Calcineurin

Calcineurin

Tacrolimus (FK506, Axon 2263) is an immunosuppressive agent that suppresses both the immune response and apoptosis through inhibition of the phosphatase activity of calcineurin (calcium dependent serine/threonine protein phosphatase 2B; EC 3.1.3.16). FKBP12, the best-characterized member of the FKBP family of immunophilins, interacts with calcineurin only in the presence of Tacrolimus. Structural studies have shown that the FKBP12–FK506 complex binds \'snugly\' to calcineurin and blocks its interaction with substrates. Calcineurin, that is activated by Ca2+ and calmodulin, is implicated in both signal transduction events and apoptosis.

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More About Calcineurin

Tacrolimus (FK506, Axon 2263) is an immunosuppressive agent that suppresses both the immune response and apoptosis through inhibition of the phosphatase activity of calcineurin (calcium dependent serine/threonine protein phosphatase 2B; EC 3.1.3.16). FKBP12, the best-characterized member of the FKBP family of immunophilins, interacts with calcineurin only in the presence of Tacrolimus[1]. Structural studies have shown that the FKBP12–FK506 complex binds 'snugly' to calcineurin and blocks its interaction with substrates. Calcineurin, that is activated by Ca2+ and calmodulin, is implicated in both signal transduction events and apoptosis[2].

[1] C.B. Kang et al. FKBP family proteins: immunophilins with versatile biological functions. Neurosignals. 2008, 16, 318-325.
[2] M. Shirane et al. Inherent calcineurin inhibitor FKBP38 targets Bcl-2 to mitochondria and inhibits apoptosis. Nat. Cell Biol. 2003, 5, 28-37. 


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