PEGylation of Biopharmaceuticals: A Review of Chemistry and Nonclinical Safety Information of Approved Drugs

Poly(ethylene glycol) in Drug Delivery: Pros and Cons as Well as Potential Alternatives

Knop, K., Hoogenboom, R., Fischer, D., & Schubert, U. S. (2010) · Angewandte Chemie International Edition · doi:10.1002/anie.200902672 · Cited by 3,533 · see citing works

PEGylation, successful approach to drug delivery

Veronese, F. M., & Pasut, G. (2005) · Drug Discovery Today · doi:10.1016/s1359-6446(05)03575-0 · Cited by 2,344 · see citing works

Chemistry for peptide and protein PEGylation

Roberts, M. J., Bentley, M. D., & Harris, J. M. (2002) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(02)00022-4 · Cited by 1,607 · see citing works

Poly(ethylene glycol) chemistry : biotechnical and biomedical applications

Harris, J. M. (1992) · Plenum Press eBooks · Cited by 1,426 · see citing works

Alteration of immunological properties of bovine serum albumin by covalent attachment of polyethylene glycol.

Abuchowski, A., Es, T. V., Palczuk, N. C., & Davis, F. F. (1977) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(17)40291-2 · Cited by 1,358 · see citing works

Effect of covalent attachment of polyethylene glycol on immunogenicity and circulating life of bovine liver catalase.

Abuchowski, A., McCoy, J. R., Palczuk, N. C., Es, T. V., & Davis, F. F. (1977) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(17)40292-4 · Cited by 1,276 · see citing works

Effective drug delivery by PEGylated drug conjugates

Greenwald, R. B., Choe, Y. H., McGuire, J., & Conover, C. D. (2003) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(02)00180-1 · Cited by 870 · see citing works

2′-Fluoropyrimidine RNA-based Aptamers to the 165-Amino Acid Form of Vascular Endothelial Growth Factor (VEGF165)

Ruckman, J., Green, L. S., Beeson, J., Waugh, S. M., Gillette, W. L., Henninger, D. D., Claesson, L., & Janjić, N. (1998) · Journal of Biological Chemistry · doi:10.1074/jbc.273.32.20556 · Cited by 744 · see citing works

State of the art in PEGylation: The great versatility achieved after forty years of research

Pasut, G., & Veronese, F. M. (2011) · Journal of Controlled Release · doi:10.1016/j.jconrel.2011.10.037 · Cited by 725 · see citing works

PEGylation of therapeutic proteins

Jevševar, S., Kunstelj, M., & Porekar, V. G. (2010) · Biotechnology Journal · doi:10.1002/biot.200900218 · Cited by 681 · see citing works

The structure of 2Zn pig insulin crystals at 1.5 Å resolution

Baker, E. N., Blundell, T. L., Cutfield, J. F., Dodson, E. J., Dodson, G. G., Hodgkin, D. M. C., Hubbard, R. E., Isaacs, N. W., Reynolds, C. D., Sakabe, K., et al. (1988) · Philosophical transactions of the Royal Society of London. Series B, Biological sciences · doi:10.1098/rstb.1988.0058 · Cited by 666 · see citing works

Rational Design of a Potent, Long-Lasting Form of Interferon: A 40 kDa Branched Polyethylene Glycol-Conjugated Interferon α-2a for the Treatment of Hepatitis C

Bailon, P., Palleroni, A. V., Schaffer, C. A., Spence, C. L., Fung, W.-J., Porter, J. E., Ehrlich, G. K., Pan, W. Q., Xu, Z., Modi, M., et al. (2001) · Bioconjugate Chemistry · doi:10.1021/bc000082g · Cited by 611 · see citing works

PEGylated antibodies and antibody fragments for improved therapy: a review

Chapman, A. P. (2002) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(02)00026-1 · Cited by 558 · see citing works

Chemistry of polyethylene glycol conjugates with biologically active molecules

Zalipsky, S. (1995) · Advanced Drug Delivery Reviews · doi:10.1016/0169-409x(95)00023-z · Cited by 553 · see citing works

Chemistry of Protein Conjugation and Cross Linking

Wong, S. S. (1991) · Medical Entomology and Zoology · Cited by 490 · see citing works

Mechanism of action of certolizumab pegol (CDP870): In vitro comparison with other anti-tumor necrosis factor α agents

Nesbitt, A. M., Fossati, G., Bergin, M., Stephens, P. E., Stephens, S., Foulkes, R., Brown, D. T., Robinson, M. K., & Bourne, T. (2007) · Inflammatory Bowel Diseases · doi:10.1002/ibd.20225 · Cited by 476 · see citing works

The Pharmacology of PEGylation: Balancing PD with PK to Generate Novel Therapeutics

Fishburn, C. S. (2008) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.21278 · Cited by 475 · see citing works

Functionalized Poly(ethylene glycols) for Preparation of Biologically Relevant Conjugates

Zalipsky, S. (1995) · Bioconjugate Chemistry · doi:10.1021/bc00032a002 · Cited by 470 · see citing works

