Radiotheranostics Coupled between an At-211-Labeled RGD Peptide and the Corresponding Radioiodine-Labeled RGD Peptide

DOI Web Site Web Site 被引用文献20件 参考文献38件

書誌事項

公開日
2019-03-01
資源種別
journal article
権利情報
  • http://pubs.acs.org/page/policy/authorchoice_termsofuse.html
DOI
  • 10.1021/acsomega.8b03679
公開者
American Chemical Society (ACS)

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説明

Alpha particle-emitting radionuclides have gained considerable attention for radionuclide therapy. Astatine-211 (211At) is a promising alpha particle-emitting radionuclide. 211At is a halogen that has similar chemical properties to iodine and exhibits a half-life of 7.2 h. However, direct labeling of proteins or peptides into the tyrosine residue with 211At was shown to be impractical. Herein, we demonstrate a novel 211At-labeling method using the RGD peptide as a model peptide. An 211At-labeled RGD peptide, [211At]c[RGDf(4-At)K], was prepared from a precursor with a tributylstannyl group on the phenylalanine residue in c(RGDfK) with a radiochemical yield of 63% and a radiochemical purity of >96%, and its potential for targeted radionuclide therapy was evaluated. Based on the results of biodistribution experiments, [125I]c[RGDf(4-I)K] and [211At]c[RGDf(4-At)K] showed high accumulation in the tumor and similar biodistribution. This study provides useful information for radiotheranostics between an 211At-la...

収録刊行物

  • ACS Omega

    ACS Omega 4 (3), 4584-4591, 2019-03-01

    American Chemical Society (ACS)

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