1. A new ‘tac’ for childhood nephrotic syndrome
Brian Becknell, Larry A. Greenbaum, William E. Smoyer 
Kidney International 
Volume 82, Issue 10, Pages (November 2012)
DOI: /ki
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2. Figure 1
Mechanism of Cyclosporin A (CsA) versus tacrolimus. CsA binds to cyclophilin (CpN) in the cytoplasm, and the CsA–CpN complex associates with and blocks calcineurin (CaN) activity. CaN is a serine-threonine phosphatase and, when inhibited, is unable to dephosphorylate the nuclear factor of activated T cells (NF-AT). Thus, NF-AT is retained in the cytoplasm and is unable to activate transcriptional targets such as interleukin-2, which is necessary for T-cell activation. Tacrolimus (FK506) associates with FK506-binding protein (FKBP), and the FK506–FKBP complex binds to and blocks CaN activity. Thus, while CsA and FK506 bind to different proteins, their mechanism of T-cell inhibition is similar.
Kidney International  , DOI: ( /ki )
Copyright © 2012 International Society of Nephrology Terms and Conditions