Radiolabeled RGD peptides as integrin alpha(v)beta3-targeted PET tracers.
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.
Department of Radiology, Yokohama City University Graduate School of Medicine, 3-9, Fukuura, Yokohama, Kanagawa, 236-0004, Japan. utateish@yokohama-cu.ac.jp
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D000818:Animals; D045744:Cell Line, Tumor; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000378:metabolism*; D007553:Isotope Labeling; D009369:Neoplasms / Q000098:blood supply / Q000000981:diagnostic imaging / Q000378:metabolism; D009842:Oligopeptides / Q000378:metabolism*; D049268:Positron-Emission Tomography / Q000379:methods*; D011849:Radioactive Tracers
D039302:Integrin alphaVbeta3; D009842:Oligopeptides; D011849:Radioactive Tracers; C047981:arginyl-glycyl-aspartic acid