PEG conjugates in clinical development or use as anticancer agents: An overview

Pasut, G., & Veronese, F. M. (2009) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2009.02.010 · Cited by 458 · see citing works

Treatment of Adenosine Deaminase Deficiency with Polyethylene Glycol–Modified Adenosine Deaminase

Hershfield, M. S., Buckley, R. H., Greenberg, M., Melton, A. L., Schiff, R. I., Hatem, C. L., Kurtzberg, J., Markert, M. L., Kobayashi, R. H., Kobayashi, A., et al. (1987) · New England Journal of Medicine · doi:10.1056/nejm198703053161005 · Cited by 443 · see citing works

Structural and biological characterization of pegylated recombinant interferon alpha-2b and its therapeutic implications

Wang, Y.-S., Youngster, S. K., Grace, M. J., Bausch, J. N., Bordens, R. W., & Wyss, D. F. (2002) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(02)00027-3 · Cited by 420 · see citing works

Probing protein structure by amino acid‐specific covalent labeling and mass spectrometry

Mendoza, V. L., & Vachet, R. W. (2008) · Mass Spectrometry Reviews · doi:10.1002/mas.20203 · Cited by 365 · see citing works

Therapeutic antibody fragments with prolonged in vivo half-lives

Chapman, A. P., Antoniw, P., Spitali, M., West, S. M., Stephens, S., & King, D. (1999) · Nature Biotechnology · doi:10.1038/11717 · Cited by 350 · see citing works

PEGylated Proteins: Evaluation of Their Safety in the Absence of Definitive Metabolism Studies

Webster, R., Didier, E., Harris, P., Siegel, N., Stadler, J., Tilbury, L., & Smith, D. (2007) · Drug Metabolism and Disposition · doi:10.1124/dmd.106.012419 · Cited by 337 · see citing works

Pegaspargase: a review of clinical studies

Graham, M. (2003) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(03)00110-8 · Cited by 322 · see citing works

Mono-N-terminal poly(ethylene glycol)–protein conjugates

Kinstler, O. B., Molineux, G., Treuheit, M. J., Ladd, D. L., & Gegg, C. V. (2002) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(02)00023-6 · Cited by 306 · see citing works

PEG-uricase in the management of treatment-resistant gout and hyperuricemia

Sherman, M. R., Saifer, M. G. P., & Pérez-Ruiz, F. (2007) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2007.06.011 · Cited by 290 · see citing works

The Design and Development of Pegfilgrastim (PEG-rmetHuG-CSF, Neulasta®)

Molineux, G. (2004) · Current Pharmaceutical Design · doi:10.2174/1381612043452613 · Cited by 285 · see citing works

Poly(ethylene glycol)-Prodrug Conjugates: Concept, Design, and Applications

Banerjee, S. S., Aher, N. D., Patil, R. B., & Khandare, J. J. (2012) · Journal of Drug Delivery · doi:10.1155/2012/103973 · Cited by 285 · see citing works

Induced and pre-existing anti-polyethylene glycol antibody in a trial of every 3-week dosing of pegloticase for refractory gout, including in organ transplant recipients

Hershfield, M. S., Ganson, N. J., Kelly, S. J., Scarlett, E., Jaggers, D. A., & Sundy, J. S. (2014) · Arthritis Research & Therapy · doi:10.1186/ar4500 · Cited by 265 · see citing works

Periodate Oxidation of Carbohydrates

Bobbitt, J. M. (1956) · Advances in carbohydrate chemistry · doi:10.1016/s0096-5332(08)60115-0 · Cited by 263 · see citing works

A Branched Monomethoxypoly(ethylene glycol) for Protein Modification

Monfardini, C., Schiavon, O., Caliceti, P., Morpurgo, M., Harris, J. M., & Veronese, F. M. (1995) · Bioconjugate Chemistry · doi:10.1021/bc00031a006 · Cited by 256 · see citing works

Emerging PEGylated drugs

Kang, J. S., DeLuca, P. P., & Lee, K. C. (2009) · Expert Opinion on Emerging Drugs · doi:10.1517/14728210902907847 · Cited by 252 · see citing works

Cancer therapy with chemically modified enzymes. I. Antitumor properties of polyethylene glycol-asparaginase conjugates.

Abuchowski, A., Kazo, G. M., Cr, V., et al. (1984) · PubMed · Cited by 250 · see citing works

Long-acting Growth Hormones Produced by Conjugation with Polyethylene Glycol

CLARK, R. G., Olson, K., Fuh, G., et al. (1996) · Journal of Biological Chemistry · doi:10.1074/jbc.271.36.21969 · Cited by 248 · see citing works

A new form of Filgrastim with sustained duration in vivo and enhanced ability to mobilize PBPC in both mice and humans

Molineux, G., Kinstler, O. B., Briddell, B., et al. (1999) · Experimental Hematology · doi:10.1016/s0301-472x(99)00112-5 · Cited by 245 · see citing works

Polyethylene glycol-conjugated pharmaceutical proteins

Bailon, P., & Berthold, W. (1998) · Pharmaceutical Science & Technology Today · doi:10.1016/s1461-5347(98)00086-8 · Cited by 243 · see citing works

