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Literature summary for 1.1.1.146 extracted from

  • Beck, K.R.; Kanagaratnam, S.; Kratschmar, D.V.; Birk, J.; Yamaguchi, H.; Sailer, A.W.; Seuwen, K.; Odermatt, A.
    Enzymatic interconversion of the oxysterols 7beta,25-dihydroxycholesterol and 7-keto,25-hydroxycholesterol by 11beta-hydroxysteroid dehydrogenase type 1 and 2 (2019), J. Steroid Biochem. Mol. Biol., 190, 19-28 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
7-keto,25-hydroxycholesterol inhibits the oxoreduction of cortisone to cortisol by the recombinant isoform 11beta-HSD1 Homo sapiens
7-keto,25-hydroxycholesterol
-
Mus musculus
7alpha,25-Dihydroxycholesterol
-
Homo sapiens
7beta,25-dihydroxycholesterol
-
Homo sapiens
7beta,25-dihydroxycholesterol
-
Mus musculus
glycyrrhetinic acid
-
Homo sapiens
additional information not inhibited by 7alpha,25-dihydroxycholesterol Homo sapiens
additional information isoform 11beta-HSD2 is not inhibited by 7alpha,25-dihydroxycholesterol Mus musculus
T0504
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.000029
-
7beta,25-dihydroxycholesterol recombinant isoform 11beta-HSD1, at pH 7.4 and 37°C Homo sapiens
0.000556
-
7beta,25-dihydroxycholesterol recombinant isoform 11beta-HSD2, at pH 7.4 and 37°C Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Homo sapiens
-
-
microsome
-
Mus musculus
-
-

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-
Homo sapiens P80365
-
-
Mus musculus P50172
-
-
Mus musculus P51661
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
Homo sapiens
-
kidney
-
Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7-keto,25-hydroxycholesterol + NADPH + H+
-
Homo sapiens 7beta,25-dihydroxycholesterol + NADP+
-
?
7-keto,25-hydroxycholesterol + NADPH + H+
-
Mus musculus 7beta,25-dihydroxycholesterol + NADP+
-
?
7-ketocholesterol + NADPH + H+
-
Homo sapiens 7beta-hydroxycholesterol + NADP+
-
?
7-ketocholesterol + NADPH + H+
-
Mus musculus 7beta-hydroxycholesterol + NADP+
-
?
7beta,25-dihydroxycholesterol + NAD+
-
Homo sapiens 7-keto,25-hydroxycholesterol + NADH + H+
-
?
7beta,25-dihydroxycholesterol + NAD+
-
Mus musculus 7-keto,25-hydroxycholesterol + NADH + H+
-
?
corticosterone + NAD+
-
Mus musculus 11-dehydrocorticosterone + NADH + H+
-
?
cortisol + NAD+
-
Homo sapiens cortisone + NADH + H+
-
?
cortisol + NAD+
-
Mus musculus cortisone + NADH + H+
-
?
cortisone + NADPH + H+
-
Homo sapiens cortisol + NADP+
-
?
cortisone + NADPH + H+
-
Mus musculus cortisol + NADP+
-
?

Synonyms

Synonyms Comment Organism
11beta-HSD1
-
Homo sapiens
11beta-HSD1
-
Mus musculus
11beta-HSD2
-
Homo sapiens
11beta-HSD2
-
Mus musculus
11beta-hydroxysteroid dehydrogenase type 1
-
Homo sapiens
11beta-hydroxysteroid dehydrogenase type 1
-
Mus musculus
11beta-hydroxysteroid dehydrogenase type 2
-
Homo sapiens
11beta-hydroxysteroid dehydrogenase type 2
-
Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000049
-
recombinant isoform 11beta-HSD2, at pH 7.4 and 37°C Homo sapiens 7-keto,25-hydroxycholesterol
0.000053
-
recombinant isoform 11beta-HSD1, at pH 7.4 and 37°C Mus musculus 7-keto,25-hydroxycholesterol
0.000091
-
recombinant isoform 11beta-HSD2, at pH 7.4 and 37°C Homo sapiens 7beta,25-dihydroxycholesterol
0.000119
-
recombinant isoform 11beta-HSD1, at pH 7.4 and 37°C Mus musculus 7beta,25-dihydroxycholesterol
0.000405
-
recombinant isoform 11beta-HSD1, at pH 7.4 and 37°C Homo sapiens 7-keto,25-hydroxycholesterol
0.002
-
IC50 of more than 0.002 mM, recombinant isoform 11beta-HSD2, at pH 7.4 and 37°C Mus musculus 7-keto,25-hydroxycholesterol
0.003
-
IC50 of more than 0.003 mM, recombinant isoform 11beta-HSD1, at pH 7.4 and 37°C Homo sapiens 7beta,25-dihydroxycholesterol
0.003
-
recombinant isoform 11beta-HSD2, at pH 7.4 and 37°C Mus musculus 7beta,25-dihydroxycholesterol