A targeted low molecular weight near-infrared fluorescent probe for prostate cancer.
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.
Department of Chemistry, Washington State University, Pullman, WA 99164, USA.
Tiancheng
T
Liu
Lisa Y
LY
Wu
Mark R
MR
Hopkins
Joseph K
JK
Choi
Clifford E
CE
Berkman
D002232:Carbocyanines; D005456:Fluorescent Dyes; D006801:Humans; D007259:Infrared Rays; D008297:Male; D008970:Molecular Weight; D017430:Prostate-Specific Antigen / Q000037:antagonists & inhibitors*; D011471:Prostatic Neoplasms / Q000175:diagnosis*; D014407:Tumor Cells, Cultured
C098793:CY5.5 cyanine dye; D002232:Carbocyanines; D005456:Fluorescent Dyes; D017430:Prostate-Specific Antigen