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Literature summary for 1.1.1.146 extracted from

  • Inderbinen, S.G.; Zogg, M.; Kley, M.; Smiesko, M.; Odermatt, A.
    Species-specific differences in the inhibition of 11beta-hydroxysteroid dehydrogenase 2 by itraconazole and posaconazole (2021), Toxicol. Appl. Pharmacol., 412, 115387 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
hydroxyitraconazole
-
Danio rerio
hydroxyitraconazole
-
Homo sapiens
hydroxyitraconazole
-
Mus musculus
hydroxyitraconazole
-
Rattus norvegicus
itraconazole
-
Danio rerio
itraconazole
-
Homo sapiens
itraconazole 95% residual activity at 0.03 mM Mus musculus
itraconazole
-
Rattus norvegicus
posaconazole
-
Danio rerio
posaconazole
-
Homo sapiens
posaconazole
-
Mus musculus
posaconazole
-
Rattus norvegicus

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ 1 mM used in assay conditions Homo sapiens
Mg2+ 1 mM used in assay conditions Mus musculus
Mg2+ 1 mM used in assay conditions Danio rerio
Mg2+ 1 mM used in assay conditions Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
cortisone + NADH + H+ Homo sapiens
-
cortisol + NAD+
-
?
cortisone + NADH + H+ Mus musculus
-
cortisol + NAD+
-
?
cortisone + NADH + H+ Danio rerio
-
cortisol + NAD+
-
?
cortisone + NADH + H+ Rattus norvegicus
-
cortisol + NAD+
-
?

Organism

Organism UniProt Comment Textmining
Danio rerio Q6P0H9
-
-
Homo sapiens P80365
-
-
Mus musculus P51661
-
-
Rattus norvegicus P50233
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
cortisone + NADH + H+
-
Homo sapiens cortisol + NAD+
-
?
cortisone + NADH + H+
-
Mus musculus cortisol + NAD+
-
?
cortisone + NADH + H+
-
Danio rerio cortisol + NAD+
-
?
cortisone + NADH + H+
-
Rattus norvegicus cortisol + NAD+
-
?

Synonyms

Synonyms Comment Organism
11beta-HSD2
-
Homo sapiens
11beta-HSD2
-
Mus musculus
11beta-HSD2
-
Danio rerio
11beta-HSD2
-
Rattus norvegicus
11beta-hydroxysteroid dehydrogenase 2
-
Homo sapiens
11beta-hydroxysteroid dehydrogenase 2
-
Mus musculus
11beta-hydroxysteroid dehydrogenase 2
-
Danio rerio
11beta-hydroxysteroid dehydrogenase 2
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000122
-
at pH 7.4 and 37°C Homo sapiens itraconazole
0.000187
-
at pH 7.4 and 37°C Homo sapiens hydroxyitraconazole
0.000512
-
at pH 7.4 and 37°C Homo sapiens posaconazole
0.000729
-
at pH 7.4 and 37°C Rattus norvegicus itraconazole
0.000835
-
at pH 7.4 and 37°C Rattus norvegicus posaconazole
0.00113
-
at pH 7.4 and 37°C Rattus norvegicus hydroxyitraconazole
0.00748
-
at pH 7.4 and 37°C Danio rerio hydroxyitraconazole
0.008212
-
at pH 7.4 and 37°C Mus musculus posaconazole
0.0098
-
at pH 7.4 and 37°C Danio rerio itraconazole
0.0101
-
at pH 7.4 and 37°C Danio rerio posaconazole
0.0119
-
at pH 7.4 and 37°C Mus musculus hydroxyitraconazole