Biological evaluation of an ornithine-modified 99mTc-labeled RGD peptide as an angiogenesis imaging agent

dc.contributor.author	Τσιάπα, Ειρήνη	el
dc.contributor.author	Λούντος, Γεώργιος	el
dc.contributor.author	Βαρβαρήγου, Αλεξάνδρα	el
dc.contributor.author	Φραγκογεώργη, Ειρήνη	el
dc.contributor.author	Ψειμάδας, Δημήτριος	el
dc.date.accessioned	2015-05-21T08:52:55Z
dc.date.available	2015-05-21T08:52:55Z
dc.date.issued	2015-05-21
dc.identifier.uri	http://hdl.handle.net/11400/10822
dc.rights	Αναφορά Δημιουργού-Μη Εμπορική Χρήση-Όχι Παράγωγα Έργα 3.0 Ηνωμένες Πολιτείες	*
dc.rights.uri	http://creativecommons.org/licenses/by-nc-nd/3.0/us/	*
dc.source	Τ.Ε.Ι. Αθήνας. Σχολή Τεχνολογικών Εφαρμογών. Τμήμα Μηχανικών Βιοϊατρικής Τεχνολογίας Τ.Ε.	el
dc.subject	Technetium
dc.subject	Radiolabeling
dc.subject	Ornithine
dc.subject	RGD
dc.subject	Integrin ανβ3
dc.subject	Τεχνήτιο
dc.subject	Ραδιοεπισήμανση
dc.subject	Chelator
dc.subject	Χηλικοποιητής
dc.subject	Ορνιθίνη
dc.title	Biological evaluation of an ornithine-modified 99mTc-labeled RGD peptide as an angiogenesis imaging agent	en
heal.type	journalArticle
heal.classification	Medicine
heal.classification	Medical physics
heal.classification	Ιατρική
heal.classification	Ιατρική φυσική
heal.classificationURI	http://id.loc.gov/authorities/subjects/sh00006614
heal.classificationURI	http://id.loc.gov/authorities/subjects/sh85083001
heal.classificationURI	N/A-Ιατρική
heal.classificationURI	N/A-Ιατρική φυσική
heal.keywordURI	http://id.loc.gov/authorities/subjects/sh85133086
heal.keywordURI	http://id.loc.gov/authorities/subjects/sh91005211
heal.keywordURI	http://id.loc.gov/authorities/subjects/sh2003008344
heal.contributorName	Τσοτάκος, Θεόδωρος	el
heal.contributorName	Ξανθόπουλος, Σταύρος	el
heal.contributorName	Μιχαηλίδης, Δημήτριος	el
heal.contributorName	Μπουζιώτη, Πηνελόπη Σ.	el
heal.contributorName	Νικηφορίδης, Γεώργιος Χ.	el
heal.contributorName	Καγκάδης, Γεώργιος Χ.	el
heal.identifier.secondary	doi:10.1016/j.nucmedbio.2012.10.015
heal.language	en
heal.access	campus
heal.recordProvider	Τ.Ε.Ι. Αθήνας. Σχολή Τεχνολογικών Εφαρμογών. Τμήμα Μηχανικών Βιοϊατρικής Τεχνολογίας Τ.Ε.	el
heal.publicationDate	2013-02
heal.bibliographicCitation	Tsiapa, E., Loudos, G., Varvarigou , A., Fragogeorgi, E., Psimadas, D., et.al. (2013). Biological evaluation of an ornithine-modified 99mTc-labeled RGD peptide as an angiogenesis imaging agent. "Nuclear Medicine and Biology", 40(2), February 2013. pp. 262–272. Available from: http://www.sciencedirect.com/science/article/pii/S0969805112002740#. [Accessed 11/12/2012]	en
heal.abstract	Introduction Radiolabeled RGD peptides that specifically target integrin ανβ3 have great potential in early tumor detection through noninvasive monitoring of tumor angiogenesis. Based on previous findings of our group on radiopeptides containing positively charged aminoacids, we developed a new cyclic cRGDfK derivative, c(RGDfK)-(Orn)3-CGG. This new peptide availing the polar linker (Orn)3 and the 99mTc-chelating moiety CGG (Cys-Gly-Gly) is appropriately designed for 99mTc-labeling, as well as consequent conjugation onto nanoparticles. Methods A tumor imaging agent, c(RGDfK)-(Orn)3-[CGG-99mTc], is evaluated with regard to its radiochemical, radiobiological and imaging characteristics. Results The complex c(RGDfK)-(Orn)3-[CGG-99mTc] was obtained in high radiochemical yield (> 98%) and was stable in vitro and ex vivo. It presented identical to the respective, fully analytically characterized 185/187Re complex retention time in RP-HPLC. In contrary to other RGD derivatives, we showed that the new radiopeptide exhibits kidney uptake and urine excretion due to the ornithine linker. High tumor uptake (3.87 ± 0.48% ID/g at 60 min p.i.) was observed and was maintained relatively high even at 24 h p.i. (1.83 ± 0.05 % ID/g), thus providing well-defined scintigraphic imaging. Accumulation in other organs was negligible. Blocking experiments indicated target specificity for integrin receptors in U87MG glioblastoma cells. Conclusion Due to its relatively high tumor uptake, renal elimination and negligible abdominal localization, the new 99mTc-RGD peptide is considered promising in the field of imaging ανβ3-positive tumors. However, the preparation of multifunctional SPECT/MRI contrast agents (RGD-conjugated nanoparticles) for dual modality imaging of integrin expressing tumors should be further investigated.	en
heal.journalName	Nuclear Medicine and Biology	en
heal.journalType	peer-reviewed
heal.fullTextAvailability	true