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

Authors: Tateishi, U.; Oka, T.; Inoue, T.

Source: Current Medicinal Chemistry, Volume 19, Number 20, July 2012 , pp. 3301-3309(9)

Publisher: Bentham Science Publishers

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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.

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

Document Type: Research article

DOI: http://dx.doi.org/10.2174/092986712801215937

Publication date: 2012-07-01

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Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.