Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1993-06-22
1995-11-07
Warden, Jill A.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
514 17, 514 18, 530329, 530331, A61K 3700, A61K 3702, C07K 500, C07K 700
Patent
active
054648203
ABSTRACT:
The invention is directed to substrate analogs which are specific for tissue kallikrein. These analogs contain a sequence which corresponds to at least positions 388 to 390 of human kininogen, and which has a 4-aminophenylalanine (Phe(4NH.sub.2)), or a structurally or functionally similar residue, corresponding to position 389. These substrate analogs are useful in compositions and methods for the treatment or prevention of biological activities associated with tissue kallikrein including inflammation, the regulation of blood flow, the regulation of proenzyme activity through processing, shock, hypotension, vascular leakage, and the perception of pain.
REFERENCES:
patent: 4818748 (1989-04-01), Bender et al.
patent: 4835253 (1989-05-01), Burton
Everest et al. J. Med. Microbiol. vol. 38 p. 316 (1993)-abstract only.
John M. Stewart et al., "Design of Bradykinin antagonists", Marshal, GR Peptides: Chemistry and Biology (1988) ESCOM: Leiden, pp. 433-437.
George Triadafilopoulos et al., "Differential Effects of Clostridium difficile Toxins A and B on Rabbit Ileum" Gastroenterology 1987; 93:273-9.
Hideki Okunishi et al., "The Design of Substrate Analogue Tissue Kallikrein Inhibitors", Hypertension Supplement I, vol. 8, No. 4, Apr. 1986, pp. 1-114-118.
R. W. Colman et al., "Kallikrein-Kinin System in Pathologic Conditions", Bradykinin, Kallidin and Kallikrein Supplement, E. G. Erdos editor Springer-Verlag, New York 1979, pp. 569-607.
R. Vogel, "Kallikrein Inhibitors", Bradykinin, Kallidin and Kallikrein Supplement, E. G. Erdos editor Springer-Verlag, New York 1979, pp. 163-225.
Hideki Okunishi et al., "In vivo inhibition of tissue kallikreins by kininogen sequence analogue peptides", In: Abe K. Kinins V. Plenum, New York 1988; In Press, 6 pp.
Hideki Okunishi et al., "Specificity of Substrate Analogue Inhibitors of Human Urinary Kallikrein", Blood Pressure Council Suppl. I Hypertension, vol. 7, No. 3, May-Jun. 1985, pp. I-72-75.
Timothy S. Gaginella et al., "Kinins as mediators of intestinal secretion", Editorial Review, 1989, the American Physiological Society, pp. G1-G15.
C. Pothoulakis, "Abstract" presented at Barcelona, Jul. 19-24, 1993, United European Gastroenterology Week, Inhibition of Intestinal Effects of Clostridium Difficile Toxin a By a Specific Substance P Antagonist.
Hideki Okunishi et al., "In Vivo Assay Of Specific Kallikrein Inhibitors", Vasodepressor Hormones, 1987 Birkhauser Verlag Basel, pp. 381-390.
J. Burton et al., Poster presented at Boston University; Evans Research Day, Sep. 1993, "Effect of the Kallikrein Antagonist on Clostridium Difficile Toxin a Induced Intestinal Secretion".
George Triadafilopoulos et al., "Comparative Study of Clostridium difficile Toxin A and Cholera Toxin in Rabbit Ileum", Gastroenterology, 1989; 97:1186-92.
Milind S. Deshpande et al., "Mapping the Binding Site of Tissue Kallikrein: Preparation and Testing of All Possible Substrate Analog Inhibitors Homologous with the Sequence of Kininogen between Ser.sup.388 and GLn.sup.392 ". Reprinted from Journal of Medicinal Chemistry, 1992, vol. 35, No. 17, pp. 3095-3102.
J. Garcia Leme, "Bradykinin-System", Inflammation, 1978, Chapter 14, pp. 464-522.
Burton James
Dong Zhengxin
Frigo Timothy B.
Huff Sheela J.
The University Hospital
Warden Jill A.
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