Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary 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

EC Number Inhibitors Comment Organism Structure
1.1.1.B40 11-deoxycorticosterone IC50: 0.001 mM Ovis aries aries
1.1.1.B40 4-pregnen-11,17-diol-3,20-dione IC50: 0.00035 mM Ovis aries aries
1.1.1.B40 4-pregnen-11alpha-ol-3,20-dione IC50: 0.0001 mM Ovis aries aries
1.1.1.B40 4-pregnen-11beta-ol-3,20-dione IC50: 0.00005 mM Ovis aries aries
1.1.1.B40 4-pregnen-16alpha-ol-3,20-dione not inhibitory Ovis aries aries
1.1.1.B40 4-pregnen-17,21-diol-3,20-dione not inhibitory Ovis aries aries
1.1.1.B40 4-pregnen-17alpha,20alpha-diol-3-one not inhibitory Ovis aries aries
1.1.1.B40 4-pregnen-17alpha-ol-3,20-dione IC50: 0.047 mM Ovis aries aries
1.1.1.B40 4-pregnen-20alpha-ol-3-one IC50: 0.007 mM Ovis aries aries
1.1.1.B40 4-pregnen-20beta-ol-3-one IC50: 0.008 mM Ovis aries aries
1.1.1.B40 4-pregnen-21-ol-3,20-dione IC50: 0.001 mM Ovis aries aries
1.1.1.B40 4-pregnen-3,11,20-trione IC50: 0.0004 mM Ovis aries aries
1.1.1.B40 4-pregnen-3,20-dione IC50: 0.0011 mM Ovis aries aries
1.1.1.B40 5-pregnen-3beta,11beta-diol-20-one IC50: 0.0001 mM Ovis aries aries
1.1.1.B40 5alpha-pregnan-11alpha-ol-3,20-dione IC50: 0.00035 mM Ovis aries aries
1.1.1.B40 5alpha-pregnan-11beta,17alpha,21-triol-3,20-dione IC50: 0.0031 mM Ovis aries aries
1.1.1.B40 5alpha-pregnan-11beta,21-diol-3,20-dione IC50: 0.00015 mM Ovis aries aries
1.1.1.B40 5alpha-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one IC50: 0.008 mM Ovis aries aries
1.1.1.B40 5alpha-pregnan-3alpha,11beta,21-triol-20-one IC50: 0.00026 mM Ovis aries aries
1.1.1.B40 5alpha-pregnan-3alpha,11beta-diol-20-one IC50: 0.00012 mM Ovis aries aries
1.1.1.B40 5alpha-pregnan-3alpha,17alpha,21-triol-11,20-dione IC50: 0.0055 mM Ovis aries aries
1.1.1.B40 5alpha-pregnan-3alpha,21-diol-11,20-dione IC50: 0.0008 mM Ovis aries aries
1.1.1.B40 5alpha-Pregnan-3alpha,21-diol-20-one IC50: 0.0024 mM Ovis aries aries
1.1.1.B40 5alpha-pregnan-3alpha-ol-20-one IC50: 0.008 mM Ovis aries aries
1.1.1.B40 5beta-pregnan-3alpha,11alpha-diol-20-one not inhibitory Ovis aries aries
1.1.1.B40 5beta-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one not inhibitory Ovis aries aries
1.1.1.B40 5beta-pregnan-3alpha,11beta,21-triol-20-one not inhibitory Ovis aries aries
1.1.1.B40 5beta-pregnan-3alpha,11beta-diol-20-one not inhibitory Ovis aries aries
