<sup>18</sup>F-Positron Emitting/Trimethine Cyanine-Fluorescent Contrast for Image-Guided Prostate Cancer Management.


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Kommidi H., Guo H., Nurili F., Vedvyas Y., Jin M. M. , McClure T. D. , ...Daha Fazla

Journal of medicinal chemistry, cilt.61, sa.9, ss.4256-4262, 2018 (SCI Expanded İndekslerine Giren Dergi) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 61 Konu: 9
  • Basım Tarihi: 2018
  • Doi Numarası: 10.1021/acs.jmedchem.8b00240
  • Dergi Adı: Journal of medicinal chemistry
  • Sayfa Sayıları: ss.4256-4262

Özet

[E-18/19]-4, an anionic GCPII/PSMA inhibitor for image-guided intervention in prostate cancer, is described. [19F]4 is radiolabeled with a radiochemical yield that is >27% and a molar activity of 190 +/- 50 mCi/ptmol in a <1 h, one-step, aqueous isotopic exchange reaction. [F-19]-4 allows PSMA expression to be imaged by fluorescence (FL) and [18F]-PET. PC3-PIP (PSMA-positive, EC50 = 6.74 +/- 1.33 nM) cancers are specifically delineated in mice that bear 3 million (18 mg) PC3-PIP and PC3 (control, PSMA-negative) cells. Colocalization of [F-18/19]-4 PET, fluorescence, scintillated biodistribution, and PSMA expression are observed.