FKBP1A binds tacrolimus

Stable Identifier
R-HSA-9690461
Type
Reaction [binding]
Species
Homo sapiens
Compartment
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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).

Literature References
PubMed ID Title Journal Year
2445721 FK-506, a novel immunosuppressant isolated from a Streptomyces. I. Fermentation, isolation, and physico-chemical and biological characteristics

Hashimoto, M, Hatanaka, H, Imanaka, H, Okuhara, M, Nishiyama, M, Aoki, H, Goto, T, Kohsaka, M, Kino, T

J. Antibiot. 1987
30294901 Rapamycin and FK506 derivative TH2849 could ameliorate neurodegenerative diseases through autophagy with low immunosuppressive effect

Ullah Khan, F, Shi, XJ, Zhong, HB, Ding, L, Li, XM, Chen, HJ, Yu, L, Zhou, LY, Zhu, XB, Nan, WH

CNS Neurosci Ther 2019
1715244 Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes

Lane, WS, Schreiber, SL, Friedman, J, Liu, J, Farmer, JD, Weissman, I

Cell 1991
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