Abstract
A variety of normal and transformed avian and mammalian cells and tissues contain high affinity specific receptors on their membranes which interact with biologically active phorbol and ingenol esters in a reversible and saturable manner. The binding of labelled phorbol-12,13-dibutyrate (PDBu) to live or glutaraldehyde-fixed cells is dose-, time- and temperature-dependent. Those phorbol or ingenol esters which stimulate cell growth in culture and have tumour-promoting activity in vivo inhibit the binding of labelled PDBu, while the biologically inactive derivatives fail to do so. Other non-diterpene tumour-promoting agents, epidermal growth factor (EGF), retinoids and prostaglandins do not compete for the binding of labelled PDBu to its specific membrane receptors.
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References
Van Duuren, B. L. Prog. exp. Tumour Res. 11, 31 (1969).
Hecker, E. Meth. Cancer Res. 6, 439 (1971).
Boutwell, R. K. Crit. Rev. Tox. 2, 419 (1974).
Slaga, T. J., Sivak, A. & Boutwell, R. K. (eds) Mechanisms of Tumor Promotion and Cocarcinogenesis (Raven, New York, 1978).
Sivak, A. Biochim. biophys. Acta 560, 67 (1979).
Hecker, E. & Schmidt, R. Fortschr. Chem. org. Natstoffe 31, 377 (1974).
Raick, A. N. Cancer Res. 32, 269 (1973).
Paul, D. L. & Hecker, E. J. Krebforshch. 73, 149 (1969).
Balmain, A., Alonso, A. & Fisher, S. Cancer Res. 37, 1548 (1977).
Mufson, R. A., Astrup, E. G., Simsiman, R. C. & Boutwell, R. K. Proc. natn. Acad. Sci. U.S.A. 74, 657 (1977).
Mufson, R. A., Simsiman, R. C. & Boutwell, R. K. Cancer Res. 37, 665 (1977).
Murray, A. W. & Froscio, M. Cancer Res. 37, 1360 (1977).
O'Brien, T. G., Simsiman, R. C. & Boutwell, R. K. Cancer Res. 35, 2426 (1975).
Balmain, A. J. invest. Derm. 67, 246 (1976).
Whitfield, J. F., McManus, J. P. & Gillan, D. J. J. cell. Physiol. 82, 151 (1973).
Boyton, A. L., Whitfield, J. F. & Issacs, R. J. J. cell. Physiol. 87, 25 (1976).
Sivak, A. J. cell. Physiol. 80, 167 (1972).
Wigler, M. & Weinstein, I. B. Nature 259, 232 (1976).
Yuspa, S. H. et al. Nature 262, 402 (1976).
Blumberg, P. M., Driedger, P. E. & Rossow, P. W. Nature 264, 446 (1976).
Wenner, C., Hackney, J., Kimelberg, H. & Mayhew, E. Cancer Res. 34, 1732 (1973).
Ohuchi, K. & Levine, L. J. biol. Chem. 13, 4783 (1978).
Sivak, A., Mossman, B. F. & Van Duuren, B. L. Communications 46, 605 (1972).
Sivak, A. & Van Duuren, B. L. Chem. biol. Interactions 3, 401 (1971).
Suss, R., Kinzel, V. & Kreebier, G. Experientia 27, 46 (1971).
Rohrschneider, L. R., O'Brien, D. H. & Boutwell, R. K. Biochim. biophys. Acta 280, 57 (1972).
Lee, L. S. & Weinstein, I. B. Science 202, 313 (1978).
Shoyab, M., De Larco, J. E. & Todaro, G. J. Nature 279, 387 (1979).
Brown, K. D., Dicker, P. & Rozengurt, E. Biochem. biophys. Res. Commun. 86, 1037 (1979).
Cohen, S. & Taylor, J. M. Recent Prog. Hormone Res. 30, 533 (1974).
De Larco, J. E. & Todaro, G. J. Proc. natn. Acad. Sci. U.S.A. 75, 4001 (1978).
Lee, L. S. & Weinstein, I. B. J. Envir. Path. Toxic. 1, 627 (1978).
Kubinyi, H. Arzneim Forest 26, 1991 (1976).
Driedger, P. E. & Blumberg, P. M. Proc. natn. Acad. Sci. U.S.A. 77, 567 (1980).
Henderson, I. C., Lieber, M. M. & Todaro, G. J. Virology 60, 282 (1974).
Aaronson, S. A. & Todaro, G. J. J. cell. Physiol. 72, 141 (1968).
Todaro, G. J., De Larco, J. E. & Cohen, S. Nature 264, 26 (1976).
Pruss, R. W. & Herschmann, H. R. Proc. natn. Acad. Sci. U.S.A. 74, 3918 (1977).
Rohrschneider, L. R. & Boutwell, R. K. Nature new Biol. 243, 212 (1973).
Goldstein, A., Cox, B. M., Gentleman, S., Lowney, L. I. & Cheung, A. L. Ann. N.Y. Acad. Sci. 297, 108 (1978).
Sharon, N. & Lis, H. Sicience 177, 949 (1972).
Cheng, C. Y. & Prusoff, W. H. Biochem. Pharmac. 22, 3099 (1973).
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Shoyab, M., Todaro, G. Specific high affinity cell membrane receptors for biologically active phorbol and ingenol esters. Nature 288, 451–455 (1980). https://doi.org/10.1038/288451a0
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DOI: https://doi.org/10.1038/288451a0
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