The mechanism of action of tacrolimus (IMAGE)
Caption
Tacrolimus binds to the intracellular protein FKBP12, forming a complex that specifically inhibits calcineurin, a protein phosphatase essential for activating the transcription factor NFAT. By preventing dephosphorylation, this inhibition blocks the translocation of active NFAT to the nucleus, thereby suppressing IL-2 gene transcription and ultimately inhibiting T cell activation. This leads to a subsequent reduction in cytokine production. (Created with image.medpeer.cn). NFAT, nuclear factor of activated T cells; IL-2, interleukin-2.
Credit
Huaie Liu
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