Radiolabeled RGD Peptides as Integrin alpha(v)beta3–targeted PET Tracers

Title:Radiolabeled RGD Peptides as Integrin alpha(v)beta3–targeted PET Tracers

Volume: 19 Issue: 20

Author(s): U. Tateishi, T. Oka and T. Inoue

Affiliation:

Keywords: Integrin, integrin alpha(v)beta3, angiogenesis, VEGF, PET, positron emission tomography, PET/CT, RGD, radiolabeled-RGD, RGD peptide

Abstract: Imaging techniques targeting tumor angiogenesis have been investigated for past decade. Of these, the radiolabeled Arg-Gly- Asp (RGD) peptide has been focused because it has high affinity and selectivity for integrin alpha(v)beta3. Integrin alpha(v)beta3 is expressed on the plasma membrane in an active status in which it binds its ligands and transduce signals when exposed activating external stimuli of tumor angiogenesis such as vascular endothelial growth factor (VEGF). Many linear or cyclic RGD peptides were developed for positron emission tomography (PET). In this review, we focused on currently developed RGD peptides as PET probes for non-invasive detection of integrin alpha(v)beta3 expression.

Cite this article as:

Tateishi U., Oka T. and Inoue T., Radiolabeled RGD Peptides as Integrin alpha(v)beta3–targeted PET Tracers, Current Medicinal Chemistry 2012; 19 (20) . https://dx.doi.org/10.2174/092986712801215937