PEGylated Protein Drugs: Basic Science and Clinical Applications

(2009) · doi:10.1007/978-3-7643-8679-5 · Cited by 241 · see citing works

Use of peginterferon alfa-2a (40 KD) (Pegasys®) for the treatment of hepatitis C

Reddy, K. R., Modi, M., & Pedder, S. C. J. (2002) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(02)00028-5 · Cited by 241 · see citing works

Effects of PEG conjugation on insulin properties

Hinds, K. D., & Kim, S. W. (2002) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(02)00025-x · Cited by 240 · see citing works

Characterization and Stability of N-terminally PEGylated rhG-CSF

Kinstler, O. B., Brems, D. N., Lauren, S. L., Paige, A. G., Hamburger, J. B., & Treuheit, M. J. (1996) · Pharmaceutical Research · doi:10.1023/a:1016042220817 · Cited by 238 · see citing works

Poly(ethylene glycol): Chemistry and Biological Applications

Brannon‐Peppas, L. (2000) · Journal of Controlled Release · doi:10.1016/s0168-3659(99)00212-6 · Cited by 238 · see citing works

Introduction to Chemistry and Biological Applications of Poly(ethylene glycol)

Zalipsky, S., & Harris, J. M. (1997) · ACS symposium series · doi:10.1021/bk-1997-0680.ch001 · Cited by 220 · see citing works

L-Asparaginase and PEG Asparaginase— Past, Present, and Future

Keating, M. J., Holmes, R., Lerner, S. A., & Ho, D. H. (1993) · Leukemia & lymphoma/Leukemia and lymphoma · doi:10.3109/10428199309149129 · Cited by 217 · see citing works

Pharmacokinetics and Safety of an Anti-Vascular Endothelial Growth Factor Aptamer (NX1838) Following Injection into the Vitreous Humor of Rhesus Monkeys

Drolet, D. W., Nelson, J., Tucker, C. E., Zack, P. M., Nixon, K., Bolin, R. J., Judkins, M. B., Farmer, J. A., Wolf, J. L., Gill, S. C., et al. (2000) · Pharmaceutical Research · doi:10.1023/a:1007657109012 · Cited by 206 · see citing works

New Detachable Poly(ethylene glycol) Conjugates: Cysteine-Cleavable Lipopolymers Regenerating Natural Phospholipid, Diacyl Phosphatidylethanolamine

Zalipsky, S., Qazen, M. M., Walker, J. A., Mullah, N. N., Quinn, Y. P., & Huang, S. K. (1999) · Bioconjugate Chemistry · doi:10.1021/bc990031n · Cited by 198 · see citing works

Pegnology: a review of PEG-ylated systems.

Bhadra, D., Bhadra, S., Jain, P., & Jain, N. K. (2002) · PubMed · Cited by 183 · see citing works

Prediction of the Viscosity Radius and the Size Exclusion Chromatography Behavior of PEGylated Proteins

Fee, C. J., & Alstine, J. M. V. (2004) · Bioconjugate Chemistry · doi:10.1021/bc049843w · Cited by 176 · see citing works

Detection and plasma pharmacokinetics of an anti-vascular endothelial growth factor oligonucleotide-aptamer (NX1838) in rhesus monkeys

Tucker, C. E., Chen, L.-S., Judkins, M. B., Farmer, J. A., Gill, S. C., & Drolet, D. W. (1999) · Journal of Chromatography B Biomedical Sciences and Applications · doi:10.1016/s0378-4347(99)00285-6 · Cited by 175 · see citing works

Structural and Biologic Characterization of Pegylated Recombinant IFN- α 2b

Grace, M. J., Youngster, S. K., Gitlin, G., et al. (2001) · Journal of Interferon & Cytokine Research · doi:10.1089/107999001317205240 · Cited by 174 · see citing works

GlycoPEGylation of recombinant therapeutic proteins produced in Escherichia coli

DeFrees, S. A., Wang, Z., Xing, R., Scott, A. E., Wang, J., Zopf, D., Gouty, D. L., Sjoberg, E. R., Panneerselvam, K., der Linden, E. C. M. B.-V., et al. (2006) · Glycobiology · doi:10.1093/glycob/cwl004 · Cited by 174 · see citing works

Pharmacokinetics, metabolism and distribution of PEGs and PEGylated proteins: quo vadis?