1.1.1.B40 5beta-Pregnan-3alpha,21-diol-20-one not inhibitory Ovis aries aries
1.1.1.B40 5beta-Pregnan-3alpha-ol-20-one not inhibitory Ovis aries aries
1.1.1.146 11-deoxycorticosterone IC50: 0.031 mM Rattus sp.
1.1.1.146 4-pregnen-11,17-diol-3,20-dione IC50: 0.1 mM Rattus sp.
1.1.1.146 4-pregnen-11alpha-ol-3,20-dione IC50: 0.0095 mM Rattus sp.
1.1.1.146 4-pregnen-11beta-ol-3,20-dione IC50: 0.011 mM Rattus sp.
1.1.1.146 4-pregnen-16alpha-ol-3,20-dione IC50: 0.9 mM Rattus sp.
1.1.1.146 4-pregnen-17,21-diol-3,20-dione IC50: 0.07 mM Rattus sp.
1.1.1.146 4-pregnen-17alpha,20alpha-diol-3-one IC50: 0.115 mM Rattus sp.
1.1.1.146 4-pregnen-17alpha-ol-3,20-dione IC50: 0.19 mM Rattus sp.
1.1.1.146 4-pregnen-20alpha-ol-3-one IC50: 0.022 mM Rattus sp.
1.1.1.146 4-pregnen-20beta-ol-3-one IC50: 0.031 mM Rattus sp.
1.1.1.146 4-pregnen-21-ol-3,20-dione IC50: 0.031 mM Rattus sp.
1.1.1.146 4-pregnen-3,11,20-trione IC50: 0.19 mM Rattus sp.
1.1.1.146 4-pregnen-3,20-dione IC50: 0.015 mM Rattus sp.
1.1.1.146 5-pregnen-3beta,11beta-diol-20-one IC50: 0.0095 mM Rattus sp.
1.1.1.146 5alpha-pregnan-11alpha-ol-3,20-dione IC50: 0.0027 mM Rattus sp.
1.1.1.146 5alpha-pregnan-11beta,17alpha,21-triol-3,20-dione IC50: 0.04 mM Rattus sp.
1.1.1.146 5alpha-pregnan-11beta,21-diol-3,20-dione IC50: 0.0075 mM Rattus sp.
1.1.1.146 5alpha-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one IC50: 0.18 mM Rattus sp.
1.1.1.146 5alpha-pregnan-3alpha,11beta,21-triol-20-one IC50: 0.008 mM Rattus sp.
1.1.1.146 5alpha-pregnan-3alpha,11beta-diol-20-one IC50: 0.016 mM Rattus sp.
1.1.1.146 5alpha-pregnan-3alpha,17alpha,21-triol-11,20-dione IC50: 0.24 mM Rattus sp.
1.1.1.146 5alpha-pregnan-3alpha,21-diol-11,20-dione IC50: 0.029 mM Rattus sp.
1.1.1.146 5alpha-Pregnan-3alpha,21-diol-20-one IC50: 0.031 mM Rattus sp.
1.1.1.146 5alpha-pregnan-3alpha-ol-20-one IC50: 0.014 mM Rattus sp.
1.1.1.146 5beta-pregnan-3alpha,11alpha-diol-20-one IC50: 0.08 mM Rattus sp.
1.1.1.146 5beta-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one IC50: 0.12 mM Rattus sp.
1.1.1.146 5beta-pregnan-3alpha,11beta,21-triol-20-one IC50: 0.14 mM Rattus sp.
1.1.1.146 5beta-pregnan-3alpha,11beta-diol-20-one IC50: 0.0 mM Rattus sp.
1.1.1.146 5beta-Pregnan-3alpha,21-diol-20-one IC50: 0.003 mM Rattus sp.
1.1.1.146 5beta-Pregnan-3alpha-ol-20-one IC50: 0.012 mM Rattus sp.

