2.50
Hdl Handle:
http://hdl.handle.net/2436/29935
Title:
Bradykinin receptors as a therapeutic target
Authors:
Howl, John D.; Payne, Sarah J.
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
Issue Date:
2003
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:
Article
Language:
en
ISSN:
1744-7631
Appears in Collections:
Molecular Pharmacology Research Group

Full metadata record

DC FieldValue Language
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): 277-85en
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.en
dc.language.isoenen
dc.publisherLondon: Informa Healthcareen
dc.relation.urlhttp://www.expertopin.com/doi/abs/10.1517/14728222.7.2.277en
dc.subjectPeptidesen
dc.subjectTherapeuticsen
dc.subject.meshAnalgesicsen
dc.subject.meshAnti-Inflammatory Agentsen
dc.subject.meshBradykininen
dc.subject.meshCardiovascular Systemen
dc.subject.meshDrug Designen
dc.subject.meshHumansen
dc.subject.meshInflammationen
dc.subject.meshKallikreinsen
dc.subject.meshKininogensen
dc.subject.meshKininsen
dc.subject.meshPainen
dc.subject.meshReceptors, Bradykininen
dc.subject.meshSignal Transductionen
dc.titleBradykinin receptors as a therapeutic targeten
dc.typeArticleen
dc.identifier.journalExpert Opinion on Therapeutic Targetsen

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