FK-506 is a potent, clinically-useful immunosuppressant in the same molecular class as cyclosporin A and rapamycin. Its mechanism of action involves the formation of a high affinity complex (Ki = 0.2 nM) with FK-506 Binding Protein 12 (FKBP12). This complex then inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T-cell activation.
Pharma Compounds & Neutraceuticals
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