A highly constrained cyclic (S,S)-CDC- peptide is a potent inhibitor of carotid artery thrombosis in rabbits

Απλή σελίδα τεκμηρίου
dc.contributor.authorRoussa, V. D.en
dc.contributor.authorStathopoulou, E. M.en
dc.contributor.authorPapamichael, N. D.en
dc.contributor.authorEnglezopoulos, C. V.en
dc.contributor.authorRousouli, K. I.en
dc.contributor.authorTrypou, P.en
dc.contributor.authorMoussis, V.en
dc.contributor.authorTellis, C. C.en
dc.contributor.authorKatsouras, C. S.en
dc.contributor.authorTsikaris, V.en
dc.contributor.authorTselepis, A. D.en
dc.contributor.authorMichalis, L. K.en
dc.date.accessioned2015-11-24T16:55:03Z
dc.date.available2015-11-24T16:55:03Z
dc.identifier.issn0953-7104-
dc.identifier.urihttps://olympias.lib.uoi.gr/jspui/handle/123456789/10246
dc.rightsDefault Licence-
dc.subjectplatelet integrinen
dc.subjectcarotid thrombosisen
dc.subjectantiplatelet drugsen
dc.subjectcyclic peptidesen
dc.subjectnon-rgd peptidesen
dc.subjectrabbitsen
dc.subjectplatelet integrin alpha(iib)beta(3)en
dc.subjectfibrinogen gamma-chainen
dc.subjectglycoprotein iib-iiiaen
dc.subjectmonoclonal-antibodyen
dc.subjectwashed plateletsen
dc.subjectrgd peptidesen
dc.subjectreceptoren
dc.subjectbindingen
dc.subjectantagonistsen
dc.subjectargen
dc.titleA highly constrained cyclic (S,S)-CDC- peptide is a potent inhibitor of carotid artery thrombosis in rabbitsen
heal.abstractInhibition of platelet aggregation is indispensable for the treatment of acute arterial thrombotic episodes. We have previously reported the synthesis of a highly constrained cyclic peptide, that incorporates the -CDC- sequence, (S,S) PSRCDCR-NH(2), which potently inhibits aggregation and fibrinogen binding to human platelets in vitro. We have tested the safety and efficacy of the peptide on the electrically induced carotid artery thrombosis experimental rabbit model. The peptide's effects on carotid blood flow, thrombus weight, in vitro and ex vivo platelet aggregation, and bleeding and hemostatic parameters were evaluated. The peptide was administered via the femoral vein. Carotid blood flow was continuously monitored for 90 min after electrical thrombus formation. The peptide, at 12 mg/kg, prevented total artery occlusion and significantly preserved carotid artery's patency compared with placebo and eptifibatide. Furthermore, (S, S) PSRCDCR-NH(2) administration at 12 mg/kg reduced thrombus weight, whereas it inhibited ex vivo ADP, arachidonic acid (AA) and collagen-induced platelet aggregation. Moreover (S,S) PSRCDCR-NH(2) at 12 mg/kg presented significantly higher inhibitory effects on AA and collagen-induced ex vivo platelet aggregation compared to eptifibatide. The peptide at any dose did not affect the coagulation cascade, the bleeding times or the hemostatic response of the animals. Thus highly constrained cyclic peptides like (S,S) PSRCDCR-NH(2) that incorporate the -CDC- motif and fulfil certain conformational criteria represent novel compounds that potently inhibit thrombus formation, ex vivo platelet aggregation and carotid artery occlusion superiorly to other non-RGD peptides, such as YMESRADR, without causing hemorrhagic complications in a rabbit model of arterial thrombosis.en
heal.accesscampus-
heal.fullTextAvailabilityTRUE-
heal.identifier.primaryDoi 10.3109/09537104.2010.531795-
heal.identifier.secondary<Go to ISI>://000293599400006-
heal.identifier.secondaryhttp://informahealthcare.com/doi/abs/10.3109/09537104.2010.531795-
heal.journalNamePlateletsen
heal.journalTypepeer reviewed-
heal.languageen-
heal.publicationDate2011-
heal.recordProviderΠανεπιστήμιο Ιωαννίνων. Σχολή Θετικών Επιστημών. Τμήμα Χημείαςel
heal.typejournalArticle-
heal.type.elΆρθρο Περιοδικούel
heal.type.enJournal articleen

Αρχεία

Φάκελος/Πακέτο αδειών

Προβολή: 1 - 1 of 1
Μικρογραφία εικόνας
Ονομα:
license.txt
Μέγεθος:
1.74 KB
Μορφότυπο:
Item-specific license agreed upon to submission
Περιγραφή:
Κατεβάστε

Συλλογές

Άρθρα σε επιστημονικά περιοδικά ( Ανοικτά). ΧΗΜ