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- W2887123655 abstract "The bombesin (BBN) antagonist binds with high affinity to the gastrin releasing peptide receptor (GRPr), a receptor overexpressed on many human cancers. We present an investigation employing BBN antagonist for highly specific near-infrared fluorescence (NIRF) imaging of GRPr-positive tumors. Nine NIRF-dye labeled BBN antagonists with differing linkers and dyes were synthesized and characterized to screen for the optimal agent. Three novel agents, AF750-G-pip-Sta-BBN (1), AF750-GSG-Sta-BBN (2), and AF750-6Ahx-Sta-BBN (3), exhibited an excellent binding-specificity and affinity to human PC-3 prostate cancer cells in vitro, and a remarkable in vivo tumor-selectivity and NIRF imaging sensitivity in PC-3 tumor-bearing mice. Compound 1 showed the fastest, and 3, the slowest, pharmacokinetics on the tumor sites. Despite of high tumor uptake, 2 had a low pancreas uptake distinct from 1 and 3 at 0.44 nmol dose. This difference was attributed to the inherent linker properties such as the hydrophilicity, polarity, and charge." @default.
- W2887123655 created "2018-08-22" @default.
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- W2887123655 date "2018-08-15" @default.
- W2887123655 modified "2023-09-23" @default.
- W2887123655 title "Design, Synthesis, and in Vitro and in Vivo Evaluation of High Affinity and Specificity Near-Infrared Fluorescent Bombesin Antagonists for Tumor Imaging" @default.
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- W2887123655 doi "https://doi.org/10.1021/acs.jmedchem.8b00614" @default.
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