TY - JOUR
T1 - 18F-Positron Emitting/Trimethine Cyanine-Fluorescent Contrast for Image-Guided Prostate Cancer Management
AU - Kommidi, Harikrishna
AU - Guo, Hua
AU - Nurili, Fuad
AU - Vedvyas, Yogindra
AU - Jin, Moonsoo M.
AU - McClure, Timothy D.
AU - Ehdaie, Behfar
AU - Sayman, Haluk B.
AU - Akin, Oguz
AU - Aras, Omer
AU - Ting, Richard
N1 - Funding Information:
The project was supported by National Institutes of Health Grants EB013904, R01CA178007, and P30CA008748.
Publisher Copyright:
© 2018 American Chemical Society.
PY - 2018/5/10
Y1 - 2018/5/10
N2 - [18/19F]-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/μmol in a <1 h, one-step, aqueous isotopic exchange reaction. [19F]-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 [18/19F]-4 PET, fluorescence, scintillated biodistribution, and PSMA expression are observed.
AB - [18/19F]-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/μmol in a <1 h, one-step, aqueous isotopic exchange reaction. [19F]-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 [18/19F]-4 PET, fluorescence, scintillated biodistribution, and PSMA expression are observed.
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U2 - 10.1021/acs.jmedchem.8b00240
DO - 10.1021/acs.jmedchem.8b00240
M3 - Article
C2 - 29676909
AN - SCOPUS:85046786143
VL - 61
SP - 4256
EP - 4262
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 9
ER -