tissue, but Obesity Is Associated with Their Increased Content in Visceral Fat Depots
Previous Article in Special Issue
High-Throughput Screening in Protein Engineering: Recent Advances and Future Perspectives
Open AccessReview

Site-Specific PEGylation of Therapeutic Proteins

1
Department of Chemistry, University of Minnesota, Minneapolis, MN 55455, USA
2
Department of Medicinal Chemistry, University of Minnesota, Minneapolis, MN 55455, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Qiang "Shawn" Chen
Int. J. Mol. Sci. 2015, 16(10), 25831-25864; https://doi.org/10.3390/ijms161025831
Received: 27 August 2015 / Revised: 19 October 2015 / Accepted: 20 October 2015 / Published: 28 October 2015
(This article belongs to the Special Issue Protein Engineering)
The use of proteins as therapeutics has a long history and is becoming ever more common in modern medicine. While the number of protein-based drugs is growing every year, significant problems still remain with their use. Among these problems are rapid degradation and excretion from patients, thus requiring frequent dosing, which in turn increases the chances for an immunological response as well as increasing the cost of therapy. One of the main strategies to alleviate these problems is to link a polyethylene glycol (PEG) group to the protein of interest. This process, called PEGylation, has grown dramatically in recent years resulting in several approved drugs. Installing a single PEG chain at a defined site in a protein is challenging. Recently, there is has been considerable research into various methods for the site-specific PEGylation of proteins. This review seeks to summarize that work and provide background and context for how site-specific PEGylation is performed. After introducing the topic of site-specific PEGylation, recent developments using chemical methods are described. That is followed by a more extensive discussion of bioorthogonal reactions and enzymatic labeling. View Full-Text
Keywords: chemical modification; enzymatic modification; PEGylation; protein PEGylation; site specific modification; therapeutic proteins chemical modification; enzymatic modification; PEGylation; protein PEGylation; site specific modification; therapeutic proteins
Show Figures

Figure 1

MDPI and ACS Style

Dozier, J.K.; Distefano, M.D. Site-Specific PEGylation of Therapeutic Proteins. Int. J. Mol. Sci. 2015, 16, 25831-25864.

Show more citation formats Show less citations formats

Article Access Map

1
Only visits after 24 November 2015 are recorded.
Back to TopTop