Tacrolimus (FK-506 or Fujimycin) is used in an immunosuppressive agent for allogeneic organ transplant to reduce the activity of the patient’s immune system and lower the risk of organ rejection. It is also used in a topical preparation in the treatment of atopic dermatitis (eczema), severe refractory uveitis after bone marrow transplants, and for the skin condition vitiligo.
FK-506 is a macrolide compound isolated from the bacterium Streptomyces tsukubaensis. It tightly binds to FK506 binding protein (FKBP12). The complex reduces peptidyl-prolyl isomerase activity and inhibits calcineurin by downregulating Ca2+ concentration in T-cells. Nuclear factor of activated T-cells (NFAT) then is not able to move into the nucleus of the T-cell and is unable to increase activity of genes coding for IL-2 and related cytokines.
It is reported that FK-506 has been shown to have an impact on cancer signaling pathways such as MAPK and the p53 pathway. NFAT inhibition via FK506 is shown to affect cancer cell growth, apoptosis, migration, and invasion in prostate cancer.
• Immunosuppressive agent
• Calcineurin inhibitor
• T cell proliferation blocker
Not for human therapeutic use or for medicinal purposes. For research applications only.
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