FK-506

Potent immunosuppressant (as cyclosporin A and rapamycin) [1-3]. Suppresses proliferation of cytotoxic T cells and inhibits the production of T cell-derived mediators such as interleukin-2 (IL-2) [2, 4]. Forms a complex with FK-506 binding protein 12 (FKBP12). Inhibits the activity of the calcium/calmodulin-dependent protein phosphatase 2B (PP2B; calcineurin), leading to disruption of T cell activation [2, 4, 6, 7]. Prevents rejection of transplanted organs [3]. Anti-inflammatory compound in the treatment of several inflammatory skin diseases (e.g. atopic dermatitis) and with potential anti-rheumatic activity (rheumatoid arthritis) [5, 9]. Neuroprotective. Regulates nitric oxide neurotoxicity. Neurotransmitter. Ca2+ release compound [8]. NF-kappaB suppressor by induction of unfolded protein response (UPR) [11]. Anti-cancer compound. Apoptosis inducer [10, 12].