title: ¹²⁵I-radiolabeled morpholine-containing arginine-glycine-aspartate (RGD) ligand of αvβ₃ integrin as a molecular imaging probe for angiogenesis.
abstract: In this paper, using a hybrid small-animal Micro SPECT/CT imaging system, we report that a new (125)I-Cilengitide-like RGD-cyclopentapeptide, containing d-morpholine-3-carboxylic acid, interacts in vivo with α(v)β(3) integrin expressed by melanoma cells. Images clearly show that the (125)I-compound has the capacity to monitor the growth of a melanoma xenograft. Indeed, retention of the labeled ligand in the tumor mass has a good tumor/background ratio, and a significant reduction of its uptake was observed after injection of unlabeled ligand. These results suggest that the use of (125)I-labeled morpholine-based RGD-cyclopentapeptides targeting α(v)β(3) positive tumors may play a role in future therapeutic strategies.
authors.affiliation: Department of Experimental Pathology and Oncology, University of Florence, Viale Morgagni 50, 50134 Florence, Italy.
authors.forename: Francesca
authors.initials: F
authors.lastname: Bianchini
authors.forename: Nicoletta
authors.initials: N
authors.lastname: Cini
authors.forename: Andrea
authors.initials: A
authors.lastname: Trabocchi
authors.forename: Anna
authors.initials: A
authors.lastname: Bottoncetti
authors.forename: Silvia
authors.initials: S
authors.lastname: Raspanti
authors.forename: Eleonora
authors.initials: E
authors.lastname: Vanzi
authors.forename: Gloria
authors.initials: G
authors.lastname: Menchi
authors.forename: Antonio
authors.initials: A
authors.lastname: Guarna
authors.forename: Alberto
authors.initials: A
authors.lastname: Pupi
authors.forename: Lido
authors.initials: L
authors.lastname: Calorini
mesh_terms: D002448:Cell Adhesion; D002465:Cell Movement; D061307:Human Umbilical Vein Endothelial Cells / Q000166:cytology / Q000187:drug effects; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000378:metabolism*; D007457:Iodine Radioisotopes; D008024:Ligands; D008545:Melanoma / Q000000981:diagnostic imaging; D008958:Models, Molecular; D015335:Molecular Probes / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D009025:Morpholines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D064847:Multimodal Imaging; D009368:Neoplasm Transplantation; D009389:Neovascularization, Pathologic / Q000000981:diagnostic imaging*; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014018:Tissue Distribution; D014057:Tomography, X-Ray Computed; D014183:Transplantation, Heterologous
chemical_list: D039302:Integrin alphaVbeta3; D007457:Iodine Radioisotopes; D008024:Ligands; D015335:Molecular Probes; D009025:Morpholines; D009842:Oligopeptides; D010456:Peptides, Cyclic; D019275:Radiopharmaceuticals; C047981:arginyl-glycyl-aspartic acid