Journal article
A targeted low molecular weight near-infrared fluorescent probe for prostate cancer
Bioorganic & medicinal chemistry letters, Vol.20(23), pp.7124-7126
2010
Handle:
https://hdl.handle.net/2376/113402
PMCID: PMC3201797
PMID: 20947349
Abstract
A novel near-infrared imaging probe was synthesized, which exhibited potent PSMA inhibitory activity (IC
50
=
0.55
nM) and PSMA-targeted imaging of prostate cancer cells in vitro.
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.
Metrics
12 Record Views
Details
- Title
- A targeted low molecular weight near-infrared fluorescent probe for prostate cancer
- Creators
- Tiancheng Liu - Department of Chemistry, Washington State University, Pullman, WA 99164, USALisa Y Wu - Department of Chemistry, Washington State University, Pullman, WA 99164, USAMark R Hopkins - Department of Chemistry, Washington State University, Pullman, WA 99164, USAJoseph K Choi - Department of Chemistry, Washington State University, Pullman, WA 99164, USAClifford E Berkman - Department of Chemistry, Washington State University, Pullman, WA 99164, USA
- Publication Details
- Bioorganic & medicinal chemistry letters, Vol.20(23), pp.7124-7126
- Academic Unit
- Chemistry, Department of
- Publisher
- Elsevier Ltd
- Identifiers
- 99900548132001842
- Language
- English
- Resource Type
- Journal article