Cyclosporin A

Cyclosporin A is a hydrophobic cyclic peptide isolated from Tolypocladium inflatum and is a potent immunosuppressant and antifungal compound. It acts via its ability to binds a family of intracellular proteins, the cyclophilins (intracellular peptidyl-prolyl cis-trans isomerases), which are abundant, ubiquitous, highly conserved, and found in multiple forms in different intracellular compartments.1 In yeast, Cyclophilin A, an 18-kDa cytoplasmic protein, mediates Cyclosporin A actions.

The immunosuppressive action of Cyclosporin A is mediated by the complex Cyclosporin A-Cyclophilin that specifically inhibits the Ca²⁺ calmodulin-dependent serine-threonine-protein phosphatase-2B (Calcineurin). This in turn inhiibts the Calcineurin and promotes dephosphorylation of transcription factor NF-AT and T-cell activation. In vivo, Cyclosporin A - induced hypertension involves, the attenuation of endothelium-derived NO production through inhibition of Calcineurin-sensitive pathway regulating eNOS dephosphorylation.

Cyclosporin A has been shown to alter cell proliferation in different systems. For hematopoietic progenitor stem and progenitor cells, smooth muscle cells, and hepatocytes, it serves as an inducer of cell proliferation or a tumor promoting effector. On the other hand, growth of interleukin-3-dependent mast cells, human lung-cancer cells, tubular kidney cells, cultured pituitary cells, T-cells, and keratinocytes were inhibited by Cyclosporin A. Moreover, Cyclosporin A has been observed in vitro and in vivo as an antimalarial agent, but the exact mechanism is not yet clear. Cell Signaling Activators and Inhibitors; Immunosuppressants. Protein Phosphatase Inhibitors; Protein Phosphatase Inhibitors (PP-2B (Calcineurin))

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