Thrombin inhibitor

Details Thrombin inhibitor Thrombin inhibitor

1996-09-17

1999-11-16

Tsang, Cecilia J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 14, 530326, 530327, 530382, A61K 3803, C07K 708

Patent

active

059858338

ABSTRACT:
A thrombin inhibitor is disclosed. The thrombin inhibitor comprises: (1) a segment which inactivates or sequesters thrombin; (2) a segment comprising a portion of the fibrinogen .gamma.' chain that binds to the thrombin exosite, such as amino acid residues (414-427) and amino acid residues (414-425) of the native human fibrinogen .gamma.' sequence.

REFERENCES:
patent: 5182260 (1993-01-01), Maraganore et al.
patent: 5196403 (1993-03-01), Maraganore et al.
patent: 5196404 (1993-03-01), Maraganore et al.
patent: 5240913 (1993-08-01), Maraganore et al.
patent: 5242810 (1993-09-01), Maraganore et al.
patent: 5256559 (1993-10-01), Maraganore et al.
patent: 5425936 (1995-06-01), Maraganore et al.
patent: 5433940 (1995-07-01), Maraganore et al.
patent: 5446131 (1995-08-01), Maraganore
Hortin et al. Inhibition of Thrombin's Clotting Activity by Synthetic Peptide Segements of its Inhibitors and Substrates, Biochemical and Biophysical Research Communications, vol. 169, No. 2, pp. 437-442. Jun. 15, 1990.
Maraganore et al. Design and Characterization of Hirulogs: A Novel Class of Bivalent Peptie Inhibitors of Thrombin, Biochemistry vol. 29, pp. 7095-7101, 1990.
Hortin et al. `Allosteric Changes in Thrombin's Activity Produced by Peptides Corresponding to Segments of Natrual Inhibitors and Substrates`, Journal of Biological Chemistry, vol. 266 pp. 6866-687, Apr. 1991.
L.J. Berliner and Y. Sugawara, "Human .alpha.-Thrombin Binding to Nonpolymerized Fibrin-Sepharose: Evidence for an Anionic Binding Region," Biochemistry 24:7005-7009, 1985.
E. Kaczmarek and J. McDonagh, "Thrombin Binding to the A.alpha.-, B.beta.-, and .gamma.-Chains of Fibrinogen and to Their Remnants Contained in Fragment E," 263 (27) :13896-13900, 1988.
J.M. Maraganore, et al., "Anticoagulant Activity of Synthetic Hirudin Peptides," J. Biol. Chem. 264 (15) 8692-8698, 1989.
D.A. Meh, et al., "Identification and Characterization of the Thrombin Binding Sites on Fibrin," J. Biol. Chem. 271 (38) :23121-23125, 1996.
M.A.A. Parry, et al., "Kinetic Mechanism for the Interaction of Hirulog with Thrombin," Biochemistry 33:14807-14814, 1994.
M. Guillin, et al., "Thrombin Specificity," Thrombosis and Haemostasis 74(1):129-133, 1995.
N.E. Kirschbaum, et al., "Characterization of the .gamma. Chain Platelet Binding Site on Fibrinogen Fragment D," Blood 79(10):2643-2648, 1992.
D.H. Farrell, et al., "Recombinant Human Fibrinogen and Sulfation of the .gamma.' Chain," Biochemistry 30:9414-9420, 1991.
K.R. Siebenlist and M.W. Mosesson, "Peak 2 fibrinogen serves as the carrier of plasma factor XIII," Abstract 48, Blood Coagulation and Fibrinolysis 4:833, 1993.
S.O. Lawrence, et al., "Purification and Functional Characterization of Homodimeric .gamma.B-.gamma.B Fibrinogen From Rat Plasma," Blood 82(8):2406-2413, 1993.
C.G. Binnie and S.T. Lord, "The Fibrinogen Sequences That Interact With Thrombin," Blood 81(12:3186-3192, 1993.
J.M. Maraganore, et al., "Design and Characterization of Hirulogs: A Novel Class of Bivalent Peptide Inhibitors of Thrombin," Biochemistry 29:7095-7101, 1990.
G.L. Hortin, "Sulfation of a Gamma-Chain Variant of Human Fibrinogen," Biochemistry International 19(6):1355-1362, 1989.
D.L. Amrani, et al., "The Role of Fibrinogen A.alpha. Chains in ADP-Induced Platelet Aggregation in the Presence of Fibrinogen Molecules Containing .gamma.' Chains," Blood 72(3):919-924, 1988.
C.W. Francis, et al., "Carboxyl-terminal amino acid sequences of two variant forms of the .gamma. chain of human plasma fibrinogen," Proc. Natl. Acad. Sci. USA 85:3358-3362, 1988.
D.W. Ghung and E.W. Davie, ".gamma. and .gamma.' Chains of Human Fibrinogen Are Produced By Alternative mRNA Processing," Biochemistry 23:4232-4236, 1984.
G.A. Homandberg, et al., "Amino Acid Sequences of the Carboxyl-Terminal Regions of Rat Plasma Fibrinogen .gamma..sub.A and .gamma.' Chains," Thrombosis Research, 39:263-269, 1985.
M.W. Mosesson, et al., "Human Platelet Fibrinogen Gamma Chain Structure," Blood 63(5):990-995, 1984.
C.D. Legrele, et al., "Evidence For Two Classes Of Rat Plasma Fibrinogen .gamma. Chains Differing By Their Cooh-Terminal Amino Acid Sequences," Biochemical and Biophysical Research Communications 105(2):521-520, 1982.
C. Wolfenstein-Todel and M.W. Mosesson, "Carboxy-Terminal Amino Acid Sequence of a Human Fibrinogen .gamma.-Chain Variant (.gamma.')," Biochemistry 20:6146-6149, 1981.
C. Wolfenstein-Todel and M.W. Mosesson, "Human plasma fibrinogen heterogeneity: Evidence for an extended carboxyl-terminal sequence in a normal .gamma. chain variant (.gamma.')," Proc. Natl. Acad. Sci. USA 77(9):5069-5073, 1980.
C.Y. Liu, et al., "The Binding of Thrombin by Fibrin*," The Journal of Biological Chemistry 254(20):10421-10425, 1979.
N.E. Stathakis, et al., "Human Fibrinogen Heterogeneities. Preparation and Characterization of .gamma. and .gamma.' Chains*," Thrombosis Research 13:467-475, 1978.
M.W. Mosesson, et al., "Human Fibrinogen Heterogeneities," The Journal of Biological Chemistry 247(16):5223-5227, 1972.
G.L. Hortin and B.M. Benutto, "Inhibition of Thrombin's Clotting Activity By Synthetic Peptide Segments Of Its Inhibitors And Substrates," Biochemical and Biophysical Research Communications 169(2):437-442, 1990.

Affiliated with

Also associated with

Rating

Thrombin inhibitor does not yet have a rating. At this time, there are no reviews or comments for this patent.

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

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-1324770