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    Bradykinin receptors as a therapeutic target

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    Authors
    Howl, John D.
    Payne, Sarah J.
    Issue Date
    2003
    
    Metadata
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    Abstract
    Biologically-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.
    Citation
    Expert Opinion on Therapeutic Targets, 7(2): 277-85
    Publisher
    London: Informa Healthcare
    Journal
    Expert Opinion on Therapeutic Targets
    URI
    http://hdl.handle.net/2436/29935
    DOI
    10.1517/14728222.7.2.277
    PubMed ID
    12667103
    Additional Links
    http://www.expertopin.com/doi/abs/10.1517/14728222.7.2.277
    Type
    Journal article
    Language
    en
    ISSN
    1744-7631
    ae974a485f413a2113503eed53cd6c53
    10.1517/14728222.7.2.277
    Scopus Count
    Collections
    Research Institute in Healthcare Science

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