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.1.1.B40 0.000014
-
 11beta,21-dihydroxypregn-4-en-3,20-dione isoform 11beta-HSD2 Ovis aries aries
1.1.1.146 0.002
-
 11beta,21-dihydroxypregn-4-en-3,20-dione isoform 11beta-HSD1 Rattus sp.

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.B40 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
1.1.1.B40 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
1.1.1.146 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+
-
 ?
1.1.1.146 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

EC Number Organism UniProt Comment Textmining
1.1.1.B40 Ovis aries aries
-
 sheep, isoform 11beta-HSD2
-
1.1.1.146 Rattus sp.
-
 isoform 11beta-HSD1
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.B40 kidney
-
 Ovis aries aries
-
1.1.1.146 kidney
-
 Rattus sp.
-
1.1.1.146 liver
-
 Rattus sp.
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.B40 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
1.1.1.B40 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
1.1.1.146 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+
-
 ?
1.1.1.146 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

Synonyms

EC Number Synonyms Comment Organism
1.1.1.B40 11beta-HSD NAD-specific 11beta-HSD isoform type 2 Ovis aries aries

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.B40 NAD+ isoform 11beta-HSD2 Ovis aries aries
1.1.1.B40 NADH isoform 11beta-HSD2 Ovis aries aries
1.1.1.146 NAD+
-
 Rattus sp.
1.1.1.146 NADH
-
 Rattus sp.
1.1.1.146 NADP+ isoform 11beta-HSD1 Rattus sp.
1.1.1.146 NADPH isoform 11beta-HSD1 Rattus sp.

