title: Tumor targeting and imaging using cyclic RGD-PEGylated gold nanoparticle probes with directly conjugated iodine-125.
abstract: Radioactive iodine-labeled, cyclic RGD-PEGylated gold nanoparticle (AuNP) probes are designed and synthesized for targeting cancer cells and imaging tumor sites. These iodine-125-labeled cRGD-PEG-AuNP probes are stable in various conditions including a range of pHs and high salt and temperature conditions. These probes can target selectively and be taken up by tumor cells via integrin αvβ3-receptor-mediated endocytosis with no cytotoxicity. The probes show a significant increase in the avidity of αvβ3 integrin compared to the corresponding free cRGD peptides. In-vivo SPECT/CT imaging results show that the iodine-125-labeled cRGD-PEG-AuNP probes can target the tumor site as soon as 10 min after injection, and also that cyclic RGD peptides are needed for efficient and long-term in-vivo monitoring. The results suggest that the probes circulate through the whole body, including renal filtration, and are excretable. These promising results show that radioactive-iodine-labeled gold nanoprobes have potential for highly specific and sensitive tumor imaging or for use as angiogenesis-targeted SPECT/CT imaging probes.
authors.affiliation: Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul 110-744, South Korea.
authors.forename: Young-Hwa
authors.initials: YH
authors.lastname: Kim
authors.forename: Jongho
authors.initials: J
authors.lastname: Jeon
authors.forename: Su Hyun
authors.initials: SH
authors.lastname: Hong
authors.forename: Won-Kyu
authors.initials: WK
authors.lastname: Rhim
authors.forename: Yun-Sang
authors.initials: YS
authors.lastname: Lee
authors.forename: Hyewon
authors.initials: H
authors.lastname: Youn
authors.forename: June-Key
authors.initials: JK
authors.lastname: Chung
authors.forename: Myung Chul
authors.initials: MC
authors.lastname: Lee
authors.forename: Dong Soo
authors.initials: DS
authors.lastname: Lee
authors.forename: Keon Wook
authors.initials: KW
authors.lastname: Kang
authors.forename: Jwa-Min
authors.initials: JM
authors.lastname: Nam
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D003952:Diagnostic Imaging / Q000379:methods*; D006046:Gold / Q000737:chemistry*; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000378:metabolism; D036341:Intercellular Signaling Peptides and Proteins; D007457:Iodine Radioisotopes; D053768:Metal Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D051379:Mice; D008819:Mice, Nude; D015335:Molecular Probes / Q000737:chemistry*; D009369:Neoplasms / Q000473:pathology*; D010455:Peptides / Q000378:metabolism; D010456:Peptides, Cyclic / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D023041:Xenograft Model Antitumor Assays
chemical_list: D039302:Integrin alphaVbeta3; D036341:Intercellular Signaling Peptides and Proteins; D007457:Iodine Radioisotopes; D015335:Molecular Probes; D010455:Peptides; D010456:Peptides, Cyclic; C507169:cyclic arginine-glycine-aspartic acid peptide; C057986:echistatin; D011092:Polyethylene Glycols; D006046:Gold