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Literature summary for 1.1.1.146 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
Search for more literature for 1.1.1.146

Inhibitors

Inhibitors Comment Organism Structure
11-deoxycorticosterone IC50: 0.031 mM Rattus sp.
4-pregnen-11,17-diol-3,20-dione IC50: 0.1 mM Rattus sp.
4-pregnen-11alpha-ol-3,20-dione IC50: 0.0095 mM Rattus sp.
4-pregnen-11beta-ol-3,20-dione IC50: 0.011 mM Rattus sp.
4-pregnen-16alpha-ol-3,20-dione IC50: 0.9 mM Rattus sp.
4-pregnen-17,21-diol-3,20-dione IC50: 0.07 mM Rattus sp.
4-pregnen-17alpha,20alpha-diol-3-one IC50: 0.115 mM Rattus sp.
4-pregnen-17alpha-ol-3,20-dione IC50: 0.19 mM Rattus sp.
4-pregnen-20alpha-ol-3-one IC50: 0.022 mM Rattus sp.
4-pregnen-20beta-ol-3-one IC50: 0.031 mM Rattus sp.
4-pregnen-21-ol-3,20-dione IC50: 0.031 mM Rattus sp.
4-pregnen-3,11,20-trione IC50: 0.19 mM Rattus sp.
4-pregnen-3,20-dione IC50: 0.015 mM Rattus sp.
5-pregnen-3beta,11beta-diol-20-one IC50: 0.0095 mM Rattus sp.
5alpha-pregnan-11alpha-ol-3,20-dione IC50: 0.0027 mM Rattus sp.
5alpha-pregnan-11beta,17alpha,21-triol-3,20-dione IC50: 0.04 mM Rattus sp.
5alpha-pregnan-11beta,21-diol-3,20-dione IC50: 0.0075 mM Rattus sp.
5alpha-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one IC50: 0.18 mM Rattus sp.
5alpha-pregnan-3alpha,11beta,21-triol-20-one IC50: 0.008 mM Rattus sp.
5alpha-pregnan-3alpha,11beta-diol-20-one IC50: 0.016 mM Rattus sp.
5alpha-pregnan-3alpha,17alpha,21-triol-11,20-dione IC50: 0.24 mM Rattus sp.
5alpha-pregnan-3alpha,21-diol-11,20-dione IC50: 0.029 mM Rattus sp.
5alpha-Pregnan-3alpha,21-diol-20-one IC50: 0.031 mM Rattus sp.
5alpha-pregnan-3alpha-ol-20-one IC50: 0.014 mM Rattus sp.
5beta-pregnan-3alpha,11alpha-diol-20-one IC50: 0.08 mM Rattus sp.
5beta-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one IC50: 0.12 mM Rattus sp.
5beta-pregnan-3alpha,11beta,21-triol-20-one IC50: 0.14 mM Rattus sp.
5beta-pregnan-3alpha,11beta-diol-20-one IC50: 0.0 mM Rattus sp.
5beta-Pregnan-3alpha,21-diol-20-one IC50: 0.003 mM Rattus sp.
5beta-Pregnan-3alpha-ol-20-one IC50: 0.012 mM Rattus sp.

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.002
-
 11beta,21-dihydroxypregn-4-en-3,20-dione isoform 11beta-HSD1 Rattus sp.

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+ Rattus sp. i.e. corticosterone 21-hydroxy-pregn-4-en-3,11,20-trione + NADH + H+
-
 ?
11beta,21-dihydroxypregn-4-en-3,20-dione + NADP+ Rattus sp. i.e. corticosterone isoform 11beta-HSD1 21-hydroxy-pregn-4-en-3,11,20-trione + NADPH + H+
-
 r

Organism

Organism UniProt Comment Textmining
Rattus sp.
-
 isoform 11beta-HSD1
-

Source Tissue

Source Tissue Comment Organism Textmining
kidney
-
 Rattus sp.
-
liver
-
 Rattus sp.
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
11beta,21-dihydroxypregn-4-en-3,20-dione + NAD+ i.e. corticosterone Rattus sp. 21-hydroxy-pregn-4-en-3,11,20-trione + NADH + H+
-
 ?
11beta,21-dihydroxypregn-4-en-3,20-dione + NADP+ i.e. corticosterone isoform 11beta-HSD1 Rattus sp. 21-hydroxy-pregn-4-en-3,11,20-trione + NADPH + H+
-
 r

Cofactor

Cofactor Comment Organism Structure
NAD+
-
 Rattus sp.
NADH
-
 Rattus sp.
NADP+ isoform 11beta-HSD1 Rattus sp.
NADPH isoform 11beta-HSD1 Rattus sp.

