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Literature summary for 1.1.1.146 extracted from

  • Buhler, H.; Perschel, F.H.; Hierholzer, K.
    Inhibition of rat renal 11beta-hydroxysteroid dehydrogenase by steroidal compounds and triterpenoids; structure/function relationship (1991), Biochim. Biophys. Acta, 1075, 206-212.
    View publication on PubMed
Search for more literature for 1.1.1.146

Inhibitors

Inhibitors Comment Organism Structure
3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate i.e. CHAPS; oxidase IC50: 0.17 mM, reductase IC50: 0.82 mM Rattus sp.
alpha-glycyrrhetinic acid oxidase, IC50: 14 nmol, reductase, IC50: 42 nmol Rattus sp.
beta-glycyrrhetinic acid oxidase, IC50: 2.9 nmol, reductase, IC50: 13 nmol Rattus sp.
betulin inhibition at 0.1 mM: oxidase 36%, reductase 34.5% Rattus sp.
cholesterol oxidase: 18.6% inhibition at 0.1 mM, reductase: 7.4% inhibition at 0.1 mM Rattus sp.
G-strophanthidin inhibition at 0.1 mM: oxidase 4.8%, reductase 6.1% Rattus sp.
glycyrrhizic acid oxidase, IC50: 0.0039 mM, reductase, IC50: 0.013 mM Rattus sp.
helvolic acid inhibition at 0.1 mM: oxidase 13%, reductase 18.5% Rattus sp.
lanosterol oxidase IC50: 0.00065 mM, reductase IC50: 0.0017 mM Rattus sp.
lupeol inhibition at 0.1 mM: oxidase 52%, reductase 38.4% Rattus sp.
additional information all inhibitory compounds tested show competitive inhibition, more effective inhibition of oxidative than reductive activity, inhibition is enhanced by C11-oxygen function and a C7-OH function, inhibition is influenced by steric conformation of inhibitor Rattus sp.
N,N-bis(3-D-gluconamidopropyl)cholamide i.e. BIGCHAP; oxidase IC50: 0.0026 mM, reductase IC50: 0.0058 mM Rattus sp.
N,N-bis(3-D-gluconamidopropyl)deoxycholamide i.e. deoxy-BIGCHAP; oxidase IC50: 0.055 mM, reductase IC50: 0.58 mM Rattus sp.
oleanolic acid oxidase IC50: 0.00015 mM, reductase IC50: 0.00055 mM 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 + NADP+ Rattus sp.
-
 21-hydroxy-pregn-4-en-3,11,20-trione + NADPH + H+
-
 r

Organism

Organism UniProt Comment Textmining
Rattus sp.
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
kidney
-
 Rattus sp.
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
11beta,21-dihydroxypregn-4-en-3,20-dione + NADP+
-
 Rattus sp. 21-hydroxy-pregn-4-en-3,11,20-trione + NADPH + H+
-
 r

Cofactor

Cofactor Comment Organism Structure
NADP+
-
 Rattus sp.
NADPH
-
 Rattus sp.

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000013
-
 oxidase, IC50: 2.9 nmol, reductase, IC50: 13 nmol Rattus sp. beta-glycyrrhetinic acid
0.000042
-
 oxidase, IC50: 14 nmol, reductase, IC50: 42 nmol Rattus sp. alpha-glycyrrhetinic acid
0.00055
-
 oxidase IC50: 0.00015 mM, reductase IC50: 0.00055 mM Rattus sp. oleanolic acid
0.0017
-
 oxidase IC50: 0.00065 mM, reductase IC50: 0.0017 mM Rattus sp. lanosterol
0.0058
-
 oxidase IC50: 0.0026 mM, reductase IC50: 0.0058 mM Rattus sp. N,N-bis(3-D-gluconamidopropyl)cholamide
0.013
-
 oxidase, IC50: 0.0039 mM, reductase, IC50: 0.013 mM Rattus sp. glycyrrhizic acid
0.58
-
 oxidase IC50: 0.055 mM, reductase IC50: 0.58 mM Rattus sp. N,N-bis(3-D-gluconamidopropyl)deoxycholamide
0.82
-
 oxidase IC50: 0.17 mM, reductase IC50: 0.82 mM Rattus sp. 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate