Factor VIIA inhibitors

Details Factor VIIA inhibitors Factor VIIA inhibitors

1997-09-17

1999-02-23

Wax, Robert A.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

435 691, 435 692, 435 697, A61K 3800, C12P 2106, C12P 2104

Patent

active

058744070

ABSTRACT:
The invention provides compositions having a Factor VIIa active site inhibitor domain and a tissue factor domain for the inhibition of FVIIa. The invention also provides pharmaceutical compositions comprising the novel compositions as well as their use in diagnostic, therapeutic, and prophylactic methods.

REFERENCES:
patent: 5312736 (1994-05-01), Rasmussen et al.
patent: 5346991 (1994-09-01), Roy et al.
patent: 5416093 (1995-05-01), Shuman
patent: 5434073 (1995-07-01), Dawson et al.
Altman et al., "Intracellular expression of BPTI fusion proteins and single column cleavage/affinity purification by chymotrypsin" Protein Eng. 4:593-600 (1991).
Auerswald et al., "Expression, Isolation and Characterization of 369:27-35 (1988).
Bach, Ronald R., "Initiation of Coagulation by Tissue Factor" CRC Critical Reviews in Biochemistry 23(4):339-368 (1988).
Badimon et al., "Hirudin and Other Thrombin Inhibitors; Experimental Results and Potential Clinical Applications" TCM 1(6):261-267 (1991).
Beckmann, J. et al., "Preparation of chemically `mutated` aprotinin homologues by semisynthesis" European Journal of Biochemistry 176:675-682 (1988).
Bode, W. et al., "Natural protein proteinase inhibitors and their interaction with proteinases" European Journal of Biochemistry 204:433-451 (1992).
Bone, R.C., "Modulators of Coagulation: A Critical Appraisal of Their Role In Sepsis" Arch Intern Med 152:1381-1389 (1992).
Bromberg et al., "Tissue factor promotes melanoma metastasis by a pathway independent of blood coagulation" Proc. Natl. Acad. Sci. USA 92:8205-8209 (1995).
Broze, Jr. et al., "The Lipoprotein-Associated Coagulation Inhibitor That Inhibits the Factor VII-Tissue Factor Complex Also Inhibits Factor Xa: Insight Into Its Possible Mechanism of Action" Blood 71(2):335-343 (Feb. 1988).
Broze, Jr. et al., "Regulation of Coagulation by a Multivalent Kunitz-Type Inhibitor" Biochemistry 29(33):7539-7546 (1990).
Broze, Jr., et al., "Inhibition of Factor VIIa/Tissue Factor by Antithrombin III and Tissue Factor Pathway Inhibitor" Blood 82:1679-1680 (1993).
Broze, Jr., George J., "The Role of Tissue Factor Pathway Inhibitor in a Revised Coagulation Cascade" Sem. in Hematology 29(3):159-169 (1992).
Carson et al., "The role of tissue factor in the production of thrombin" Blood. Coag. Fibrinol. 4:281-292 (1993).
Castro et al., "Does the Kunitz domain from the Alzheimer's amyloid Beta protein precursor inhibit a kallikrein responsible for post-translational processing of nerve growth factor precursor?" FEBS 08591 267(2):207-212 (1990).
Chabbat et al., "Aprotinin Is A competitive Inhibitor of The Factor VIIa-Tissue Factor Complex" Thrombosis Research 71:205-215 (1993).
Chu et al., "Mosaic structure of globular domains in the human type VI collagen .alpha. 3 chain: similarity to von Willebrand Factor, fibronectin, actin, salivary proteins and aprotinin type protease inhibitors" EMBO Journal 9(3):385-393 (1990).
Colman, R.W., "The Role of Plasma Proteases In Septic Shock" The New England J. of Med. 320(18):1207-1209 (1989).
Creasey et al., "Tissue Factor Pathway Inhibitor Reduces Mortality from Escherichia coli Septic Shock" J. Clin. Invest. 91:2850-2860 (1993).
Creighton et al., "Biosynthesis, Processing, and Evolution of Bovine Pancreatic Trypsin Inhibitor" Cold Spring Harbor Symp Quant Biol. 52:511-519 (1987).
Davie et al., "The Coagulation Cascade: Initiation, Maintenance, and Regulation" Biochemistry 30(43):10363-10370 (1991).
Dennis et al., "Kunitz Domain Inhibitors of Tissue Factor--Factor VIIa; I. Potent Inhibitors Selected from Libraries by Phage Display" Journal of Biological Chemistry 269(35):22129-22136 (1994).
Dennis et al., "Kunitz Domain Inhibitors of Tissue Factor--Factor VIIa; I. Potent and Specific Inhibitors by Competitive Phage Selection" Journal of Biological Chemistry 269(35):22137-22144 (1994).
Drake et al., "Functional Tissue Factor Is Entirely Cell Surface Expressed on Lipopolysaccharide-stimulated Human Blood Monocytes and a Constitutively Tissue Factor-producing Neoplastic Cell Line" Journal of Cell Biology 109:389 (1989).
