Bradykinin receptor ligands: therapeutic perspectives
Top Cited Papers
- 1 October 2004
- journal article
- review article
- Published by Springer Nature in Nature Reviews Drug Discovery
- Vol. 3 (10) , 845-852
- https://doi.org/10.1038/nrd1522
Abstract
Kinins, which are produced by the action of kallikrein enzymes, are blood-derived local-acting peptides that have broad effects mediated by two related G-protein-coupled receptors termed the bradykinin receptors. The endogenous kallikrein-kinin system controls blood circulation and kidney function, and promotes inflammation and pain in pathological conditions, which has led to interest in developing modulators of bradykinin receptors as potential therapeutics. This review discusses recent progress in our understanding of the genetics, molecular biology and pathophysiology of kinins and their receptors, as well as developments in medicinal chemistry, which have brought us closer to therapeutic applications of kinin receptor ligands in various indications. The potential of kinin receptor antagonists as novel analgesic agents that do not result in tolerance or have a liability for abuse has attracted particular interest.Keywords
This publication has 62 references indexed in Scilit:
- Variation in bradykinin receptor genes increases the cardiovascular risk associated with hypertensionPublished by Oxford University Press (OUP) ,2003
- Structure of the mammalian kinin receptor gene locusInternational Immunopharmacology, 2002
- Nonpeptide Bradykinin B2 Receptor Antagonists: Conversion of Rodent-Selective Bradyzide Analogues into Potent, Orally-Active Human Bradykinin B2 Receptor AntagonistsJournal of Medicinal Chemistry, 2002
- The kallikrein-kininogen-kinin system: lessons from the quantification of endogenous kininsPeptides, 2000
- Bradykinin B 2 Receptor Antagonism Attenuates Blood Pressure Response to Acute Angiotensin-Converting Enzyme Inhibition in Normal MenHypertension, 2000
- Hypoalgesia and altered inflammatory responses in mice lacking kinin B1 receptorsProceedings of the National Academy of Sciences, 2000
- Effect of Bradykinin-Receptor Blockade on the Response to Angiotensin-Converting–Enzyme Inhibitor in Normotensive and Hypertensive SubjectsNew England Journal of Medicine, 1998
- Effect of High Salt Intake in Mutant Mice Lacking Bradykinin-B 2 ReceptorsHypertension, 1997
- Targeted Disruption of a B2 Bradykinin Receptor Gene in Mice Eliminates Bradykinin Action in Smooth Muscle and NeuronsJournal of Biological Chemistry, 1995
- Expression cloning of a rat B2 bradykinin receptor.Proceedings of the National Academy of Sciences, 1991