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Literature summary for 1.1.1.B40 extracted from

  • Latif, S.A.; Sheff, M.F.; Ribeiro, C.E.; Morris, D.J.
    Selective inhibition of sheep kidney 11beta-hydroxysteroid dehydrogenase isoform 2 activity by 5alpha-reduced (but not 5beta) derivates of adrenocorticosteroids (1997), Steroids, 62, 230-237.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
11-deoxycorticosterone IC50: 0.001 mM Ovis aries aries
4-pregnen-11,17-diol-3,20-dione IC50: 0.00035 mM Ovis aries aries
4-pregnen-11alpha-ol-3,20-dione IC50: 0.0001 mM Ovis aries aries
4-pregnen-11beta-ol-3,20-dione IC50: 0.00005 mM Ovis aries aries
4-pregnen-16alpha-ol-3,20-dione not inhibitory Ovis aries aries
4-pregnen-17,21-diol-3,20-dione not inhibitory Ovis aries aries
4-pregnen-17alpha,20alpha-diol-3-one not inhibitory Ovis aries aries
4-pregnen-17alpha-ol-3,20-dione IC50: 0.047 mM Ovis aries aries
4-pregnen-20alpha-ol-3-one IC50: 0.007 mM Ovis aries aries
4-pregnen-20beta-ol-3-one IC50: 0.008 mM Ovis aries aries
4-pregnen-21-ol-3,20-dione IC50: 0.001 mM Ovis aries aries
4-pregnen-3,11,20-trione IC50: 0.0004 mM Ovis aries aries
4-pregnen-3,20-dione IC50: 0.0011 mM Ovis aries aries
5-pregnen-3beta,11beta-diol-20-one IC50: 0.0001 mM Ovis aries aries
5alpha-pregnan-11alpha-ol-3,20-dione IC50: 0.00035 mM Ovis aries aries
5alpha-pregnan-11beta,17alpha,21-triol-3,20-dione IC50: 0.0031 mM Ovis aries aries
5alpha-pregnan-11beta,21-diol-3,20-dione IC50: 0.00015 mM Ovis aries aries
5alpha-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one IC50: 0.008 mM Ovis aries aries
5alpha-pregnan-3alpha,11beta,21-triol-20-one IC50: 0.00026 mM Ovis aries aries
5alpha-pregnan-3alpha,11beta-diol-20-one IC50: 0.00012 mM Ovis aries aries
5alpha-pregnan-3alpha,17alpha,21-triol-11,20-dione IC50: 0.0055 mM Ovis aries aries
5alpha-pregnan-3alpha,21-diol-11,20-dione IC50: 0.0008 mM Ovis aries aries
5alpha-Pregnan-3alpha,21-diol-20-one IC50: 0.0024 mM Ovis aries aries
5alpha-pregnan-3alpha-ol-20-one IC50: 0.008 mM Ovis aries aries
5beta-pregnan-3alpha,11alpha-diol-20-one not inhibitory Ovis aries aries
5beta-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one not inhibitory Ovis aries aries
5beta-pregnan-3alpha,11beta,21-triol-20-one not inhibitory Ovis aries aries
5beta-pregnan-3alpha,11beta-diol-20-one not inhibitory Ovis aries aries
5beta-Pregnan-3alpha,21-diol-20-one not inhibitory Ovis aries aries
5beta-Pregnan-3alpha-ol-20-one not inhibitory Ovis aries aries

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.000014
-
11beta,21-dihydroxypregn-4-en-3,20-dione isoform 11beta-HSD2 Ovis aries aries

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
11beta,21-dihydroxypregn-4-en-3,20-dione + NAD+ Ovis aries aries isoform 11beta-HSD2 21-hydroxy-pregn-4-en-3,11,20-trione + NADH + H+
-
r
11beta,21-dihydroxypregn-4-en-3,20-dione + NAD+ Ovis aries aries i.e. corticosterone 21-hydroxy-pregn-4-en-3,11,20-trione + NADH + H+
-
r

Organism

Organism UniProt Comment Textmining
Ovis aries aries
-
sheep, isoform 11beta-HSD2
-

Source Tissue

Source Tissue Comment Organism Textmining
kidney
-
Ovis aries aries
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
11beta,21-dihydroxypregn-4-en-3,20-dione + NAD+ isoform 11beta-HSD2 Ovis aries aries 21-hydroxy-pregn-4-en-3,11,20-trione + NADH + H+
-
r
11beta,21-dihydroxypregn-4-en-3,20-dione + NAD+ i.e. corticosterone Ovis aries aries 21-hydroxy-pregn-4-en-3,11,20-trione + NADH + H+
-
r

Synonyms

Synonyms Comment Organism
11beta-HSD NAD-specific 11beta-HSD isoform type 2 Ovis aries aries

Cofactor

Cofactor Comment Organism Structure
NAD+ isoform 11beta-HSD2 Ovis aries aries
NADH isoform 11beta-HSD2 Ovis aries aries

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00005
-
IC50: 0.00005 mM Ovis aries aries 4-pregnen-11beta-ol-3,20-dione
0.0001
-
IC50: 0.0001 mM Ovis aries aries 4-pregnen-11alpha-ol-3,20-dione
0.0001
-
IC50: 0.0001 mM Ovis aries aries 5-pregnen-3beta,11beta-diol-20-one
0.00012
-
IC50: 0.00012 mM Ovis aries aries 5alpha-pregnan-3alpha,11beta-diol-20-one
0.00015
-
IC50: 0.00015 mM Ovis aries aries 5alpha-pregnan-11beta,21-diol-3,20-dione
0.00026
-
IC50: 0.00026 mM Ovis aries aries 5alpha-pregnan-3alpha,11beta,21-triol-20-one
0.00035
-
IC50: 0.00035 mM Ovis aries aries 4-pregnen-11,17-diol-3,20-dione
0.00035
-
IC50: 0.00035 mM Ovis aries aries 5alpha-pregnan-11alpha-ol-3,20-dione
0.0004
-
IC50: 0.0004 mM Ovis aries aries 4-pregnen-3,11,20-trione
0.0008
-
IC50: 0.0008 mM Ovis aries aries 5alpha-pregnan-3alpha,21-diol-11,20-dione
0.001
-
IC50: 0.001 mM Ovis aries aries 11-deoxycorticosterone
0.001
-
IC50: 0.001 mM Ovis aries aries 4-pregnen-21-ol-3,20-dione
0.0011
-
IC50: 0.0011 mM Ovis aries aries 4-pregnen-3,20-dione
0.0024
-
IC50: 0.0024 mM Ovis aries aries 5alpha-Pregnan-3alpha,21-diol-20-one
0.0031
-
IC50: 0.0031 mM Ovis aries aries 5alpha-pregnan-11beta,17alpha,21-triol-3,20-dione
0.0055
-
IC50: 0.0055 mM Ovis aries aries 5alpha-pregnan-3alpha,17alpha,21-triol-11,20-dione
0.007
-
IC50: 0.007 mM Ovis aries aries 4-pregnen-20alpha-ol-3-one
0.008
-
IC50: 0.008 mM Ovis aries aries 5alpha-pregnan-3alpha-ol-20-one
0.008
-
IC50: 0.008 mM Ovis aries aries 4-pregnen-20beta-ol-3-one
0.008
-
IC50: 0.008 mM Ovis aries aries 5alpha-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one
0.047
-
IC50: 0.047 mM Ovis aries aries 4-pregnen-17alpha-ol-3,20-dione