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.B40 0.00005
-
 IC50: 0.00005 mM Ovis aries aries 4-pregnen-11beta-ol-3,20-dione
1.1.1.B40 0.0001
-
 IC50: 0.0001 mM Ovis aries aries 4-pregnen-11alpha-ol-3,20-dione
1.1.1.B40 0.0001
-
 IC50: 0.0001 mM Ovis aries aries 5-pregnen-3beta,11beta-diol-20-one
1.1.1.B40 0.00012
-
 IC50: 0.00012 mM Ovis aries aries 5alpha-pregnan-3alpha,11beta-diol-20-one
1.1.1.B40 0.00015
-
 IC50: 0.00015 mM Ovis aries aries 5alpha-pregnan-11beta,21-diol-3,20-dione
1.1.1.B40 0.00026
-
 IC50: 0.00026 mM Ovis aries aries 5alpha-pregnan-3alpha,11beta,21-triol-20-one
1.1.1.B40 0.00035
-
 IC50: 0.00035 mM Ovis aries aries 4-pregnen-11,17-diol-3,20-dione
1.1.1.B40 0.00035
-
 IC50: 0.00035 mM Ovis aries aries 5alpha-pregnan-11alpha-ol-3,20-dione
1.1.1.B40 0.0004
-
 IC50: 0.0004 mM Ovis aries aries 4-pregnen-3,11,20-trione
1.1.1.B40 0.0008
-
 IC50: 0.0008 mM Ovis aries aries 5alpha-pregnan-3alpha,21-diol-11,20-dione
1.1.1.B40 0.001
-
 IC50: 0.001 mM Ovis aries aries 11-deoxycorticosterone
1.1.1.B40 0.001
-
 IC50: 0.001 mM Ovis aries aries 4-pregnen-21-ol-3,20-dione
1.1.1.B40 0.0011
-
 IC50: 0.0011 mM Ovis aries aries 4-pregnen-3,20-dione
1.1.1.B40 0.0024
-
 IC50: 0.0024 mM Ovis aries aries 5alpha-Pregnan-3alpha,21-diol-20-one
1.1.1.B40 0.0031
-
 IC50: 0.0031 mM Ovis aries aries 5alpha-pregnan-11beta,17alpha,21-triol-3,20-dione
1.1.1.B40 0.0055
-
 IC50: 0.0055 mM Ovis aries aries 5alpha-pregnan-3alpha,17alpha,21-triol-11,20-dione
1.1.1.B40 0.007
-
 IC50: 0.007 mM Ovis aries aries 4-pregnen-20alpha-ol-3-one
1.1.1.B40 0.008
-
 IC50: 0.008 mM Ovis aries aries 5alpha-pregnan-3alpha-ol-20-one
1.1.1.B40 0.008
-
 IC50: 0.008 mM Ovis aries aries 4-pregnen-20beta-ol-3-one
1.1.1.B40 0.008
-
 IC50: 0.008 mM Ovis aries aries 5alpha-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one
1.1.1.B40 0.047
-
 IC50: 0.047 mM Ovis aries aries 4-pregnen-17alpha-ol-3,20-dione
1.1.1.146 0.0027
-
 IC50: 0.0027 mM Rattus sp. 5alpha-pregnan-11alpha-ol-3,20-dione
1.1.1.146 0.003
-
 IC50: 0.003 mM Rattus sp. 5beta-Pregnan-3alpha,21-diol-20-one
1.1.1.146 0.0075
-
 IC50: 0.0075 mM Rattus sp. 5alpha-pregnan-11beta,21-diol-3,20-dione
1.1.1.146 0.008
-
 IC50: 0.008 mM Rattus sp. 5alpha-pregnan-3alpha,11beta,21-triol-20-one
1.1.1.146 0.0095
-
 IC50: 0.0095 mM Rattus sp. 4-pregnen-11alpha-ol-3,20-dione
1.1.1.146 0.0095
-
 IC50: 0.0095 mM Rattus sp. 5-pregnen-3beta,11beta-diol-20-one
1.1.1.146 0.011
-
 IC50: 0.011 mM Rattus sp. 4-pregnen-11beta-ol-3,20-dione
1.1.1.146 0.012
-
 IC50: 0.012 mM Rattus sp. 5beta-Pregnan-3alpha-ol-20-one
1.1.1.146 0.014
-
 IC50: 0.014 mM Rattus sp. 5alpha-pregnan-3alpha-ol-20-one
1.1.1.146 0.015
-
 IC50: 0.015 mM Rattus sp. 4-pregnen-3,20-dione
1.1.1.146 0.016
-
 IC50: 0.016 mM Rattus sp. 5alpha-pregnan-3alpha,11beta-diol-20-one
1.1.1.146 0.022
-
 IC50: 0.022 mM Rattus sp. 4-pregnen-20alpha-ol-3-one
1.1.1.146 0.029
-
 IC50: 0.029 mM Rattus sp. 5alpha-pregnan-3alpha,21-diol-11,20-dione
1.1.1.146 0.031
-
 IC50: 0.031 mM Rattus sp. 11-deoxycorticosterone
1.1.1.146 0.031
-
 IC50: 0.031 mM Rattus sp. 5alpha-Pregnan-3alpha,21-diol-20-one
1.1.1.146 0.031
-
 IC50: 0.031 mM Rattus sp. 4-pregnen-21-ol-3,20-dione
1.1.1.146 0.031
-
 IC50: 0.031 mM Rattus sp. 4-pregnen-20beta-ol-3-one
1.1.1.146 0.04
-
 IC50: 0.04 mM Rattus sp. 5alpha-pregnan-11beta,17alpha,21-triol-3,20-dione
1.1.1.146 0.07
-
 IC50: 0.07 mM Rattus sp. 4-pregnen-17,21-diol-3,20-dione
1.1.1.146 0.08
-
 IC50: 0.08 mM Rattus sp. 5beta-pregnan-3alpha,11alpha-diol-20-one
1.1.1.146 0.1
-
 IC50: 0.1 mM Rattus sp. 4-pregnen-11,17-diol-3,20-dione
1.1.1.146 0.115
-
 IC50: 0.115 mM Rattus sp. 4-pregnen-17alpha,20alpha-diol-3-one
1.1.1.146 0.12
-
 IC50: 0.12 mM Rattus sp. 5beta-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one
1.1.1.146 0.14
-
 IC50: 0.14 mM Rattus sp. 5beta-pregnan-3alpha,11beta,21-triol-20-one
1.1.1.146 0.18
-
 IC50: 0.18 mM Rattus sp. 5alpha-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one
1.1.1.146 0.19
-
 IC50: 0.19 mM Rattus sp. 4-pregnen-17alpha-ol-3,20-dione
1.1.1.146 0.19
-
 IC50: 0.19 mM Rattus sp. 4-pregnen-3,11,20-trione
1.1.1.146 0.24
-
 IC50: 0.24 mM Rattus sp. 5alpha-pregnan-3alpha,17alpha,21-triol-11,20-dione
1.1.1.146 0.9
-
 IC50: 0.9 mM Rattus sp. 4-pregnen-16alpha-ol-3,20-dione