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@ARTICLE{Accardo:9565,
author = {Accardo, A. and Mansi, R. and Mirisco, A. and Mangiapia, G.
and Paduano, L. and Tesauro, D. and Radulescu, A. and
Aurilio, M. and Aloj, L. and Arra, C. and Morelli, G.},
title = {{P}eptide modified nanocarriers for selective targeting of
bombesin receptors},
journal = {Molecular BioSystems},
volume = {6},
issn = {1742-206X},
address = {Cambridge},
publisher = {Royal Society of Chemistry},
reportid = {PreJuSER-9565},
pages = {878 - 887},
year = {2010},
note = {We 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.},
abstract = {The 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).},
keywords = {Cell Line, Tumor / Chelating Agents: chemistry /
Heterocyclic Compounds, 1-Ring: chemistry / Humans /
Liposomes: chemistry / Models, Theoretical / Molecular
Structure / Peptides: chemistry / Peptides: metabolism /
Receptors, Bombesin: metabolism / Chelating Agents (NLM
Chemicals) / Heterocyclic Compounds, 1-Ring (NLM Chemicals)
/ Liposomes (NLM Chemicals) / Peptides (NLM Chemicals) /
Receptors, Bombesin (NLM Chemicals) /
1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
(NLM Chemicals) / J (WoSType)},
cin = {IFF-4 / IFF-5 / Jülich Centre for Neutron Science JCNS
(JCNS) ; JCNS},
ddc = {540},
cid = {I:(DE-Juel1)VDB784 / I:(DE-Juel1)VDB785 /
I:(DE-Juel1)JCNS-20121112},
pnm = {BioSoft: Makromolekulare Systeme und biologische
Informationsverarbeitung / Großgeräte für die Forschung
mit Photonen, Neutronen und Ionen (PNI)},
pid = {G:(DE-Juel1)FUEK505 / G:(DE-Juel1)FUEK415},
experiment = {EXP:(DE-MLZ)KWS2-20140101},
shelfmark = {Biochemistry $\&$ Molecular Biology},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:20567774},
UT = {WOS:000277315800015},
doi = {10.1039/b923147a},
url = {https://juser.fz-juelich.de/record/9565},
}