Chemistry: molecular biology and microbiology – Treatment of micro-organisms or enzymes with electrical or... – Modification of viruses
Patent
1995-04-21
1998-06-16
Hendricks, Keith D.
Chemistry: molecular biology and microbiology
Treatment of micro-organisms or enzymes with electrical or...
Modification of viruses
435188, 435212, 435219, C12N 1500, C12N 996, C12N 948, C12N 950
Patent
active
057668973
ABSTRACT:
Methods and compositions are provided for the production of PEGylated proteins having polyethylene glycol covalently bound to a cysteine residue present in either the naturally-occurring protein or introduced by site-specific mutation. Where the cysteine residue is introduced by mutation, the site for mutation is selected on the basis of the presence of an N-linked glycosylation site or the position of the residue which is normally solvent-accessible in the naturally-occurring protein. The modified proteins produced by the method of the invention are referred to as cysteine-PEGylated proteins. Proteins PEGylated according to the invention have increased half-lives following administration to a subject and decreased immunogenicity and antigenicity, while retaining substantially the same level of biological activity as that of the naturally-occurring, unmodified protein. Modification of proteins according to methods of the invention thus provide improved pharmaceutical compositions.
REFERENCES:
patent: 4179337 (1979-12-01), Davis et al.
patent: 4474752 (1984-10-01), Haslam et al.
patent: 4478822 (1984-10-01), Haslam et al.
patent: 4657760 (1987-04-01), Kung et al.
patent: 4690915 (1987-09-01), Rosenberg
patent: 4731439 (1988-03-01), Marquardt et al.
patent: 4766106 (1988-08-01), Katre et al.
patent: 4816439 (1989-03-01), Jorgensen
patent: 4863910 (1989-09-01), Takayanagi
patent: 4902502 (1990-02-01), Nitecki et al.
patent: 4965251 (1990-10-01), Stamatoyannopoulos
patent: 4978332 (1990-12-01), Luck et al.
patent: 5006509 (1991-04-01), Waago
patent: 5010175 (1991-04-01), Rutter et al.
patent: 5013718 (1991-05-01), Adamson et al.
patent: 5032574 (1991-07-01), Wilde et al.
patent: 5089261 (1992-02-01), Nitecki et al.
patent: 5089274 (1992-02-01), Marra et al.
patent: 5112608 (1992-05-01), Scott et al.
patent: 5122614 (1992-06-01), Zalipsky
patent: 5140008 (1992-08-01), Jorgensen
patent: 5166322 (1992-11-01), Shaw et al.
patent: 5182259 (1993-01-01), Kita
patent: 5187089 (1993-02-01), Scott et al.
patent: 5196196 (1993-03-01), Scott et al.
patent: 5198417 (1993-03-01), Donahue
patent: 5206344 (1993-04-01), Katre et al.
patent: 5223409 (1993-06-01), Ladner et al.
patent: 5225212 (1993-07-01), Martin et al.
patent: 5234903 (1993-08-01), Nho et al.
patent: 5234912 (1993-08-01), Marra et al.
patent: 5260066 (1993-11-01), Wood et al.
patent: 5264209 (1993-11-01), Mikayama et al.
patent: 5283317 (1994-02-01), Saifer et al.
patent: 5290773 (1994-03-01), Takayanagi
patent: 5292724 (1994-03-01), Kita
patent: 5298410 (1994-03-01), Phillips et al.
patent: 5326562 (1994-07-01), Scott
patent: 5348942 (1994-09-01), Little, II et al.
patent: 5354934 (1994-10-01), Pitt et al.
Lehninger, A.L., "The molecular basis of cell structure and function," Biochemistry, Second Edition, Worth Publishers, Inc., (1975) pp. 72-75.
Dellinger, C.T., "Comparison of anaphylactic reactions to asparaginase derived from Escherichia Coli and from Erwinia cultures," (1976) Cancer 38(4):1843-1846.
Savoca et al., "Preparation of a non-immunogenic arginase by the covalent attachment of polyethylene glycol," Biochimica et Biophysica ACTA, (1979) 578:47-53.
Bieth, J.G., "Pathophysiological interpretation of kinetic constants of protease inhibitors," Bull. Euro. Physiopath. Resp. (1980) 16:183-195.
Davis et al., "Hypouricaemic effect of polyethyleneglycol modified urate oxidase," (1981) Lancet 2:281-283.
Davis, S. et al., "Alteration of the circulating life and antigenic properties of bovine adenosine deaminase in mice by attachment of polyethylene glycol," (1981) Clin. exp. Immunol. 46:649-652.
