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Calcineurin is a calcium and calmodulin-dependent serine/threonine protein phosphatase that plays a crucial role in various cellular processes, most notably in T cell activation. It is a heterodimer composed of a catalytic subunit (calcineurin A) and a regulatory subunit (calcineurin B). Its activity is inhibited by the formation of a complex with cyclosporin A or tacrolimus bound to their respective immunophilins, cyclophilin and FKBP. This inhibition prevents NFAT dephosphorylation and the subsequent transcription of genes involved in T cell activation, making it a key target for immunosuppressant drugs.
Inhibition of calcineurin phosphatase activity via formation of a ternary complex with an immunophilin-drug complex, preventing NFAT dephosphorylation and subsequent gene transcription.
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