Cysteine protease inhibitors effective for in vivo use

Details Cysteine protease inhibitors effective for in vivo use Cysteine protease inhibitors effective for in vivo use

1992-08-20

1994-12-20

Higel, Floyd D.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530330, 530332, 530331, 544168, 560 10, 560 18, 560 37, 560 45, A61K 3702, C07K 506, C07K 508, C07K 510

Patent

active

053746236

ABSTRACT:
A method of treating medical conditions with proteinase inhibitors of the formula: ##STR1## wherein B is H or an amino acid blocking group for the N-terminal amino acid nitrogen;

REFERENCES:
patent: 4518528 (1985-05-01), Rasnick
patent: 5055451 (1991-10-01), Krantz et al.
van Noorden and Everts, "Selective Inhibition of Cysteine Proteinases by Z-Phe-AlaCH.sub.2 F Suppresses Digestion of Collagen by Fibroblasts and Osteoclasts," 178 Biochemical and Biophysical Research Communications 178-184 (1991).
Rifkin, Vernillo, Kleekner, Auszmann, Rosenberg and Zimmerman, "Cathepsin B and L Activities in Isolated Osteoclasts," 179 Biochemical and Biophysical Research Communications 63-69 (1991).
Grinde, "The Thiol Proteinase Inhibitors, Z-Phe-Phe-CHN.sub.2 and Z-Phe-Ala-CHN.sub.2, Inhibit Lysosomal Protein Degradation in Isolated Rat Hepatocytes," 757 Biochimica et Biophysica Acta 15-19 (1983).
Mason, Bartholomew and Hardwick, "The Use of Benzyloxycarbonyl[.sup.125 I]iodotyrosylalanyldiazomethane as a Probe for Active Cysteine Proteinases in Human Tissues," 263 Biochem. J. 945-949 (1989).
van Noorden, Smith and Rasnick, "Cysteine Proteinase Activity in Arthritic Rat Knee Joints and the Effects of a Selective Systemic Inhibitor, Z-Phe-Ala-CH.sub.2 F," 15 J. Rheumatol. 1525-1535 (1988).
van Noorden, Vogels and Smith, "Localization and Cytophotometric Analysis of Cathepsin B Activity in Unfixed and Undecalified Cryostat Sections of Whole Rat Knee Joints," 37 J. Histochemistry and Cytochemistry 617-624 (1989).
Delaisse, Eeckhout and Vaes, "In Vivo and In Vitro Evidence for the Involvement of Cysteine Proteinases in Bone Resorption," 125 Biochemical and Biophysical Research Communications 441-447 (1984).
Hayes, Stubberfield, McBride and Wilson, "Alterations in Cysteine Proteinase Content of Rat Lung Associated with Development of Pneumocystis Carinii Infection," 59 Infection and Immunity 3581-3588 (1991).
Cohen, Gregoret, Amiri, Aldape, Railey and McKerrow, "Arresting Tissue Invasion of a Parasite by Protease Inhibitors Chosen With The Aid of Computer Modeling," 30 Biochemistry 11221-11229 (1991).
Ashall, Harris, Roberts, Healy and Shaw, "Substrate Specificity and Inhibitor Sensitivity of a Trypanosomatid Alkaline Peptidase," 1035 Biochimica et Biophysica Acta 293-299 (1990).
Ashall, Angliker and Shaw, "Lysis of Trypanosomes by Peptidyl Fluoromethyl Ketones," 170 Biochemical and Biophysical Research Communications 923-929 (1990).
Rosenthal, Wollish, Palmer and Rasnick, "Antimalarial Effects of Peptide Inhibitors of a Plasmodium Falciparum Cysteine Proteinase," 88 J. Clin Invest. 1467-1472 (1991).
Smith, Rasnick, Burdick, Cho, Rose and Vahratian, "Visualization of Time-Dependent Inactivation of Human Tumor Cathepsin B Isozymes by a Peptidyl Fluoromethyl Ketone Using a Fluorescent Print Technique," 8 Anti-cancer Research 525-530 (1988).
Gordon and Mourad, "The Site of Activation of Factor X by Cancer Procoagulant," 2 Blood Coagulation and Fibrinolysis 735-739 (1991).
