2. Academic Validation
  3. A targeted low molecular weight near-infrared fluorescent probe for prostate cancer

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

  • Bioorg Med Chem Lett. 2010 Dec 1;20(23):7124-6. doi: 10.1016/j.bmcl.2010.09.057.
Tiancheng Liu 1,  Lisa Y Wu,  Mark R Hopkins,  Joseph K Choi,  Clifford E Berkman
Affiliations

Affiliation

  • 1 Department of Chemistry, Washington State University, Pullman, WA 99164, USA.
PMID: 20947349 DOI: 10.1016/j.bmcl.2010.09.057
Abstract

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.

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