Knauer, D.J. et al., "The .gamma. subunit of 7 S nerve growth factor binds to cells via complexes formed with two cell-secreted nexins," (1982) J. Biol. Chem. 257(23):15098-15104.
Veronese, et al., "Anti-inflammatory and pharmacokinetic properties of superoxide dismutase derivatized with polyethylne glycol via active esters," (1983) J. Pharm. Pharmacol. 35:281-283.
Eaton, D.L. et al., "Purification of human fibroblast urokinase proenzyme and analysis of its regulation by proteases and protease nexin," (1984) J. Biol. Chem. 259(10):6241-6247.
Travis, J. et al., "Human plasma proteinase inhibitors," (1983) Ann. Rev. Biochem. 52:655-709.
Eaton, D.L. et al., "Phorbol ester and mitogens stimulate human fibroblast secretions of plasmin-activatable plasminogen activator and protease nexin, an antiactivator/antiplasmin," (1983) J. Cell Biol. 97(2):323-8.
Till, G.O. et al., "Oxygen radical dependent lung damage following thermal injury of rat skin," (1983) J. Trauma 23(4):269-277.
Scott, R.W. et al., "Purification of human protease nexin," (1983) J. Biol. Chemistry 258(7):10439-10444.
Nishimura, H. et al., "Modification of batroxobin with activated polyethylene glycol: reduction of binding ability towards anti-batroxobin antibody and retention of defrinogenation activity in circulation of preimmunized dogs," (1983) Life Sciences 33:1467-1473.
Scott, R.W., et al., "Protease-nexin," (1985) J. Biol. Chem. 260(11):7029-7034.
Courtney, M., et al., "Synthesis in E. coli of .alpha..sub.1 -antitrypsin variants of therapeutic potential for emphysema and thrombosis," (1985) Nature 313:149-151.
Gardell et al., "Site-directed mutagenesis shows that tyrosine 248 of carboxypeptidase A does not play a crucial role in catalysis," (1985) Nature 317:551-555.
Graf, L., et al., "Selective alteration of substrate specificity by replacement of aspartic acid-189 with lysine in the binding pocket of tryspin," (1987) Biochemistry 26:2616-2623.
Farrell, D.H., et al. "Glycosaminoglycans on fibroblasts accelerate thrombin inhibition by protease nexin-1," (1987) Biochem. J. 245:543-550.
Baker, J.B., et al., "Protease nexin I. Structure and potential functions," (1987) The Pharmacology and Toxicology of Proteins, UCLA Symposia, Alan R. Liss, Inc., Series V, 65:307-323.
Sommer, J. et al., "cDNA sequence coding for a rat gli-derived nexin and its homology to members of the serpin superfamily," (1987) Biochemistry 26:6407-6410.
McGrogan, M. et al., "Molecular cloning and expression of two forms of human protease nexin I," (1988) Bio/Technology 6:172-177.
Cunningham B.C. et al. "High-resolution epitope mapping of hGH-receptor interactions by alanine-scanning mutagenesis," (1989) Science 244:1081-1085.
Engh, R.A., et al., "Modeling the intact form of the .alpha..sub.1 -proteinase inhibitor," (1990) Protein Engineering 3(5):469-477.
Nucci, M.L. et al., "The therapeutic value of poly(ethylene glycol)-modified proteins," (1991) Adv. Drug Delivery Res. 6:133-151.
Evans, D.L., "Protease specificity and heparin binding and activation of recombinant protease nexin I," (1991) J. Biol. Chem. 266(33):22307-22312.
De Vos, A.M. et al., "Human growth hormone and extracellular domain of its receptor: crystal structure of the complex," (1992) Science 255:306-312.
Hedstrom, L. et al., "Converting trypsin to chymotrypsin: the role of surface loops," (1992) Science 255:1249-1253.
Konrad, M.W., "The immune system as a barrier to delivery of protein therapeutics," (1993) Biological Barriers to Protein Delivery, Plenum Press, N.Y. and London, Chapter 14, pp. 409-437.
Ferraiolo, B.L. et al., "Goals and analytical methodologies for protein disposition studies," (1992) Protein Pharmacokinetics and Metabolism, Plenum Press, NY, Chapter 1, pp. 1-33.
Hendricks Keith D.
Hobbs Lisa J.
Incyte Pharmaceuticals Inc.
LandOfFree
Cysteine-pegylated proteins does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Cysteine-pegylated proteins, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Cysteine-pegylated proteins will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1724419