Baumann, A., Tuerck, D., Prabhu, S., Dickmann, L. J., & Sims, J. (2014) · Drug Discovery Today · doi:10.1016/j.drudis.2014.06.002 · Cited by 163 · see citing works

PEGylated Biopharmaceuticals

Ivens, I. A., Achanzar, W. E., Baumann, A., Braendli-Baiocco, A., Cavagnaro, J. A., Dempster, M., Depelchin, B. O., Rovira, A. R. I., Dill-Morton, L., Lane, J. H., et al. (2015) · Toxicologic Pathology · doi:10.1177/0192623315591171 · Cited by 162 · see citing works

Anti-cancer PEG-enzymes: 30 years old, but still a current approach

Pasut, G., Sergi, M., & Veronese, F. M. (2007) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2007.04.018 · Cited by 152 · see citing works

Increased activity and stability of poly(ethylene glycol)-modified trypsin

Gaertner, H., & PUIGSERVER, A. J. (1992) · Enzyme and Microbial Technology · doi:10.1016/0141-0229(92)90174-m · Cited by 148 · see citing works

N-Terminally PEGylated Human Interferon-β-1a with Improved Pharmacokinetic Properties and in Vivo Efficacy in a Melanoma Angiogenesis Model

Baker, D. P., Lin, E. Y.-S., Lin, K., Pellegrini, M., Petter, R. C., Chen, L. L., Arduini, R. M., Brickelmaier, M., Wen, D., Hess, D. M., et al. (2005) · Bioconjugate Chemistry · doi:10.1021/bc050237q · Cited by 144 · see citing works

Prolonged half-life and preserved enzymatic properties of factor IX selectively PEGylated on native N-glycans in the activation peptide

Østergaard, H., Bjelke, J. R., Hansen, L., Petersen, L. C., Pedersen, A. A., Elm, T., Møller, F., Hermit, M. B., Holm, P. K., Krogh, T. N., et al. (2011) · Blood · doi:10.1182/blood-2011-02-336172 · Cited by 144 · see citing works

Releasable PEGylation of proteins with customized linkers

Filpula, D. R., & Zhao, H. (2007) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2007.02.001 · Cited by 137 · see citing works

Identification of the Major Positional Isomer of Pegylated Interferon Alpha-2b

Wang, Y.-S., Youngster, S. K., Bausch, J. N., et al. (2000) · Biochemistry · doi:10.1021/bi000617t · Cited by 130 · see citing works

Protein, peptide and non-peptide drug PEGylation for therapeutic application

Pasut, G., Guiotto, A., & Veronese, F. (2004) · Expert Opinion on Therapeutic Patents · doi:10.1517/13543776.14.6.859 · Cited by 126 · see citing works

Evaluation of a new reagent for covalent attachment of polyethylene glycol to proteins.“

Zalipsky, S., Seltzer, R. D., & Menon-Rudolph, S. (1992) · Biotechnology and Applied Biochemistry · doi:10.1111/j.1470-8744.1992.tb00198.x · Cited by 120 · see citing works

A novel B-domain O-glycoPEGylated FVIII (N8-GP) demonstrates full efficacy and prolonged effect in hemophilic mice models

Stennicke, H. R., Kjalke, M., Karpf, D. M., Balling, K. W., Johansen, P. B., Elm, T., Øvlisen, K., Møller, F., Holmberg, H. L., Gudme, C. N., et al. (2013) · Blood · doi:10.1182/blood-2012-01-407494 · Cited by 116 · see citing works

Formulation of Neulasta® (pegfilgrastim)

Piedmonte, D. M., & Treuheit, M. J. (2007) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2007.04.017 · Cited by 115 · see citing works

Positional Isomers of Monopegylated Interferon α-2a: Isolation, Characterization, and Biological Activity

Monkarsh, S. P., Ma, Y., Aglione, A., Bailon, P., Ciolek, D., Debarbieri, B., Graves, M. C., Hollfelder, K., Michel, H., Palleroni, A. V., et al. (1997) · Analytical Biochemistry · doi:10.1006/abio.1997.2128 · Cited by 114 · see citing works

Structural and Biophysical Characterization of the 40 kDa PEG−Interferon-α2aand Its Individual Positional Isomers

Dhalluin, C., Ross, A., Leuthold, L. A., et al. (2005) · Bioconjugate Chemistry · doi:10.1021/bc049781+ · Cited by 112 · see citing works

Stabilization of α‐chymotrypsin upon PEGylation correlates with reduced structural dynamics

Rodríguez‐Martínez, J. A., Solá, R. J., Castillo, B., et al. (2008) · Biotechnology and Bioengineering · doi:10.1002/bit.22014 · Cited by 112 · see citing works

Drug Delivery Systems Employing 1,4- or 1,6-Elimination: Poly(ethylene glycol) Prodrugs of Amine-Containing Compounds

Greenwald, R. B., Pendri, A., Conover, C. D., et al. (1999) · Journal of Medicinal Chemistry · doi:10.1021/jm990166e · Cited by 110 · see citing works

PEG ylated therapeutic proteins for haemophilia treatment: a review for haemophilia caregivers

Ivens, I. A., Baumann, A., McDonald, T. A., Humphries, T. J., Michaels, L. A., & Mathew, P. (2012) · Haemophilia · doi:10.1111/j.1365-2516.2012.02931.x · Cited by 107 · see citing works

Aminooxy-, Hydrazide-, and Thiosemicarbazide-Functionalized Saccharides: Versatile Reagents for Glycoconjugate Synthesis

Rodriguez, E. C., Marcaurelle, L. A., & Bertozzi, C. R. (1998) · The Journal of Organic Chemistry · doi:10.1021/jo981351n · Cited by 105 · see citing works

Effect of PEG molecular weight and linking chemistry on the biological activity and thermal stability of PEGylated trypsin

Treetharnmathurot, B., Ovartlarnporn, C., Wungsintaweekul, J., et al. (2008) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2008.01.016 · Cited by 102 · see citing works

BAX 855, a PEGylated rFVIII product with prolonged half-life. Development, functional and structural characterisation.

