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000009565 0247_ $$2DOI$$a10.1039/b923147a
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000009565 084__ $$2WoS$$aBiochemistry & Molecular Biology
000009565 1001_ $$0P:(DE-HGF)0$$aAccardo, A.$$b0
000009565 245__ $$aPeptide modified nanocarriers for selective targeting of bombesin receptors
000009565 260__ $$aCambridge$$bRoyal Society of Chemistry$$c2010
000009565 300__ $$a878 - 887
000009565 3367_ $$0PUB:(DE-HGF)16$$2PUB:(DE-HGF)$$aJournal Article
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000009565 440_0 $$020661$$aMolecular BioSystems$$v6$$x1742-206X$$y5
000009565 500__ $$aWe thank Prof. Helmut Maecke, University Hospital Basel, Switzerland for the helpful discussions and suggestions. We are indebted to EMIL, European Molecular Imaging Laboratories, for financial support. Some of us (LP, GM, AR) wish to thank the Forschungszentrum Julich for provision of beam time.
000009565 520__ $$aThe present work describes new supramolecular aggregates obtained by co-assembling two different amphiphilic molecules, one containing the bioactive bombesin peptide (BN), or a scramble sequence, and the other, the DOTA chelating agent, (C18)(2)DOTA, capable of forming stable complexes with the radioactive (111)In(III) isotope. The peptide in the amphiphilic monomer is spaced by the lipophilic moiety through ethoxylic spacers of different length: a shorter spacer with five units of dioxoethylene moieties in (C18)(2)L5-peptide, or a longer spacer consisting of a Peg3000 residue in (C18)(2)Peg3000-peptide. Structural characterization by SANS and DLS techniques indicates that, independently from the presence of the peptide containing monomer in the final composition, the predominant aggregates are liposomes of similar shape and size with a hydrodynamic radius R(h) around 200 nm and bilayer thickness, d, of 4 nm. In vitro data show specific binding of the (111)In-(C18)(2)DOTA/(C18)(2)L5-[7-14]BN 90:10 liposomes in receptor expressing cells. However, the presence of the Peg3000 unit on the external liposomal surface, could hide the peptide and prevent the receptor binding. In vivo experiments using (111)In-(C18)(2)DOTA/(C18)(2)L5-[7-14]BN show the expected biological behavior of aggregates of such size and molecular composition, moreover there is an increase in concentration of the GRPR targeting aggregate in the tumors compared to control at the 48 h time point evaluated (2.4% ID/g versus 1.6% ID/g).
000009565 536__ $$0G:(DE-Juel1)FUEK505$$2G:(DE-HGF)$$aBioSoft: Makromolekulare Systeme und biologische Informationsverarbeitung$$cP45$$x0
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000009565 588__ $$aDataset connected to Web of Science, Pubmed
000009565 650_2 $$2MeSH$$aCell Line, Tumor
000009565 650_2 $$2MeSH$$aChelating Agents: chemistry
000009565 650_2 $$2MeSH$$aHeterocyclic Compounds, 1-Ring: chemistry
000009565 650_2 $$2MeSH$$aHumans
000009565 650_2 $$2MeSH$$aLiposomes: chemistry
000009565 650_2 $$2MeSH$$aModels, Theoretical
000009565 650_2 $$2MeSH$$aMolecular Structure
000009565 650_2 $$2MeSH$$aPeptides: chemistry
000009565 650_2 $$2MeSH$$aPeptides: metabolism
000009565 650_2 $$2MeSH$$aReceptors, Bombesin: metabolism
000009565 650_7 $$00$$2NLM Chemicals$$aChelating Agents
000009565 650_7 $$00$$2NLM Chemicals$$aHeterocyclic Compounds, 1-Ring
000009565 650_7 $$00$$2NLM Chemicals$$aLiposomes
000009565 650_7 $$00$$2NLM Chemicals$$aPeptides
000009565 650_7 $$00$$2NLM Chemicals$$aReceptors, Bombesin
000009565 650_7 $$060239-18-1$$2NLM Chemicals$$a1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
000009565 650_7 $$2WoSType$$aJ
000009565 693__ $$0EXP:(DE-MLZ)KWS2-20140101$$1EXP:(DE-MLZ)FRMII-20140101$$5EXP:(DE-MLZ)KWS2-20140101$$6EXP:(DE-MLZ)NL3ao-20140101$$aForschungs-Neutronenquelle Heinz Maier-Leibnitz$$eKWS-2: Small angle scattering diffractometer$$fNL3ao$$x0
000009565 7001_ $$0P:(DE-HGF)0$$aMansi, R.$$b1
000009565 7001_ $$0P:(DE-HGF)0$$aMirisco, A.$$b2
000009565 7001_ $$0P:(DE-HGF)0$$aMangiapia, G.$$b3
000009565 7001_ $$0P:(DE-HGF)0$$aPaduano, L.$$b4
000009565 7001_ $$0P:(DE-HGF)0$$aTesauro, D.$$b5
000009565 7001_ $$0P:(DE-Juel1)VDB4342$$aRadulescu, A.$$b6$$uFZJ
000009565 7001_ $$0P:(DE-HGF)0$$aAurilio, M.$$b7
000009565 7001_ $$0P:(DE-HGF)0$$aAloj, L.$$b8
000009565 7001_ $$0P:(DE-HGF)0$$aArra, C.$$b9
000009565 7001_ $$0P:(DE-HGF)0$$aMorelli, G.$$b10
000009565 773__ $$0PERI:(DE-600)2188635-0$$a10.1039/b923147a$$gVol. 6, p. 878 - 887$$p878 - 887$$q6<878 - 887$$tMolecular BioSystems$$v6$$x1742-206X$$y2010
000009565 8567_ $$uhttp://dx.doi.org/10.1039/b923147a
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