Drug name: Cyclosporine A


Related CSCTT Targets

ABCG2 [ref.1]Q9UNQ0
ABCB1 [ref.2]P08183

cyclosporine A, CyA

Cas.no PubChem ID
59865-13-3 5284373
Known Target
Calcium signal-modulating cyclophilin ligandP49069
Calcineurin subunit B type 2Q96LZ3
Peptidyl-prolyl cis-trans isomerase AP62937
Peptidyl-prolyl cis-trans isomerase F, mitochondrialP30405
Introduction
A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. Cyclosporine is produced as a metabolite by the fungus species Cordyceps militaris. Cyclosporin A inhibits calcineurin with IC50 of 7 nM, then blocks the nuclear translocation of NF-AT. Cyclosporin A also affects mitochondria by preventing the MTP (mitochondrial permeability transition pore) from opening with an IC50 of 39 nM.

cyclosporine A, CyA-Structure

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Reference

  • [1] Salinomycin overcomes ABC transporter-mediated multidrug and apoptosis resistance in human leukemia stem cell-like KG-1a cells. Fuchs, D., et al. (2010).Biochem Biophys Res Commun. 394(4):1098-104.
    20350531. [ 20350531 ]
  • [2] Reversing paclitaxel resistance in ovarian cancer cells via inhibition of the ABCB1 expressing side population. Eyre, R., et al. (2014).Tumour Biol.35(10):9879-92.
    24993095. [ 24993095 ]

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