Journal
CURRENT MEDICINAL CHEMISTRY
Volume 19, Issue 20, Pages 3301-3309Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/092986712801215937
Keywords
Integrin; integrin alpha(v)beta3; angiogenesis; VEGF; PET; positron emission tomography; PET/CT; RGD; radiolabeled-RGD; RGD peptide
Funding
- Grant for Research and Development Project II of Yokohama City University, Japan
- Ministry of Education, Science, Sports and Culture of Japan [21591753]
- Grants-in-Aid for Scientific Research [21591753] Funding Source: KAKEN
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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.
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