Turecek, P. L., Bossard, M. J., Graninger, M., et al. (2012) · PubMed · Cited by 95 · see citing works

Site of Pegylation and Polyethylene Glycol Molecule Size Attenuate Interferon-α Antiviral and Antiproliferative Activities through the JAK/STAT Signaling Pathway

Grace, M. J., Lee, S., Bradshaw, S. L., et al. (2005) · Journal of Biological Chemistry · doi:10.1074/jbc.m412134200 · Cited by 89 · see citing works

Site-Specific Pegylation of G-CSF by Reversible Denaturation

Veronese, F. M., Mero, A., Caboi, F., Sergi, M., Marongiu, C., & Pasut, G. (2007) · Bioconjugate Chemistry · doi:10.1021/bc070123+ · Cited by 88 · see citing works

Use of an indirect pharmacodynamic stimulation model of MX protein induction to compare in vivo activity of interferon alfa-2a and a polyethylene glycol-modified derivative in healthy subjects

Nieforth, K. A., Nadeau, R., Patel, I. H., & Mould, D. R. (1996) · Clinical Pharmacology & Therapeutics · doi:10.1016/s0009-9236(96)90003-x · Cited by 83 · see citing works

Polyethylene Glycol Modification: Relevance of Improved Methodology to Tumour Targeting

Francis, G. E., Delgado, C., Fisher, D., Malik, F., & Agrawal, A. K. (1996) · Journal of drug targeting · doi:10.3109/10611869608996824 · Cited by 82 · see citing works

Controlled Release of Proteins from Their Poly(Ethylene Glycol) Conjugates: Drug Delivery Systems Employing 1,6-Elimination

Greenwald, R. B., Yang, K., Zhao, H., et al. (2003) · Bioconjugate Chemistry · doi:10.1021/bc025652m · Cited by 79 · see citing works

Effects of PEG size on structure, function and stability of PEGylated BSA

Plesner, B., Fee, C. J., Westh, P., et al. (2011) · European Journal of Pharmaceutics and Biopharmaceutics · doi:10.1016/j.ejpb.2011.05.003 · Cited by 77 · see citing works

Prolonging the Action of Protein and Peptide Drugs by a Novel Approach of Reversible Polyethylene Glycol Modification

Tsubery, H., Mironchik, M., Fridkin, M., et al. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m405155200 · Cited by 76 · see citing works

Pharmacology of Escherichia coli-L-asparaginase polyethylene glycol adduct.

Park, Y. K., Abuchowski, A., Davis, S., et al. (1981) · PubMed · Cited by 72 · see citing works

Biochemical and biopharmaceutical properties of PEGylated uricase

Freitas, D. D. S., Spencer, P. J., Vassão, R. C., et al. (2009) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2009.11.034 · Cited by 70 · see citing works

Effect of PEGylation on Protein Hydrodynamics

Gokarn, Y. R., McLean, M. A., & Laue, T. M. (2012) · Molecular Pharmaceutics · doi:10.1021/mp200470c · Cited by 69 · see citing works

[35] Labeling glycoconjugates with hydrazide reagents

Wilchek, M., & Bayer, E. A. (1987) · Methods in enzymology on CD-ROM/Methods in enzymology · doi:10.1016/0076-6879(87)38037-1 · Cited by 68 · see citing works

Reversible PEGylation: A Novel Technology To Release Native Interferon α2 over a Prolonged Time Period

Peleg‐Shulman, T., Tsubery, H., Mironchik, M., et al. (2004) · Journal of Medicinal Chemistry · doi:10.1021/jm0497693 · Cited by 67 · see citing works

Anti-inflammatory and pharmacokinetic properties of superoxide dismutase derivatized with polyethylene glycol via active esters

Veronese, F. M., Boccu, E., Schiavon, O., et al. (1983) · Journal of Pharmacy and Pharmacology · doi:10.1111/j.2042-7158.1983.tb02888.x · Cited by 67 · see citing works

Use of Functionalized Poly(Ethylene Glycol)s for Modification of Polypeptides

Zalipsky, S., & Lee, C. (1992) · Springer eBooks · doi:10.1007/978-1-4899-0703-5_21 · Cited by 62 · see citing works

Safety of PEGylated recombinant human full‐length coagulation factor VIII (BAX 855) in the overall context of PEG and PEG conjugates

Stidl, R., Fuchs, S. P., Bossard, M. J., et al. (2015) · Haemophilia · doi:10.1111/hae.12762 · Cited by 61 · see citing works

Certolizumab pegol for the treatment of rheumatoid arthritis

Horton, S., Walsh, C. A., & Emery, P. E. (2011) · Expert Opinion on Biological Therapy · doi:10.1517/14712598.2012.645533 · Cited by 58 · see citing works

