RELATIONSHIPS AMONG RETINOID STRUCTURE, INHIBITION OF GROWTH, AND CELLULAR RETINOIC ACID-BINDING PROTEIN IN CULTURED S91 MELANOMA-CELLS

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  • 1 January 1980
    • journal article
    • research article
    • Vol. 40  (4) , 1097-1102
Abstract
S-91 [mouse] melanoma cells, which are sensitive to retinoic acid and contain a cellular retinoic acid-binding protein (RABP), were used to study the possible correlation between the capacities of various retinoids to inhibit cell proliferation and to bind to the RABP. Each of 27 different retinoids was evaluated for growth-inhibitory activity by exposing S-91 melanoma cells to various retinoid concentrations between 1 nM and 10 .mu.M. The ability of 17 of these retinoids to compete with [3H]retinoic acid for binding to RABP was determined. In addition to retinoic acid, many retinoids are capable of inhibiting the proliferation of S-91 melanoma cells, although some are considerably less active. A positive correlation was found between the abilities of retinoids possessing a free carboxyl group at carbon 15 to inhibit cell proliferation and to bind to RABP. The structure-activity relationships established with the S-91 cells are compared with previous reports on the biological activities of various retinoids in other systems.