Cox, Cho, Eley and Smith, "A Simple, Combined Fluorogenic and Chromogenic Method for the Assay of Proteases in Gingival Crevicular Fluid," 25 J. Periodont. Res. 164-171 (1990).
Uitto, Larjava, Heino and Sorsa, "A Protease of Bacteroides Gingivalis Degrades Cell Surface and Matrix Glycoproteins of Cultured Gingival Fibroblasts and Induces Secretion of Collagenase and Plasminogen Activator," 57 Infection and Immunity 213-218 (1989).
Kunimatsu, Yamamoto, Ichimaru, Kato and Kato, "Cathepsins B, H and L Activities in Gingival Crevicular Fluid From Chronic Adult Periodontitis Patients and Experimental Gingivitis Subjects," 25 J Periodont Res 69-73 (1990).
Beighton, Radford and Naylor, "Protease Activity in Gingival Crevicular Fluid From Discrete Periodontal Sites in Humans With Periodontitis or Gingivitis"; 35 Archs oral Biol. 329-335 (1990).
Cox and Eley, "Preliminary Studies on Cysteine and Serine Proteinase Activities in Inflamed Human Gingiva Using Different 7-Amino-4-Trifluoromethyl Courmarin Substrates and Protease Inhibitors," 32 Archs oral Biol. 599-605 (1987).
Eisenhauer, Hutchinson, Javed and McDonald, "Identification of a Cathepsin B-Like Protease in the Crevicular Fluid of Gingivitis Patients," 62 J Dent Res 917 (1983).
von Figura, Steckel, Conary, Hasilik and Shaw, "Heterogeneity in Late-Onset Metachromatic Leukodystrophy. Effect of Inhibitors of Cysteine Proteinases," 39 Am J Hum Genet. 371-382 (1986).
Valentine, Winand, Pradhan, Moise, de Lahunta, Kornegay and Cooper, "Canine X-Linked Muscular Dystrophy as an Animal Model of Duchenne Muscular Dystrophy: A Review," 42 Am J Hum Genet 352-356 (1992).
Knott, Orr, Montgomery, Sullivan and Weston, "the Expression and Purification of Human Rhinovirus Protease 3C," 182 Eur. J. Biochem. 547-555 (1989).
Baricos, O'Connor, Cortez, Wu and Shah, "The Cysteine Proteinase Inhibitor, E-64, Reduces Proteinuria in an Experimental Model of Glomerulonephritis," 155 Biochemical and Biophysical Research Communications 1318-1323 (1988).
Dahlmann, Rutschmann, Kuehn and Reinauer, "Activation of the Multicatalytic Proteinase from Rat Skeletal Muscle by Fatty Acids or Sodium Dodecyl Sulphate," 228 Biochem. J. 171-177 (1985).
Kaltenbronn, "Renin Inhibitors Containing Isosteric Replacements of the Amide Bond Connecting the P.sub.3 and P.sub.2 Sites," 33, J. Med. Chem., 838-841 (1990).
Krantz, et al. Copp, Coles, Smith and Heard, "Peptidyl (Acyloxy)methyl Ketones and the Quiescent Affinity Label Concept: The Departing Group as a Variable Structural Element in the Design of Inactivators of Cysteine Proteinases," 30 Biochemistry 4678-4687 (1991).
Smith, Copp, Coles, Pauls, Robinson, Spencer, Heard and Krantz, "New Inhibitors of Cysteine Proteinases. Peptidyl Acyloxymethyl Ketones and the Quiescent Nucleofuge Strategy," 110 J. Am. Chem. Soc. 4429-4431 (1988).
Shaw, Wikstrom and Ruscica, "An Exploration of the Primary Specificity Site of Cathepsin B," 222 Archives of Biochemistry and Biophysics 424-429 (1983).
Shaw, "Cysteinyl Proteinases and Their Selective Inactivation," 63 Advances in Enzymology and Related Areas of Molecular Biology 271-347 (1990).

Affiliated with

Also associated with

Rating

Cysteine protease inhibitors effective for in vivo use 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 protease inhibitors effective for in vivo use, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Cysteine protease inhibitors effective for in vivo use will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-2386317