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dc.contributor.authorHowl, John D.
dc.contributor.authorPayne, Sarah J.
dc.date.accessioned2008-06-12T08:32:07Z
dc.date.available2008-06-12T08:32:07Z
dc.date.issued2003
dc.identifier.citationExpert Opinion on Therapeutic Targets, 7(2): 277-85
dc.identifier.issn1744-7631
dc.identifier.pmid12667103
dc.identifier.doi10.1517/14728222.7.2.277
dc.identifier.urihttp://hdl.handle.net/2436/29935
dc.description.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.
dc.language.isoen
dc.publisherLondon: Informa Healthcare
dc.relation.urlhttp://www.expertopin.com/doi/abs/10.1517/14728222.7.2.277
dc.subjectPeptides
dc.subjectTherapeutics
dc.subject.meshAnalgesics
dc.subject.meshAnti-Inflammatory Agents
dc.subject.meshBradykinin
dc.subject.meshCardiovascular System
dc.subject.meshDrug Design
dc.subject.meshHumans
dc.subject.meshInflammation
dc.subject.meshKallikreins
dc.subject.meshKininogens
dc.subject.meshKinins
dc.subject.meshPain
dc.subject.meshReceptors, Bradykinin
dc.subject.meshSignal Transduction
dc.titleBradykinin receptors as a therapeutic target
dc.typeArticle
dc.identifier.journalExpert Opinion on Therapeutic Targets
html.description.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.


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