Tacrolimus (also FK-506 or Fujimycin) is a macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to immunophilins. Tacrolimus is an immunosuppressive drug whose main use is after organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejection. It reduces peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP1A, creating a new complex. This complex inhibits calcineurin (Bierer et al. 1991) which inhibits T-lymphocyte signal transduction and IL-2 transcription (Kino et al. 1987, Ding et al. 2019).
Hashimoto, M, Hatanaka, H, Imanaka, H, Okuhara, M, Nishiyama, M, Aoki, H, Goto, T, Kohsaka, M, Kino, T
Ullah Khan, F, Shi, XJ, Zhong, HB, Ding, L, Li, XM, Chen, HJ, Yu, L, Zhou, LY, Zhu, XB, Nan, WH
Lane, WS, Schreiber, SL, Friedman, J, Liu, J, Farmer, JD, Weissman, I
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