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Literature summary for 3.1.3.16 extracted from

  • Smit, N.P.; Van Rossum, H.H.; Romijn, F.P.; Sellar, K.J.; Breetveld, M.; Gibbs, S.; Van Pelt, J.
    Calcineurin activity and inhibition in skin and (epi)dermal cell cultures (2008), J. Invest. Dermatol., 128, 1686-1690.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
cyclosporin A an immunosuppressive drug. 25% inhibition in keratinocytes at 831 nM, 49% in melanocytes Homo sapiens
EGTA
-
Homo sapiens
additional information calcineurin inhibition in fibroblasts and keratinocytes may be of influence on the overall functioning of the skin immune system. No inhibition of calcineurin by okadaic acid Homo sapiens
pimecrolimus an immunosuppressive drug Homo sapiens
tacrolimus an immunosuppressive drug. 89% inhibition in keratinocytes at 124 nM, 74% in fibroblasts, and 75% in melanocytes Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ calcium-dependent protein phosphatase 2B Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood
-
Homo sapiens
-
fibroblast
-
Homo sapiens
-
fibroblast cell line F0502 cell Homo sapiens
-
fibroblast cell line F0503 cell Homo sapiens
-
keratinocyte
-
Homo sapiens
-
melanocyte
-
Homo sapiens
-
skin
-
Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.0038 0.0077 keratinoyctes Homo sapiens
0.0085 0.0127 fibroblasts Homo sapiens

Synonyms

Synonyms Comment Organism
calcineurin
-
Homo sapiens
calcium-dependent protein phosphatase 2B
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000004 0.0000013 in fibroblasts Homo sapiens tacrolimus
0.000002 0.0000027 in fibroblasts Homo sapiens cyclosporin A
0.000006 0.0000201 in fibroblasts Homo sapiens pimecrolimus

General Information

General Information Comment Organism
malfunction calcineurin inhibition in fibroblasts and keratinocytes may be of influence on the overall functioning of the skin immune system Homo sapiens