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Metabolism-Resistant Bradykinin Antagonists: Development and Applications

  • John M. Stewart , Lajos Gera , Eunice J. York , Daniel C. Chan , Eric J. Whalleya , Paul A. Bunn and Raymond J. Vavrek
Published/Copyright: July 5, 2005
Biological Chemistry
From the journal Volume 382 Issue 1

Abstract

Bradykinin plays many roles in normal and pathological physiology, but rapid enzymatic degradation made elucidation of its functions extremely difficult. Development of effective degradation-resistant antagonists made it possible to delineate these roles and to open the way for development of new drugs to control pathology due to excess production of bradykinin. Presently available peptide bradykinin antagonists are extremely potent, are completely resistant to enzymatic degradation, and are orally available. Non-peptide bradykinin antagonists have also been discovered. Development of bradykinin antagonists as drugs for cancer, inflammation and trauma is anticipated.

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Published Online: 2005-07-05
Published in Print: 2001-01-06

Copyright © 2001 by Walter de Gruyter GmbH & Co. KG

Articles in the same Issue

  1. To Our Authors, Readers and Subscribers
  2. Kinins 1925-2000
  3. The Expanded Human Kallikrein (KLK) Gene Family: Genomic Organisation, Tissue-Specific Expression and Potential Functions
  4. Novel Roles of Kallistatin, a Specific Tissue Kallikrein Inhibitor, in Vascular Remodeling
  5. Signal Transduction from Bradykinin, Angiotensin, Adrenergic and Muscarinic Receptors to Effector Enzymes, Including ADP-Ribosyl Cyclase
  6. Classification of Kinin Receptors
  7. Metabolism-Resistant Bradykinin Antagonists: Development and Applications
  8. Kinins, Receptors, Kininases and Inhibitors Where Did They Lead Us?
  9. Bradykinin Signalling to MAP Kinase: Cell-Specific Connections versus Principle Mitogenic Pathways
  10. Kinins and Epithelial Ion Transport in the Alimentary Tract
  11. Role of the Renal Kallikrein-Kinin System in the Development of Salt-Sensitive Hypertension
  12. Role of the Light Chain of High Molecular Weight Kininogen in Adhesion, Cell-Associated Proteolysis and Angiogenesis
  13. Activation of the Kinin-Forming Cascade on the Surface of Endothelial Cells
  14. Kallikrein and Kinin Receptor Expression in Inflammation and Cancer
  15. Altered Neutrophil Homeostasis in Kinin B1 Receptor-Deficient Mice
  16. Cystatins as Calpain Inhibitors: Engineered Chicken Cystatin- and Stefin B-Kininogen Domain 2 Hybrids Support a Cystatin-Like Mode of Interaction with the Catalytic Subunit of µ-Calpain
  17. Synthetic Peptides and Fluorogenic Substrates Related to the Reactive Site Sequence of Kunitz-Type Inhibitors Isolated from Bauhinia: Interaction with Human Plasma Kallikrein
  18. Identification and Characterization of an Aromatic Amino Acid Decarboxylase from the Filarial Nematode, Dirofilaria immitis
  19. Molecular Cloning and Pharmacological Characterization of the Canine B1 and B2 Bradykinin Receptors
  20. Ligand-Mediated Regulation of Kinin Receptors in the Rabbit
  21. Activation of Sphingosine Kinase by the Bradykinin B2 Receptor and Its Implication in Regulation of the ERK/MAP Kinase Pathway
https://doi.org/10.1515/BC.2001.006

Articles in the same Issue

  1. To Our Authors, Readers and Subscribers
  2. Kinins 1925-2000
  3. The Expanded Human Kallikrein (KLK) Gene Family: Genomic Organisation, Tissue-Specific Expression and Potential Functions
  4. Novel Roles of Kallistatin, a Specific Tissue Kallikrein Inhibitor, in Vascular Remodeling
  5. Signal Transduction from Bradykinin, Angiotensin, Adrenergic and Muscarinic Receptors to Effector Enzymes, Including ADP-Ribosyl Cyclase
  6. Classification of Kinin Receptors
  7. Metabolism-Resistant Bradykinin Antagonists: Development and Applications
  8. Kinins, Receptors, Kininases and Inhibitors Where Did They Lead Us?
  9. Bradykinin Signalling to MAP Kinase: Cell-Specific Connections versus Principle Mitogenic Pathways
  10. Kinins and Epithelial Ion Transport in the Alimentary Tract
  11. Role of the Renal Kallikrein-Kinin System in the Development of Salt-Sensitive Hypertension
  12. Role of the Light Chain of High Molecular Weight Kininogen in Adhesion, Cell-Associated Proteolysis and Angiogenesis
  13. Activation of the Kinin-Forming Cascade on the Surface of Endothelial Cells
  14. Kallikrein and Kinin Receptor Expression in Inflammation and Cancer
  15. Altered Neutrophil Homeostasis in Kinin B1 Receptor-Deficient Mice
  16. Cystatins as Calpain Inhibitors: Engineered Chicken Cystatin- and Stefin B-Kininogen Domain 2 Hybrids Support a Cystatin-Like Mode of Interaction with the Catalytic Subunit of µ-Calpain
  17. Synthetic Peptides and Fluorogenic Substrates Related to the Reactive Site Sequence of Kunitz-Type Inhibitors Isolated from Bauhinia: Interaction with Human Plasma Kallikrein
  18. Identification and Characterization of an Aromatic Amino Acid Decarboxylase from the Filarial Nematode, Dirofilaria immitis
  19. Molecular Cloning and Pharmacological Characterization of the Canine B1 and B2 Bradykinin Receptors
  20. Ligand-Mediated Regulation of Kinin Receptors in the Rabbit
  21. Activation of Sphingosine Kinase by the Bradykinin B2 Receptor and Its Implication in Regulation of the ERK/MAP Kinase Pathway
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