Abstract
The photoaffinity labelling technique was applied to the study of receptors for α-melanocyte-stimulating hormone (α-MSH; α-melanotropin) on mouse and human melanoma cells as well as on Xenopus and Anolis melanophores. Twenty different α-MSH analogues containing one, two or three photolabels were synthesized and tested as photoprobes. A highly potent nitrene-generating azidophenyl compound, monoiodinated [4-Nle, 7- D-Phe, 9-Trp(Naps)]-α-MSH, was most suitable for the biochemical analysis of MSH receptors on melanoma cells whereas the physiological effects following photolabelling of intact cultured cells were best studied by using carbene-generating phenyldiazirine α-MSH analogues. Covalent linkage of α-MSH to its receptor on both melanoma cells and melanophores produced a long-lasting receptor stimulation. This irreversible agonism served as a new tool for the analysis of signal transduction mechanisms. The biochemical characterization of the covalent α-MSH-receptor complex of melanoma cells revealed a 45 kDa membrane glycoprotein, probably containing a relatively high content of sialic acid, thus explaining the acidic pi (4.7) of this receptor.
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© 1989 Kluwer Academic Publishers
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Eberle, A.N., Solca, F., Siegrist, W., Scimonelli, T., Girard, J., de Graan, P.N.E. (1989). Photoaffinity Labelling of Receptors for Melanocyte-Stimulating Hormone. In: Nielsen, P.E. (eds) Photochemical Probes in Biochemistry. NATO ASI Series, vol 272. Springer, Dordrecht. https://doi.org/10.1007/978-94-009-0925-0_6
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DOI: https://doi.org/10.1007/978-94-009-0925-0_6
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