Generation and biochemical characterization of glycoPEGylated factor VIIa derivatives

Østergaard, H., Bayer, R. J., Kalo, M. S., et al. (2008) · Thrombosis and Haemostasis · doi:10.1160/th08-04-0268 · Cited by 58 · see citing works

Structure-Function Perturbation and Dissociation of Tetrameric Urate Oxidase by High Hydrostatic Pressure

Girard, É., Marchal, S., Pérez, J., et al. (2010) · Biophysical Journal · doi:10.1016/j.bpj.2010.01.058 · Cited by 57 · see citing works

Structural, Kinetic, and Thermodynamic Analysis of the Binding of the 40 kDa PEG−Interferon-α2a and Its Individual Positional Isomers to the Extracellular Domain of the Receptor IFNAR2

Dhalluin, C., Ross, A., Huber, W., et al. (2005) · Bioconjugate Chemistry · doi:10.1021/bc049780h · Cited by 53 · see citing works

Amino Acid Sequence of L-Asparaginase from Escherichia coli

Maita, T., MOROKUMA, K., & Matsuda, G. (1974) · The Journal of Biochemistry · doi:10.1093/oxfordjournals.jbchem.a130690 · Cited by 52 · see citing works

A simple modified carbodiimide method for conjugation of small-molecular-weight compounds to immunoglobulin G with minimal protein crosslinking

Davis, M.-T. B., & Preston, J. F. (1981) · Analytical Biochemistry · doi:10.1016/0003-2697(81)90380-8 · Cited by 48 · see citing works

Carboxyalkylated Histidine Is a pH-Dependent Product of Pegylation with SC-PEG

Wylie, D. C., Voloch, M., Lee, S., et al. (2001) · Pharmaceutical Research · doi:10.1023/a:1013006515587 · Cited by 47 · see citing works

NMR Structure of Two Novel Polyethylene Glycol Conjugates of the Human Growth Hormone-Releasing Factor, hGRF(1−29)−NH2

Digilio, G., Barbero, L. M., Bracco, C., et al. (2003) · Journal of the American Chemical Society · doi:10.1021/ja021264j · Cited by 44 · see citing works

Characterisation and physical stability of PEGylated glucagon

Stigsnaes, P., Frøkjær, S., Bjerregaard, S., et al. (2006) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2006.09.002 · Cited by 44 · see citing works

Treatment of L5178Y tumor-bearing BDF1 mice with a nonimmunogenic L-glutaminase-L-asparaginase.

Abuchowski, A., Es, T. V., Palczuk, N. C., McCoy, J. R., & Davis, F. F. (1979) · PubMed · Cited by 43 · see citing works

PEGylation of Human Serum Albumin: Reaction of PEG-Phenyl-Isothiocyanate with Protein

Meng, F., Manjula, B. N., Smith, P. K., et al. (2008) · Bioconjugate Chemistry · doi:10.1021/bc7003878 · Cited by 43 · see citing works

Pegvisomant in the treatment of acromegaly

Parkinson, C. (2003) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(03)00111-x · Cited by 42 · see citing works

Conjugates of Peptides and Proteins to Polyethylene Glycols

Morpurgo, M., & Veronese, F. M. (2004) · Humana Press eBooks · doi:10.1385/1-59259-813-7:045 · Cited by 42 · see citing works

Isolation of Positional Isomers of Mono-poly(ethylene glycol)ylated Interferon/α-2a and the Determination of Their Biochemical and Biological Characteristics

Monkarsh, S. P., Spence, C. L., Porter, J. E., et al. (1997) · ACS symposium series · doi:10.1021/bk-1997-0680.ch015 · Cited by 39 · see citing works

Pegylating IFNs at His-34 Improves the in Vitro Antiviral Activity Through the JAK/STAT Pathway

Grace, M. J., & Cutler, D. L. (2004) · Antiviral chemistry & chemotherapy · doi:10.1177/095632020401500601 · Cited by 32 · see citing works

PEGylation enhancement of pH stability of uricase via inhibitive tetramer dissociation

Tian, H., Yuan, G., Gao, X., & Yao, W. (2012) · Journal of Pharmacy and Pharmacology · doi:10.1111/j.2042-7158.2012.01575.x · Cited by 32 · see citing works

Management of Viral Hepatitis: Clinical and Public Health Perspectives – A Consensus Statement

Sherman, M., & Casl Hapatitis Consensus Group (1997) · Canadian Journal of Gastroenterology · doi:10.1155/1997/454278 · Cited by 32 · see citing works

Effects of monomethoxypoly(ethylene glycol) modification of ribonuclease on antibody recognition, substrate accessibility and conformational stability

Caliceti, P., Schiavon, O., Veronese, F. M., et al. (1990) · Journal of Molecular Recognition · doi:10.1002/jmr.300030206 · Cited by 31 · see citing works

Alkyl succinimidyl carbonates undergo Lossen rearrangement in basic buffers

Zalipsky, S. (1998) · Chemical Communications · doi:10.1039/a706713e · Cited by 31 · see citing works

