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
Department of Medicinal Chemistry, Immunology and Inflammation, Merck Sharp & Dohme Research Laboratories, Rahway, NJ 07065.
Transplant Proc. 1988 Apr;20(2 Suppl 2):51-7.
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.
