| Literature DB >> 29676909 |
Harikrishna Kommidi1, Hua Guo1, Fuad Nurili2, Yogindra Vedvyas1, Moonsoo M Jin1, Timothy D McClure3, Behfar Ehdaie4, Haluk B Sayman5, Oguz Akin2, Omer Aras2, Richard Ting1.
Abstract
[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.Entities:
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Year: 2018 PMID: 29676909 PMCID: PMC6263152 DOI: 10.1021/acs.jmedchem.8b00240
Source DB: PubMed Journal: J Med Chem ISSN: 0022-2623 Impact factor: 7.446