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

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

Journal Name: Current Medicinal Chemistry

Volume 19 , Issue 20 , 2012

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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.

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

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Article Details

Year: 2012
Page: [3301 - 3309]
Pages: 9
DOI: 10.2174/092986712801215937
Price: $65

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