On the structural basis of the hypertensive properties of angiotensin II: A solved mystery or a controversial issue?

dc.contributor.authorTzakos, A. G.en
dc.contributor.authorGerothanassis, I. P.en
dc.contributor.authorTroganis, A. N.en
dc.date.accessioned2015-11-24T16:43:19Z
dc.date.available2015-11-24T16:43:19Z
dc.identifier.issn1568-0266-
dc.identifier.urihttps://olympias.lib.uoi.gr/jspui/handle/123456789/8682
dc.rightsDefault Licence-
dc.subjectprotein-coupled receptorsen
dc.subjectnuclear-magnetic-resonanceen
dc.subjectside-chain conformationen
dc.subjectaqueous-solutionen
dc.subjectbiological-activitiesen
dc.subjectat(1) receptoren
dc.subjecttype-1 receptoren
dc.subjectcyclic analogsen
dc.subjectcircular-dichroismen
dc.subjectbinding-sitesen
dc.titleOn the structural basis of the hypertensive properties of angiotensin II: A solved mystery or a controversial issue?en
heal.abstractAngiotensin II (AII), Asp(1)-Arg(2)-Val(3)-Tyr(4)-Ile(5)-His(6)-Pro(7)-Phe(8), the primary active hormone of the Renin-Angiotensin-System (RAS), is a major vasoconstrictor implicated in the cause of hypertension. To unravel the question of the biologically active conformation(s) of this flexible peptide hormone and to better understand the stereoelectronic requirements that lead to the molecular basis of hypertension, we will analyze research efforts in the identification of pharmacophoric groups of AII and three general approaches for structural characterisation: the free peptide - ligand approach, the receptor based approach, and approaches that target the peptide - receptor complex. The free peptide ligand based approach can be further categorized to: (a) conformational analysis of AII and linear peptide analogues in aqueous solution; (b) the use of solvents of medium dielectric constants; (c) conformationally restricted analogues, with emphasis to cyclic analogues; (d) the use of receptor - simulating environments, and (e) non-peptide mimetics. The receptor and peptide - receptor based approaches can be categorised to: (a) The use of monoclonal antibodies and (b) the generic description of AII receptor sites through homology modelling and mutagenesis studies. These investigations, with particular emphasis to recent developments, have greatly assisted in the identification of pharmacophoric groups for receptor activation and the development of several models of AII - receptor complexes.en
heal.accesscampus-
heal.fullTextAvailabilityTRUE-
heal.identifier.primaryDoi 10.2174/1568026043451375-
heal.identifier.secondary<Go to ISI>://000220152200004-
heal.journalNameCurr Top Med Chemen
heal.journalTypepeer reviewed-
heal.languageen-
heal.publicationDate2004-
heal.publisherBentham Science Publishersen
heal.recordProviderΠανεπιστήμιο Ιωαννίνων. Σχολή Θετικών Επιστημών. Τμήμα Χημείαςel
heal.typejournalArticle-
heal.type.elΆρθρο Περιοδικούel
heal.type.enJournal articleen

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