Eigenbrot et al., "Structural effects induced by removal of a disulfide-bridge: the X-ray structure of the C30A/C51A mutant of basic pancreatic trypsin inhibitor at 1.6 Angstrom" Protein Eng. 3:591-598 (1990).
Gibbs et al., "Identification of the Factor VIIa Binding Site on Tissue Factor by Homologous Loop Swap and Alanine Scanning Mutagenesis" Biochemistry 33:14003-14010 (1994).
Girard et al., "Functional significance of the Kunitz-type inhibitory domains of lipoprotein-associated coagulation inhibitor" Nature 338:518-520 (1989).
Girard et al., "Inhibition of Factor VIIa--Tissue Factor Coagulation Activity by a Hybrid Protein" Science 248:1421-1424 (1990).
Hagen et al., "Characterization of a cDNA coding for human factor VII" Proc. Natl. Acad. Sci. USA 83:2412-2416 (1986).
Hamamoto et al., "Inhibitory Properties of Full-length and Truncated Recombinant Tissue Factor Pathway Inhibitor (TFPI)" Journal of Biological Chemistry 268(12):8704-8710 (1993).
Harlos et al., "Crystal structure of the extracellular region of human tissue factor" Nature 370:662-666 (1994).
Haskel et al., "Prevention of Arterial Reocclusion After Thrombolysis With Recombinant Lipoprotein-Associated Coagulation Inhibitor" Circulation 84:821-827 (1991).
Hochstrasser, "Kunitz-Type Proteinase Inhibitors Derived by Limited Proteolysis of the Inter-.alpha.-Trypsin Inhibitor, X" Biol. Chem. Hoppe-Seyler 366:473-478 (1985).
Holst et al., "Antithrombotic Properties of a Truncated Recombinant Tissue Factor Pathway Inhibitor in an Experimental Venous Thrombosis Model" Haemostasis 23(Suppl. 1):112-117 (1993).
Hynes et al., "X-ray Crystal Structure of the Protease Inhibitor Domain of Alzheimer's Amyloid .beta.-Protein Precursor" Biochemistry 29:10018-10022 (1990).
Kelley et al., "Analysis of the Factor VIIa Binding Site on Human Tissue Factor: Effects of Tissue Factor Mutations on the Kinetics and Thermodynamics of Binding" Biochemistry 34:10383-10392 (1995).
Kossiakoff et al., "Molecular recognition in biological systems: From activation to inhibition" Bio. Society Transactions 21:614-618 (1993).
Kunitz et al., "Isolation from Beef Pancreas of Crystalline Trypsinogen, Trypsin, a Trypsin Inhibitor, and an Inhibitor-Trypsin Compound" J. Gen. Physiol. 19:991-1007 (1936).
Kunkel et al., "Rapid and Efficient Site-specific Mutagenesis Without Phenotypic Selection" Methods in Enzymology 154:367-382 (1987).
Laskowski et al., "Protein Inhibitors of Proteinases" Ann. Rev. Biochem. 49:593-626 (1980).
Lauritzen et al., "BPTI and N-Terminal Extended Analogues Generated by Factor X.sub.a Cleavage and Cathepsin C Trimming of a Fusion Protein Expressed in Escherichia coli" Prot. Express. Purif. 2:372-378 (1991).
Lawson et al., "Complex-dependent Inhibition of Factor VIIa by Antithrombin III and Heparin" Journal of Biological Chemistry 268(2):767-770 (1993).
Mann, Kenneth G., "Correspondence--Response" Blood 82:1680-1681 (1993).
Maraganore, "Thrombin, Thrombin Inhibitors, and the Arterial Thrombotic Process" Thrombosis and Haemostasis 70(1):208-211 (1993).
Maraganore et al., "Design and Characterization of Hirulogs: A Novel Class of Divalent Peptide Inhibitors of Thrombin" Biochemistry 29:7095-7101 (1990).
Means et al., "Chemical Modifications of Proteins: History and Applications" Bioconjugate Chemistry 1:2-12 (1990).
Morrissey et al., "Molecular Cloning of cDNA for Tissue Factor, the Cellular Receptor for the Initiation of the Coagulation Protease Cascade" Cell 50(1):129-135 (1987).
Muller et al., "Structure of the Extracellular Domain of Human Tissue Factor: Location of the Factor VIIa Binding Site" Biochemistry 33:10864-10870 (1994).
O'Brien et al., "Factor VIII-Bypassing Activity of Bovine Tissue Factor Using the Canine Hemophilic Model" J. Clin. Invest. 82:206-211 (1988).
Paborsky et al., "Mammalian Cell Transient Expression of Tissue Factor for the Production of Antigen" Protein Eng. 3(6):547-553 (1990).
Paborsky et al., "Purification of Recombinant Human Tissue Factor" Biochemistry 28(20):8072-8077 (1989).
Pawashe e

Affiliated with

Also associated with

Rating

Factor VIIA inhibitors does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Factor VIIA inhibitors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Factor VIIA inhibitors will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-306959