A targeted low molecular weight near-infrared fluorescent probe for prostate cancer

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:20

Article

Liu, Tiancheng¹  Wu, Lisa Y.¹  Hopkins, Mark R.¹  Choi, Joseph K.¹  Berkman, Clifford E.^1,2 

[1] Washington State Univ, Dept Chem, Pullman, WA 99164 USA

[2] Canc Targeted Technol, Woodinville, WA 98072 USA

关键词: Tumor-targeting;    Near-infrared imaging;    PSMA;    Cy5.5 conjugate;   

DOI  :  10.1016/j.bmcl.2010.09.057

来源: Elsevier

【 摘 要 】

Prostate-specific membrane antigen (PSMA) remains an active target for imaging and therapeutic applications for prostate cancer. Although radionuclide-based imaging is generally more sensitive and also has been deeply explored, near-infrared fluorescence imaging agents are simple to prepare and compatible with long-term storage conditions. In the present study, a near-infrared fluorescent imaging probe (Cy5.5-CTT-54.2) has been developed by chemical conjugation of Cy5.5N-hydroxysuccinimide ester (Cy5.5-NHS) with a potent PSMA inhibitor CTT-54.2 (IC(50) = 144 nM). The probe displays a highly potency (IC(50) = 0.55 nM) against PSMA and has demonstrated successful application for specifically labeling PSMA-positive prostate cancer cells in both two and three-dimensional cell culture conditions. These results suggest that the potent, near-infrared Cy5.5-PSMA inhibitor conjugate may be useful for the detection of prostate tumor cells by optical in vivo imaging. (C) 2010 Elsevier Ltd. All rights reserved.

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