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Molecular Heterogeneity of Somatostatin Analogue BIM-23014C Receptors in Human Breast Carcinoma Cells Using the Chemical Cross-Linking Assay¹

Institut d'Oncologie Cellulaire et Moléculaire Humaine, 129 route de Stalingrad, Bobigny, 93000, France [G. P., N. V., W. G., R. B., A. S.]; Laboratoire de Biologie des tumeurs, 2, bis Boulevard Tonnelle, 37032, Tours, France [M. L.]; Ipsen-Biotech, 15, rue Cambronne, 75737, Paris, France [F. T.]; and Biomeasure, Inc., 11-15 "E" Avenue, Hopkinton, Massachusetts [A. B.]

Distinct proteins complexed with somatostatin and the somatostatin analogue BIM-23014C were revealed in human breast cancer cells using the cross-linking assay. One BIM-23014C-specific complex (M_r 57,000) was observed in MCF-7 (monolayer, nodule, and tumor) and T47D. Growth inhibition of MCF-7 tumor xenografts by BIM-23014C was dose related in the 6-day subrenal capsule assay. Three complexes (M_r 27,000, 42,000, and 57,000) were detected in MDA-MB-231, and no complex was visible in HBL-100. No correlation was found between receptors for BIM-23014C and epidermal growth factor in these lines. Twenty-seven of 30 human breast tumors (90%) had at least one BIM-23014C receptor. Sixteen had three complexes (M_r, 27,000, 42,000, and 57,000). Six had the two complexes (M_r 27,000 and 57,000), two had M_r 42,000 and 57,000 complexes, two had just the M_r 27,000 complex, and one had just the M_r 42,000 complex. The presence of the three BIM-23014C receptors was positively correlated (P < 0.05) to the low amount of sex steroid receptors (<20 fmol/mg) [seven of eight (estrogen receptor negative, progesterone receptor negative) versus four of 14 (estrogen receptor positive, progesterone receptor positive)]. Another positive correlation was established between the absence of progesterone receptors and the presence of these three complexes [12 of 16 (progesterone receptor negative) versus four of 14 (progesterone receptor positive)]. This high percentage of BIM-23014C receptor-positive biopsies and its inhibitory activity would support its clinical potential for the treatment of breast cancer.

¹ This work was supported by grants from the Association de Recherche sur le Cancer (ARC), Ipsen-Biotech, and CNRS.

² To whom requests for reprints should be addressed.

Received 7/ 9/91. Accepted 11/20/91.

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