F-18-Positron Emitting/Trimethine Cyanine-Fluorescent Contrast for Image-Guided Prostate Cancer Management
JOURNAL OF MEDICINAL CHEMISTRY, vol.61, no.9, pp.4256-4262, 2018 (SCI-Expanded, Scopus)
- Publication Type: Article / Article
- Volume: 61 Issue: 9
- Publication Date: 2018
- Doi Number: 10.1021/acs.jmedchem.8b00240
- Journal Name: JOURNAL OF MEDICINAL CHEMISTRY
- Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Page Numbers: pp.4256-4262
- Istanbul University Affiliated: Yes
Abstract
[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.