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Literature summary extracted from

  • Hult, M.; Shafqat, N.; Elleby, B.; Mitschke, D.; Svensson, S.; Forsgren, M.; Barf, T.; Vallgarda, J.; Abrahmsen, L.; Oppermann, U.
    Active site variability of type 1 11beta-hydroxysteroid dehydrogenase revealed by selective inhibitors and cross-species comparisons (2006), Mol. Cell. Endocrinol., 248, 26-33.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.146 arylsulfoamidothiazole
-
Cavia porcellus
1.1.1.146 arylsulfoamidothiazole
-
Homo sapiens
1.1.1.146 arylsulfoamidothiazole
-
Rattus norvegicus
1.1.1.146 arylsulfoamidothiazoles weak or not binding inhibitors, inhibition mode and profiles Cavia porcellus
1.1.1.146 arylsulfoamidothiazoles specific, tight-binding inhibitors, inhibition mode and profiles Homo sapiens
1.1.1.146 arylsulfoamidothiazoles intermediate binding inhibitors, inhibition mode and profiles Mus musculus
1.1.1.146 arylsulfoamidothiazoles weak or not binding binding inhibitors, inhibition mode and profiles Rattus norvegicus
1.1.1.146 BVT-2733 mixed-type inhibition pattern Mus musculus
1.1.1.146 BVT-528 competitive, tight-binding inhibition pattern Homo sapiens
1.1.1.146 carbenoxolone unspecific inhibitor Cavia porcellus
1.1.1.146 carbenoxolone unspecific inhibitor Homo sapiens
1.1.1.146 carbenoxolone unspecific inhibitor Mus musculus
1.1.1.146 carbenoxolone unspecific inhibitor Rattus norvegicus
1.1.1.146 additional information structure-activity analysis for inhibitor design Cavia porcellus
1.1.1.146 additional information structure-activity analysis for inhibitor design Homo sapiens
1.1.1.146 additional information structure-activity analysis for inhibitor design Mus musculus
1.1.1.146 additional information structure-activity analysis for inhibitor design Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.1.1.146 endoplasmic reticulum membrane isozyme 11beta-HSD1 is anchored through an N-terminal transmembrane domain Cavia porcellus 5789
-
1.1.1.146 endoplasmic reticulum membrane isozyme 11beta-HSD1 is anchored through an N-terminal transmembrane domain Mus musculus 5789
-
1.1.1.146 endoplasmic reticulum membrane isozyme 11beta-HSD1 is anchored through an N-terminal transmembrane domain Rattus norvegicus 5789
-
1.1.1.146 endoplasmic reticulum membrane isozyme 11beta-HSD1 is anchored through an N-terminal transmembrane domain Homo sapiens 5789
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.146 cortisone + NADPH + H+ Homo sapiens isozyme 11beta-HSD1 cortisol + NADP+
-
?
1.1.1.146 additional information Cavia porcellus the enzyme activates pro-glucocorticoid hormones in a tissue-specific manner ?
-
?
1.1.1.146 additional information Mus musculus the enzyme activates pro-glucocorticoid hormones in a tissue-specific manner ?
-
?
1.1.1.146 additional information Rattus norvegicus the enzyme activates pro-glucocorticoid hormones in a tissue-specific manner ?
-
?
1.1.1.146 additional information Homo sapiens the enzyme activates pro-glucocorticoid hormones in a tissue-specific manner ?
-
?

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.146 Cavia porcellus
-
isozyme 11beta-HSD1
-
1.1.1.146 Homo sapiens P28845 isozyme 11beta-HSD1
-
1.1.1.146 Mus musculus
-
isozyme 11beta-HSD1
-
1.1.1.146 Rattus norvegicus
-
isozyme 11beta-HSD1
-

Reaction

EC Number Reaction Comment Organism Reaction ID
1.1.1.146 an 11beta-hydroxysteroid + NADP+ = an 11-oxosteroid + NADPH + H+ active site variability of isozyme 11beta-HSD1, structure-activity analysis, catalytic mechanism Cavia porcellus
1.1.1.146 an 11beta-hydroxysteroid + NADP+ = an 11-oxosteroid + NADPH + H+ active site variability of isozyme 11beta-HSD1, structure-activity analysis, catalytic mechanism Mus musculus
1.1.1.146 an 11beta-hydroxysteroid + NADP+ = an 11-oxosteroid + NADPH + H+ active site variability of isozyme 11beta-HSD1, structure-activity analysis, catalytic mechanism Rattus norvegicus
1.1.1.146 an 11beta-hydroxysteroid + NADP+ = an 11-oxosteroid + NADPH + H+ active site variability of isozyme 11beta-HSD1, structure-activity analysis, catalytic mechanism Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.146 cortisone + NADPH + H+ isozyme 11beta-HSD1 Homo sapiens cortisol + NADP+
-
?
1.1.1.146 additional information the enzyme activates pro-glucocorticoid hormones in a tissue-specific manner Cavia porcellus ?
-
?
1.1.1.146 additional information the enzyme activates pro-glucocorticoid hormones in a tissue-specific manner Mus musculus ?
-
?
1.1.1.146 additional information the enzyme activates pro-glucocorticoid hormones in a tissue-specific manner Rattus norvegicus ?
-
?
1.1.1.146 additional information the enzyme activates pro-glucocorticoid hormones in a tissue-specific manner Homo sapiens ?
-
?

Subunits

EC Number Subunits Comment Organism
1.1.1.146 More comparison of primary structures, three-dimensional structure around the substrate binding site, and active site amino acid sequences of several mammalia Cavia porcellus
1.1.1.146 More comparison of primary structures, three-dimensional structure around the substrate binding site, and active site amino acid sequences of several mammalia Mus musculus
1.1.1.146 More comparison of primary structures, three-dimensional structure around the substrate binding site, and active site amino acid sequences of several mammalia Rattus norvegicus
1.1.1.146 More comparison of primary structures, three-dimensional structure around the substrate binding site, and active site amino acid sequences of several mammalia Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
1.1.1.146 11beta-HSD1
-
Cavia porcellus
1.1.1.146 11beta-HSD1
-
Mus musculus
1.1.1.146 11beta-HSD1
-
Rattus norvegicus
1.1.1.146 11beta-HSD1
-
Homo sapiens
1.1.1.146 More the enzyme belongs to the short-chain dehydrogenase/reductase superfamily Cavia porcellus
1.1.1.146 More the enzyme belongs to the short-chain dehydrogenase/reductase superfamily Mus musculus
1.1.1.146 More the enzyme belongs to the short-chain dehydrogenase/reductase superfamily Rattus norvegicus
1.1.1.146 More the enzyme belongs to the short-chain dehydrogenase/reductase superfamily Homo sapiens
1.1.1.146 type 1 11beta-hydroxysteroid dehydrogenase
-
Cavia porcellus
1.1.1.146 type 1 11beta-hydroxysteroid dehydrogenase
-
Mus musculus
1.1.1.146 type 1 11beta-hydroxysteroid dehydrogenase
-
Rattus norvegicus
1.1.1.146 type 1 11beta-hydroxysteroid dehydrogenase
-
Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.146 NADPH
-
Cavia porcellus
1.1.1.146 NADPH
-
Mus musculus
1.1.1.146 NADPH
-
Rattus norvegicus
1.1.1.146 NADPH
-
Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.1.1.146 0.00005
-
arylsulfoamidothiazole
-
Homo sapiens
1.1.1.146 0.003
-
arylsulfoamidothiazole above Cavia porcellus
1.1.1.146 0.003
-
arylsulfoamidothiazole above Rattus norvegicus