Director:
Zsolt Szabo, M.D., Ph.D.
Brief Discription and findings:
Cancer cell lines with high and low endothelin type A receptor (ETAR) expression were implanted into SCID mice. Our study represents the first attempt to develop a new technology for in vivo imaging of the ETAR in cancer. Preliminary in vivo imaging studies of cancer xenografts were done on both SCID and nude mice. Correlative immunostaining and RT-PCR studies were performed on tissue samples harvested at the end of the experiment to determine whether the new radioligand is a reliable marker of the ETAR. Preliminary results demonstrate our ability to carry out PET/CT experiments to evaluate in vivo tumor uptake of the PET radioligand. We recently developed [11C]ABT-627 as a tracer for PET imaging of the ETAR, but in mice and rats it was rapidly metabolized and resulted in poor target-to-nontarget (specifically myocardium-to-lung) binding ratio. In order to select the best radioligand for further studies, we have the NIH R21 grant extended that was funded to radiolabel and evaluate BMS-207940.
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