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₂ Receptors as Potential Biomarkers of Proliferation in Breast Cancer¹

Departments of Radiology [R. H. M., C. R. S., B. R. W.], Radiation Oncology [I. A., K. T. W.], and Physiology and Pharmacology [R. H. M., S. R. C.], Bowman Gray School of Medicine, Winston-Salem, North Carolina 27157

₁ and ₂ receptors have been shown to exist in a number of rodent and human tumor cell lines. Although their expression is heterogeneous and their function is unknown, receptors have been proposed as potential targets for diagnostic tumor-imaging agents. In this study, the density of ₂ receptors in proliferative (P) and quiescent (Q) cells of the mouse mammary adenocarcinoma, line 66, was examined. Scatchard analyses of ₂ receptors were performed on membrane preparations of 66 P cells from 3-day cultures and 66 Q cells from 7-, 10-, and 12-day cultures. The Scatchard studies revealed that 66 P cells had 10 times more ₂ receptors/cell than the 66 Q cells from 10-day cultures. Although >97% of the cells were quiescent after 7 days in culture, the maximum differential in the ₂ expression between 66 P and 66 Q cells was not attained until these cells had been in culture for 10 days. These data suggest that ligands labeled with positron-emitting or single photon-emitting radionuclides, which selectively bind ₂ receptors, have the potential to noninvasively assess the proliferative status of human breast tumors.

¹ This work was supported by NIH Grants NS-31907 (to R. H. M.) and CA-45156 (to K. T. W.).

² To whom requests for reprints should be addressed, at Department of Radiation Oncology, Bowman Gray School of Medicine, Medical Center Blvd., Winston-Salem, NC 27157.

Received 8/13/96. Accepted 11/15/96.

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