Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary 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

Activating Compound

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.3.16 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
3.1.3.16 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
3.1.3.16 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

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

Organism

EC Number Organism UniProt Comment Textmining
3.1.3.16 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.3.16 T-lymphocyte
-
 Homo sapiens
-

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.1.3.16 0.0038
-
 6-(3,4-dichloro-phenyl)-4-(N,N-dimethylaminoethylthio)-2-phenyl-pyrimidine
-
 Homo sapiens

General Information

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