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AbstractBiologically-active kinins, including bradykinin (BK) and Lys(0)-BK (kallidin), are short-lived peptide mediators predominantly generated by the enzymatic action of kallikreins on kininogen precursors. A diverse spectrum of physiological and pathological actions attributed to local kinin production is a consequence of the activation of G-protein-coupled receptors (GPCRs). Currently, two major subtypes of kinin receptor, designated B(1) and B(2), are recognised, although there is much evidence for pharmacological heterogeneity, particularly within the B(2) receptors. Considering these facts and the widespread distribution of kinin receptors in many human tissues, it is no surprise that the therapeutic potential of kinins and kinin receptor antagonists remains the focus of numerous investigations. Studies in animals and animal tissues, instrumental in elucidating the biological roles of kinins, are well-documented in numerous excellent reviews. Unfortunately, and despite the enormous potential illustrated by animal studies, attempts to develop kinin analogues as therapeutic agents to combat human disease have largely proven disappointing. Consequently, this review selectively focuses upon studies that are directly relevant to the targeting of human BK receptors as a therapeutic intervention. In addition to providing a succinct review of well-documented pathological conditions to which kinin receptors contribute, the authors have also included more recent data that illustrate new avenues for the therapeutic application of kinin analogues.
CitationExpert Opinion on Therapeutic Targets, 7(2): 277-85
PublisherLondon: Informa Healthcare
JournalExpert Opinion on Therapeutic Targets
CollectionsMolecular Pharmacology Research Group
- Kinins and kinin receptors in the nervous system.
- Authors: Walker K, Perkins M, Dray A
- Issue date: 1995 Jan
- International union of pharmacology. XLV. Classification of the kinin receptor family: from molecular mechanisms to pathophysiological consequences.
- Authors: Leeb-Lundberg LM, Marceau F, Müller-Esterl W, Pettibone DJ, Zuraw BL
- Issue date: 2005 Mar
- The plasma and tissue kininogen-kallikrein-kinin system: role in the cardiovascular system.
- Authors: Marcondes S, Antunes E
- Issue date: 2005 Jan
- Kinin B(1) receptors and the cardiovascular system: regulation of expression and function.
- Authors: McLean PG, Perretti M, Ahluwalia A
- Issue date: 2000 Nov
- Bradykinin receptor ligands: therapeutic perspectives.
- Authors: Marceau F, Regoli D
- Issue date: 2004 Oct