¹²⁵I-radiolabeled morpholine-containing arginine-glycine-aspartate (RGD) ligand of αvβ₃ integrin as a molecular imaging probe for angiogenesis

Francesca Bianchini; Nicoletta Cini; Andrea Trabocchi; Anna Bottoncetti; Silvia Raspanti; Eleonora Vanzi; Gloria Menchi; Antonio Guarna; Alberto Pupi; Lido Calorini

doi:10.1021/jm2016232

¹²⁵I-radiolabeled morpholine-containing arginine-glycine-aspartate (RGD) ligand of αvβ₃ integrin as a molecular imaging probe for angiogenesis

J Med Chem. 2012 Jun 14;55(11):5024-33. doi: 10.1021/jm2016232. Epub 2012 Jun 1.

Authors

Francesca Bianchini¹, Nicoletta Cini, Andrea Trabocchi, Anna Bottoncetti, Silvia Raspanti, Eleonora Vanzi, Gloria Menchi, Antonio Guarna, Alberto Pupi, Lido Calorini

Affiliation

¹ Department of Experimental Pathology and Oncology, University of Florence, Viale Morgagni 50, 50134 Florence, Italy.

PMID: 22621422
DOI: 10.1021/jm2016232

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Cell Adhesion
Cell Movement
Human Umbilical Vein Endothelial Cells / cytology
Human Umbilical Vein Endothelial Cells / drug effects
Humans
Integrin alphaVbeta3 / metabolism*
Iodine Radioisotopes
Ligands
Melanoma / diagnostic imaging
Models, Molecular
Molecular Probes / chemical synthesis*
Molecular Probes / chemistry
Molecular Probes / pharmacokinetics
Morpholines / chemical synthesis*
Morpholines / chemistry
Morpholines / pharmacokinetics
Multimodal Imaging
Neoplasm Transplantation
Neovascularization, Pathologic / diagnostic imaging*
Oligopeptides / chemical synthesis*
Oligopeptides / pharmacokinetics
Oligopeptides / pharmacology
Peptides, Cyclic / chemical synthesis*
Peptides, Cyclic / chemistry
Peptides, Cyclic / pharmacokinetics
Peptides, Cyclic / pharmacology
Positron-Emission Tomography
Radiopharmaceuticals / chemical synthesis*
Radiopharmaceuticals / chemistry
Radiopharmaceuticals / pharmacokinetics
Stereoisomerism
Structure-Activity Relationship
Tissue Distribution
Tomography, X-Ray Computed
Transplantation, Heterologous

Substances

Integrin alphaVbeta3
Iodine Radioisotopes
Ligands
Molecular Probes
Morpholines
Oligopeptides
Peptides, Cyclic
Radiopharmaceuticals
arginyl-glycyl-aspartic acid