Spectroscopic characterization of polyethyleneglycol modified superoxide dismutase: 1H NMR studies on its Cu2Co2 derivative

Banci, L., Bertini, I., Scolaro, L. M., Caliceti, P., Schiavon, O., & Veronese, F. M. (1990) · Journal of Inorganic Biochemistry · doi:10.1016/0162-0134(90)80023-q · Cited by 29 · see citing works

Instability of succinyl ester linkages in O2′-monosuccinyl cyclic AMP-protein conjugates at neutral pH

Carter, M., & Meyerhoff, M. E. (1985) · Journal of Immunological Methods · doi:10.1016/0022-1759(85)90210-8 · Cited by 29 · see citing works

Biophysical characterisation of GlycoPEGylated recombinant human factor VIIa

Plesner, B., Westh, P., & Nielsen, A. D. (2011) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2010.12.034 · Cited by 27 · see citing works

Modification and immobilization of proteins with polyethylene glycol tresylates and polysaccharide tresylates: Evidence suggesting a revision of the coupling mechanism and the structure of the polymer-polymer linkage

Gais, H., & Ruppert, S. (1995) · Tetrahedron Letters · doi:10.1016/0040-4039(95)00633-n · Cited by 27 · see citing works

Anchimeric assistance effect on regioselective hydrolysis of branched PEGs: a mechanistic investigation

Guiotto, A., Canevari, M., Pozzobon, M., et al. (2004) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2004.07.041 · Cited by 27 · see citing works

l-Asparaginase from Erwinia carotovora

Shifrin, S., Solis, B. G., & CHAIKEN, I. M. (1973) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(19)43952-5 · Cited by 22 · see citing works

The Effect of Protein PEGylation on Physical Stability in Liquid Formulation

Holm, L. S., McUmber, A. C., Rasmussen, J. E., Obiols‐Rabasa, M., Thulstrup, P. W., Kasimova, M. R., Randolph, T. W., & van de Weert, M. (2014) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.24094 · Cited by 20 · see citing works

A Comparative Study of Enzymatic, Structural, and Pharmacokinetic Properties of Superoxide Dismutase Isolated from Two Sources and Modified by Monomethoxypolyethylene Glycol Using Different Methods of Couplinga

Veronese, F. M., Sartore, L., Schiavon, O., et al. (1990) · Annals of the New York Academy of Sciences · doi:10.1111/j.1749-6632.1990.tb18202.x · Cited by 17 · see citing works

Preferential Interactions and the Effect of Protein PEGylation

Holm, L. S., Thulstrup, P. W., Kasimova, M. R., et al. (2015) · PLoS ONE · doi:10.1371/journal.pone.0133584 · Cited by 14 · see citing works

Preclinical Evaluation of Hematide™, a Novel Erythropoietic Receptor Agonist for the Treatment of Anemia Caused by Kidney Disease.

Woodburn, K. W., Fan, Q., Leuther, K. K., et al. (2004) · Blood · doi:10.1182/blood.v104.11.2904.2904 · Cited by 13 · see citing works

PEGylation of human growth hormone: strategies and properties

Finn, R. F. (2009) · Birkhäuser Basel eBooks · doi:10.1007/978-3-7643-8679-5_11 · Cited by 12 · see citing works

Reactive PEGs for protein conjugation

Bonora, G. M., & Drioli, S. (2009) · Birkhäuser Basel eBooks · doi:10.1007/978-3-7643-8679-5_3 · Cited by 11 · see citing works

Enzymatic techniques for PEGylation of biopharmaceuticals

Sergi, M., Caboi, F., Maullu, C., et al. (2009) · Birkhäuser Basel eBooks · doi:10.1007/978-3-7643-8679-5_5 · Cited by 10 · see citing works

The Somatotrophic Axis in Brain Function

Long, D. M. (2006) · Neurosurgery Quarterly · doi:10.1097/00013414-200606000-00014 · Cited by 10 · see citing works

Certolizumab pegol: a PEGylated anti-tumour necrosis factor alpha biological agent

Nesbitt, A. M., Stephens, S., & Chartash, E. (2009) · Birkhäuser Basel eBooks · doi:10.1007/978-3-7643-8679-5_14 · Cited by 9 · see citing works

Reduction of immunoreactivity of bovine serum albumin conjugated with polyethylene glycol(PEG) in relation to its esterase activity.

