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A study of the correlation between cyclophilin binding and in vitro immunosuppressive activity of cyclosporine a and analogues

Durette, P.L.; Boger, J.; Dumont, F.; Firestone, R.; Frankshun, R.A.; Koprak, S.L.; Lin, C.S.; Melino, M.R.; Pessolano, A.A.; Pisano, J.

Transplantation Proceedings 20(2 Suppl 2: 51-57

1988

ISSN/ISBN: 0041-1345
PMID: 2966482
Document Number: 310156
In order to establish whether CyP is the pharmacologically relevant CsA receptor, the CyP binding v immunosuppressive activity was measured for an extensive, structurally varied group of CsA analogues. Overall, CyP binding was found to parallel immunosuppressive activity. Other than MeAla6-CsA, the few exceptions to the correlation could be ascribed to cellular metabolism. These results strongly implicate CyP or a related protein in the mechanism of action of cyclosporine.

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