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Characterization of Receptors for -Melanocyte-stimulating Hormone on Human Melanoma Cells¹

Laboratory of Endocrinology, Department of Research, University Hospital and University Children's Hospital, CH-4031 Basel, Switzerland [W. S., F. S., S. S., J. G., A. N. E.] and Ludwig Institute for Cancer Research, CH-1066 Epalinges/Lausanne, Switzerland [L. G., S. C.]

Receptors for -melanocyte-stimulating hormone (-MSH) on human malignant melanoma cell lines were investigated with a specific binding assay and characterized with structural analogues of -MSH and adrenocorticotropic hormone and by photoaffinity cross-linking of the hormone-receptor complex. Specific binding of high-performance liquid chromatography-purified, monoiodinated -MSH in the presence of 1 mM 1,10-phenanthroline as protease inhibitor was highest after a 2-h incubation at 37°C. The nonspecific binding was <20% and dissociation of the ligand-receptor complex was relatively slow. Ten out of 12 human cell lines showed specific binding sites for -MSH with K_D values ranging from 0.195 to 2.87 nM and the sites/cell being 400 to 1600. Virtually identical results were obtained in an assay where the cells remained attached to the culture dishes during the entire experiment. The study of hormone analogues with the D10 cell line showed that oxidized -MSH had an 40-fold lower affinity than -MSH whereas [Nle⁴,D-Phe⁷]--MSH displayed a threefold and the adrenocorticotropic hormone fragments (1–17) and (1–24) a 20- and 8-fold higher affinity. Cross-linking of the -MSH-receptor complex of three cell lines using monoiodinated [Nle⁴,D-Phe⁷,Trp(2-nitro-4-azidophenylsulfenyl)⁹]--MSH as photoaffinity label revealed a major M_r 45,000 protein band on sodium dodecyl sulfate-polyacrylamide gels, analogous to the MSH receptor of mouse B16 melanoma cells.

¹ This work was supported by the Swiss National Science Foundation (Grant 3.287-0.85) and the Swiss and Basel Cancer Leagues (Grant For. 314.85).

² To whom requests for reprints should be addressed, at the Department of Research (ZLF), University Hospital, Hebelstrasse 20, CH-4031 Basel, Switzerland.

Received 5/24/88. Revised 7/19/89. Accepted 8/18/89.

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