Matsushima, A., Sasaki, H., Kodera, Y., et al. (1992) · PubMed · Cited by 8 · see citing works

Development of PEGylated mammalian urate oxidase as a therapy for patients with refractory gout

Hershfield, M. S., Sundy, J. S., Ganson, N. J., & Kelly, S. J. (2009) · Birkhäuser Basel eBooks · doi:10.1007/978-3-7643-8679-5_13 · Cited by 7 · see citing works

Poly(ethylene) Glycol Conjugates of Biopharmaceuticals in Drug Delivery

Bentley, M. D., Bossard, M. J., Burton, K. W., et al. (2005) · doi:10.1002/9783527620982.ch57 · Cited by 7 · see citing works

Protein carboxyl amidation increases the potential extent of protein polyethylene glycol conjugation

Li, S., Yang, Z., Sun, X., et al. (2004) · Analytical Biochemistry · doi:10.1016/j.ab.2004.03.034 · Cited by 7 · see citing works

Characterization of Interferon a2B Pegylated via Carboxyalkylation: A Case Study

Wylie, D. C., Voloch, M., Lee, S., et al. (2005) · Humana Press eBooks · doi:10.1385/1-59259-922-2:337 · Cited by 5 · see citing works

Discrete PEG Reagents

Hermanson, G. T. (2007) · Elsevier eBooks · doi:10.1016/b978-0-12-370501-3.00018-7 · Cited by 3 · see citing works

Growth Hormone Antagonists: A Pharmacological Tool in Present and Future Therapies

Kopchick, J. J., OJU, L., Sustarsic, E. G., et al. (2006) · Elsevier eBooks · doi:10.1016/b978-012088484-1/50027-6 · Cited by 1 · see citing works

The evolution of commercial drug delivery technologies

Vargason, A. M., Anselmo, A. C., & Mitragotri, S. (2021) · Nature Biomedical Engineering · doi:10.1038/s41551-021-00698-w · Cited by 1,361 · see citing works

Smart nanoparticles for cancer therapy

Sun, L., Liu, H., Ye, Y., Lei, Y., Islam, R., Tan, S., Tong, R., Miao, Y.-B., & Cai, L. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01642-x · Cited by 1,073 · see citing works

Anti-PEG antibodies: Properties, formation, testing and role in adverse immune reactions to PEGylated nano-biopharmaceuticals

Kozma, G. T., Shimizu, T., Ishida, T., & Szebeni, J. (2020) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2020.07.024 · Cited by 696 · see citing works

The Importance of Poly(ethylene glycol) Alternatives for Overcoming PEG Immunogenicity in Drug Delivery and Bioconjugation

Hoang Thi, T. T., Pilkington, E. H., Nguyen, D. H., Lee, J. S., Park, K. D., & Truong, N. P. (2020) · Polymers · doi:10.3390/polym12020298 · Cited by 668 · see citing works

Stimuli‐responsive nanotherapeutics for precision drug delivery and cancer therapy

Qiao, Y., Wan, J., Zhou, L., Ma, W., Yang, Y., Luo, W., Yu, Z., & Wang, H. (2019) · WIREs Nanomedicine and Nanobiotechnology · doi:10.1002/wnan.1527 · Cited by 332 · see citing works

Understanding the Role and Impact of Poly (Ethylene Glycol) (PEG) on Nanoparticle Formulation: Implications for COVID-19 Vaccines

Padín-González, E., Lancaster, P., Bottini, M., Gasco, P., Tran, L., Fadeel, B., Wilkins, T., & Monopoli, M. P. (2022) · Frontiers in Bioengineering and Biotechnology · doi:10.3389/fbioe.2022.882363 · Cited by 166 · see citing works

Recent Advances in Incretin-Based Pharmacotherapies for the Treatment of Obesity and Diabetes

Tan, Q., Akindehin, S. E., Orsso, C. E., Waldner, R. C., DiMarchi, R. D., Müller, T. D., & Haqq, A. M. (2022) · Frontiers in Endocrinology · doi:10.3389/fendo.2022.838410 · Cited by 146 · see citing works

Characterization of a PEGylated protein therapeutic by ion exchange chromatography with on-line detection by native ESI MS and MS/MS

Muneeruddin, K., Bobst, C. E., Frenkel, R., Houde, D., Turyan, I., Sosic, Z., & Kaltashov, I. A. (2017) · The Analyst · doi:10.1039/c6an02041k · Cited by 38 · see citing works

ULTRASOUND PROMOTED ONE POT SYNTHESIS OF 1,5-BENZOTHIAZEPINES USING POLYETHYLENE GLYCOL (PEG-400)

Devkate, C. G., Kola, S., Gaikwad, D. D., et al. (2018) · International Research Journal of Pharmacy · doi:10.7897/2230-8407.0911280 · Cited by 10 · see citing works

Peptide and protein PEGylation

Veronese, F. M. (2001) · Biomaterials · doi:10.1016/s0142-9612(00)00193-9 · Cited by 1,068 · see citing works

Application of microchip CGE for the analysis of PEG‐modified recombinant human granulocyte‐colony stimulating factors

Park, E. J., Lee, K. S., Lee, K. C., et al. (2010) · Electrophoresis · doi:10.1002/elps.201000302 · Cited by 16 · see citing works

Author Index for Volume 376, Number 1

(2000) · Archives of Biochemistry and Biophysics · doi:10.1006/abbi.2000.1796

PEGylated Antibodies and DNA in Organic Media and Genetic PEGylation

Tada, S., Abe, H., & Ito, Y. (2013) · ACS symposium series · doi:10.1021/bk-2013-1144.ch016 · Cited by 1 · see citing works