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Clinical Chemistry 39: 122-125, 1993;
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Clinical Chemistry, Vol 39, 122-125, Copyright © 1993 by American Association for Clinical Chemistry

Cyclosporin G and metabolite binding to cyclophilin and a 50-kDa binding protein related to in vitro immunosuppression

JG Donnelly, Y Chen, RW Yatscoff, KR Copeland, EW Palaszynski and SJ Soldin
Department of Biology, Catholic University of America, Washington, DC.

Seven purified metabolites of cyclosporin G (CsG) were studied for binding to cyclophilin and a 50-kDa binding protein (50-kDa BP). The ratios of the metabolite dissociation constants with respect to CsG were compared with in vitro immunosuppression by using the primary mixed lymphocyte suppression assay. The immunosuppressive potency ratio of the parent compounds, both cyclosporin A (CsA) and CsG, compared favorably with the drug dissociation constants for cyclophilin and the 50-kDa BP. Three of the seven metabolites had comparable binding and potency ratios for the 50-kDa BP. In contrast, none of the seven metabolites appreciably bound to cyclophilin in the concentration range tested.




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Copyright © 1993 by the American Association for Clinical Chemistry.