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Literature summary for 3.1.3.16 extracted from

  • Erdmann, F.; Weiwad, M.; Kilka, S.; Karanik, M.; Paetzel, M.; Baumgrass, R.; Liebscher, J.; Fischer, G.
    The novel calcineurin inhibitor CN585 has potent immunosuppressive properties in stimulated human T cells (2010), J. Biol. Chem., 285, 1888-1898.
    View publication on PubMedView publication on EuropePMC
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Activating Compound

Activating Compound Comment Organism Structure
Calmodulin calcineurin is dependent on Ca2+/calmodulin Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
6-(3,4-dichloro-phenyl)-4-(N,N-dimethylaminoethylthio)-2-phenyl-pyrimidine i.e. CN585, noncompetitively and reversibly inhibits calcineurin activity, without affecting other Ser/Thr protein phosphatases or peptidyl prolyl cis/trans isomerases. The compound shows potent immunosuppressive effects by inhibiting NFAT nuclear translocation and transactivation, cytokine production, and T cell proliferation Homo sapiens
cyclosporin A the calcineurin inhibitor can block T-cell activation and is used as immunosuppressiv drug to prevent graft-versus-host reactions and autoimmune diseases Homo sapiens
FK506 the calcineurin inhibitor can block T-cell activation and is used as immunosuppressive drug to prevent graft-versus-host reactions and autoimmune diseases Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ calcineurin is dependent on Ca2+/calmodulin Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
T-lymphocyte
-
 Homo sapiens
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0038
-
 6-(3,4-dichloro-phenyl)-4-(N,N-dimethylaminoethylthio)-2-phenyl-pyrimidine
-
 Homo sapiens

General Information

General Information Comment Organism
physiological function the Ca2+/calmodulin-dependent protein phosphatase calcineurin is a key mediator in antigen-specific T-cell activation Homo sapiens