Comparative in vivo evaluation of two novel 99mTc labelled bombesin derivatives

Gourni, E; Bouziotis, P; Zikos, C; Loudos, G; Xanthopoulos, S; Fani, M; Archimandritis, SC; Varvarigou, AD

dc.contributor.author	Gourni, E	en
dc.contributor.author	Bouziotis, P	en
dc.contributor.author	Zikos, C	en
dc.contributor.author	Loudos, G	en
dc.contributor.author	Xanthopoulos, S	en
dc.contributor.author	Fani, M	en
dc.contributor.author	Archimandritis, SC	en
dc.contributor.author	Varvarigou, AD	en
dc.date.accessioned	2014-03-01T01:23:42Z
dc.date.available	2014-03-01T01:23:42Z
dc.date.issued	2006	en
dc.identifier.issn	0168-9002	en
dc.identifier.uri	https://dspace.lib.ntua.gr/xmlui/handle/123456789/17109
dc.subject	99mTc	en
dc.subject	Bombesin	en
dc.subject	Gamma camera imaging	en
dc.subject	Gastrin releasing peptide	en
dc.subject.classification	Instruments & Instrumentation	en
dc.subject.classification	Nuclear Science & Technology	en
dc.subject.classification	Physics, Particles & Fields	en
dc.subject.classification	Spectroscopy	en
dc.subject.other	Biological organs	en
dc.subject.other	Cells	en
dc.subject.other	Derivatives	en
dc.subject.other	Growth kinetics	en
dc.subject.other	Synthesis (chemical)	en
dc.subject.other	Tumors	en
dc.subject.other	99mTc	en
dc.subject.other	Bombesin	en
dc.subject.other	Gamma camera imaging	en
dc.subject.other	Gastrin releasing peptides	en
dc.subject.other	Amino acids	en
dc.title	Comparative in vivo evaluation of two novel 99mTc labelled bombesin derivatives	en
heal.type	journalArticle	en
heal.identifier.primary	10.1016/j.nima.2006.08.141	en
heal.identifier.secondary	http://dx.doi.org/10.1016/j.nima.2006.08.141	en
heal.language	English	en
heal.publicationDate	2006	en
heal.abstract	Bombesin (BN), a 14 amino acid peptide, is an analogue of human gastrin-releasing-peptide (GRP) that binds to GRP receptors (GRP-R) with high affinity and specificity. In addition to this physiological role, GRP, through its interaction with GRP-R, promotes tumour growth in a number of human cancer cell lines. The GRP receptors are over-expressed on a variety of human cancer cells. Aim of the present work is the study of two novels BN-like peptides, by investigating the radiochemical and radiopharmacological behaviour of their complexes with metals. The derivatives under study are: Gly-Gly-Cys-Aca-BN [2-14] where Aca: 6-amino-hexanoic acid. Pyroglutamic acid in the bombesin molecule has been replaced by the chemical group Gly-Gly-Cys-Aca, which bears an amino-acid combination capable of complexing a variety of radiometals. The other derivative under study is: Gly-Gly-Cys-Aca-BN [7-14]. This moiety of the peptide has been chosen because it has been proven to be a potent GRP agonist. The peptide derivatives were synthesized by SPPS, according to the Fmoc strategy and were identified by reverse phase high performance liquid chromatography (RP-HPLC). Radiolabelling with Tc-99m was performed via the precursor Tc-99m-gluconate. The stability of the radiolabelled species was examined with time. In vivo studies of the two Tc-99m-labelled derivatives were performed, comparatively, in normal mice, attention being focused on GRP receptor-bearing organs, and in experimentally induced prostate cancer models. Experimental tumours were imaged in a small field-of-view animal gamma camera. (c) 2006 Elsevier B.V. All rights reserved.	en
heal.publisher	ELSEVIER SCIENCE BV	en
heal.journalName	Nuclear Instruments and Methods in Physics Research, Section A: Accelerators, Spectrometers, Detectors and Associated Equipment	en
dc.identifier.doi	10.1016/j.nima.2006.08.141	en
dc.identifier.isi	ISI:000243241300080	en
dc.identifier.volume	569	en
dc.identifier.issue	2 SPEC. ISS.	en
dc.identifier.spage	518	en
dc.identifier.epage	521	en