The mechanism of action of cyclosporin A and FK506
S Ho, N Clipstone, L Timmermann, J Northrop… - Clinical immunology and …, 1996 - Elsevier
The immunosuppressants cyclosporin A (CsA), FK506, and rapamycin suppress the immune
response by inhibiting evolutionary conserved signal transduction pathways. CsA, FK506,
and rapamycin bind to their intracellular receptors, immunophilins, creating composite
surfaces that block the activity of specific targets. For CsA/cyclophilin and FK506/FKBP the
target is calcineurin. Because of the large surface area of interaction of the drug–
immunophilin complex with calcineurin, FK506 and CsA have a specificity for their biologic …
response by inhibiting evolutionary conserved signal transduction pathways. CsA, FK506,
and rapamycin bind to their intracellular receptors, immunophilins, creating composite
surfaces that block the activity of specific targets. For CsA/cyclophilin and FK506/FKBP the
target is calcineurin. Because of the large surface area of interaction of the drug–
immunophilin complex with calcineurin, FK506 and CsA have a specificity for their biologic …