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0027
-
 IC50: 0.0027 mM Rattus sp. 5alpha-pregnan-11alpha-ol-3,20-dione
0.003
-
 IC50: 0.003 mM Rattus sp. 5beta-Pregnan-3alpha,21-diol-20-one
0.0075
-
 IC50: 0.0075 mM Rattus sp. 5alpha-pregnan-11beta,21-diol-3,20-dione
0.008
-
 IC50: 0.008 mM Rattus sp. 5alpha-pregnan-3alpha,11beta,21-triol-20-one
0.0095
-
 IC50: 0.0095 mM Rattus sp. 4-pregnen-11alpha-ol-3,20-dione
0.0095
-
 IC50: 0.0095 mM Rattus sp. 5-pregnen-3beta,11beta-diol-20-one
0.011
-
 IC50: 0.011 mM Rattus sp. 4-pregnen-11beta-ol-3,20-dione
0.012
-
 IC50: 0.012 mM Rattus sp. 5beta-Pregnan-3alpha-ol-20-one
0.014
-
 IC50: 0.014 mM Rattus sp. 5alpha-pregnan-3alpha-ol-20-one
0.015
-
 IC50: 0.015 mM Rattus sp. 4-pregnen-3,20-dione
0.016
-
 IC50: 0.016 mM Rattus sp. 5alpha-pregnan-3alpha,11beta-diol-20-one
0.022
-
 IC50: 0.022 mM Rattus sp. 4-pregnen-20alpha-ol-3-one
0.029
-
 IC50: 0.029 mM Rattus sp. 5alpha-pregnan-3alpha,21-diol-11,20-dione
0.031
-
 IC50: 0.031 mM Rattus sp. 11-deoxycorticosterone
0.031
-
 IC50: 0.031 mM Rattus sp. 5alpha-Pregnan-3alpha,21-diol-20-one
0.031
-
 IC50: 0.031 mM Rattus sp. 4-pregnen-21-ol-3,20-dione
0.031
-
 IC50: 0.031 mM Rattus sp. 4-pregnen-20beta-ol-3-one
0.04
-
 IC50: 0.04 mM Rattus sp. 5alpha-pregnan-11beta,17alpha,21-triol-3,20-dione
0.07
-
 IC50: 0.07 mM Rattus sp. 4-pregnen-17,21-diol-3,20-dione
0.08
-
 IC50: 0.08 mM Rattus sp. 5beta-pregnan-3alpha,11alpha-diol-20-one
0.1
-
 IC50: 0.1 mM Rattus sp. 4-pregnen-11,17-diol-3,20-dione
0.115
-
 IC50: 0.115 mM Rattus sp. 4-pregnen-17alpha,20alpha-diol-3-one
0.12
-
 IC50: 0.12 mM Rattus sp. 5beta-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one
0.14
-
 IC50: 0.14 mM Rattus sp. 5beta-pregnan-3alpha,11beta,21-triol-20-one
0.18
-
 IC50: 0.18 mM Rattus sp. 5alpha-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one
0.19
-
 IC50: 0.19 mM Rattus sp. 4-pregnen-17alpha-ol-3,20-dione
0.19
-
 IC50: 0.19 mM Rattus sp. 4-pregnen-3,11,20-trione
0.24
-
 IC50: 0.24 mM Rattus sp. 5alpha-pregnan-3alpha,17alpha,21-triol-11,20-dione
0.9
-
 IC50: 0.9 mM Rattus sp. 4-pregnen-16alpha-ol-3,20-dione