Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1994-08-02
1996-09-24
Allen, Marianne P.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
514 4, 530303, 530304, 530305, 530866, C07K 1462, A61K 3828, C12N 1500, C12N 1517
Patent
active
055590942
ABSTRACT:
Analogs of human insulin containing an aspartic acid at position 1 of the B chain (Asp.sup.B1), and optionally, having a gln modification at position 13 (Gln.sup.B13), display modified physico-chemical and pharmacokinetic properties which enable them to be long acting. These analogs are useful in the treatment of hyperglycemia because they are soluble and display an increased tendency to self-associate.
REFERENCES:
patent: 4617149 (1986-10-01), DiMarchi et al.
Brader, et. al., "Insulin hexamers: new conformations and applications", Trends In Biochemical Sciences, 16:341-345 (1991).
Derewenda, et al., "Phenol stabilizes more helix in a new symmetrical zinc insulin hexamer", Nature, 338:594-596 (1989).
Chothia, et al., "Transmission of conformational change in insulin", Nature, 302: 500-505 (1983).
Kruger, et. al., "Cooperativity and Intermediate States in the T.fwdarw.R Structural Transformation of Insulin", Biol. Chem. Hoppe-Seyler, 371: 669-673 (1990).
Bentley, et. al., "Structure of insulin in 4-zinc insulin", Nature, 261: 166-168 (1976).
Smith et. al., "The Structure of a Rhombohedral R.sub.6 Insulin Hexamer That Binds Phenol", Biopolymers, 32: 441-445 (1992).
Renscheidt, et. al., "A Solution Equivalent of the 2Zn.fwdarw.4Zn transformation of insulin in the crystal", Eur. J. Biochem, 142: 7-14 (1984).
Brader, et. al., "Characterization of the R-State Insulin Hexamer and Its Derivatives. The Hexamer Is Stabilized by Heterotropic Ligand Binding Interactions", Biochemistry, 30: 6636-6645 (1991).
Brange, et. al., "Chemical Stability of Insulin 2. Formation of Higher Molecular Weight Transformation Products During Storage of Pharmaceutical Preparations", Pharmaceutical Research 9: No. 6, 727-734 (1992).
Brange, et. al., "Chemical stability of insulin 3. Influence of excipients, formulations, and pH" Acta Pharm. Nord., 4: 149-158 (1992).
Brange, et. al., "Chemical Stability of Insulin. 1. Hydrolytic Degradation During Storage of Pharmaceutical Preparations", Pharmaceutical Research, 9: No. 6, 715-726 (1992).
Brems, et, al. "Improved insulin stability through amino acid substitution" Protein Engineering, 5 (No. 6), 519-525 (1992).
Brange, et, al., "Monomeric Insulins and Their Experimental and Clinical Implications", Diabetes Care, 13, No. 9, 923-954 (1990).
Brange, et. al., "Designing insulin for diabeses therapy by protein engineering" Current Opinion in Structural Biology, 1, 934-940 (1991).
DiMarchi, et. al., "Synthesis of a fast-acting insulin based on structural homology with insulin-like growth factor I", Peptides: Chemistry and Biology, Proceedings of the Twelfth American Peptide Symposium, 26-28 (1992).
Goldman, et, al., "Zinc Binding, Circular Dichroism, and Equilibrium Sedimentation Studies on Insulin (Bovine) and Several of Its Derivatives" Biochemistry, 13, No. 22, 4566-4574 (1974).
Bentley, et. al., "Role of B13 Glu in Insulin Assembly" J. Mol. Biol. 228, 1163-1176 (1992).
Wollmer, et. al., "Structural Transition in the Metal-Free Hexamer of Protein-Engineered [B13 Gln] Insulin" Biol. Chem. Hoppe-Seyler, 370 1045-1053 (1989).
Wollmer, et. al., "Phenol-Promoted Structural Transformation of Insulin in Solution" Biol. Chem. Hoppe-Seyler, 368, 903-911 (1987).
Grant, et. al., "Differences in the Nature of the Interaction of Insulin and Proinsulin with Zinc" Biochem. J., 126, 433-440 (1972).
Hol, et. al., "The a-helix dipole and the properties of proteins" Nature, 273, 443-446 (1978).
Shoemaker, et. al., "Tests of the helix dipole model for stabilization of a-helices" Nature, 326 563-567 (1987).
Presta, et. al., "Helix Signals in Proteins" Science, 240, 1632-1641 (1988).
Richardson, et. al., "Amino Acid Preferences for Specific Locations at the Ends of a Helices", Science, 240, 1648-1652 (1988).
Kline, et. al., "Complete Sequence-Specific .sup.1 H NMR Assignments for Human Insulin" Biochemistry, 29, 2906-2913 (1990).
Goeders, et. al., "Absorption Kinetics of Regular and Isophane (NPH) Insulin In The Normal Dog" Domestic Animal Endocrinology, 4(1): 43-50 (1987).
Blundell, et al. "Insulin: The Structure In The Crystal And Its Reflection In Chemistry and Biology",, Adv. Protein Chem., 26:279-329 (1972).
Baker, et al, "The Structure of 2Zn Pig Insulin Crystals At 1.5.ANG. Resolution" Philos. Trans. R. Soc. London, B., 319: 369-456 (1988).
Merck Index (11th Edition), 789-790 (1989).
Frank, et al, "The production of Human Proinsulin And Its Transformation To Human Insulin And C-Peptide" Peptides: Synthesis-Structure-Function, Proc. Seventh Am. Pept. Symp. Eds.D. Rich and E. Gross, 729-738 (1981).
Frank, et al, "Insulin and Proinsulin Conformation in Solution" Diabetes, 21 supp.2: 486-491 (1972).
Serrano, et al, "Capping and .alpha.-helix stability" Nature 342:296-299 (1989).
Markowitz, J., et al, "Experimental Surgery of the Pancreas" Experimental Surgery Including Surgical Physiology, 236-252 (1964).
Kornberg, et al, "Glucose-6-Phosphate Dehydrogenase" Methods In Enzymology 1:323-327 (1955).
Bathelmai, et al "Enzymatische Bestimmungen der Glucose in Blut, Liquor und Harn" Klin. Wochenschr. 40:585 (1962).
Monod, et al. "On The Nature of Allosteric Transistions: A Plausible Model" J. Mol. Biol. 12: 88.varies.118 (1965).
Binder, et al "A Theoretical Model for the Absorption of Soluble Insulin" Artifical Systems For Insulin Delivery edited by P. Brunetti, et al., Raven Press, N.Y. 53-57 1983).
Stewart, et al Solid Phase Peptide Synthesis Freeman and Co., San Francisco, 1-103 (1969).
Chance, et al, "The Production of Human Insulin Using Recombinant DNA Technology And A New Chain Combination Procedure" Peptides: Synthesis-Structure-Function Proceedings of the Seventh American Peptide Symposium Edited by D. H. Rich and E. Gross, 721-728 (1981).
Bakaysa Diane L.
Brems David N.
Allen Marianne P.
Eli Lilly and Company
Maciak Ronald S.
Norman Douglas K.
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