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Literature summary for 1.1.1.146 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

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

Localization

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

Natural Substrates/ Products (Substrates)

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

Organism

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

Reaction

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

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

Subunits

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

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

Cofactor

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

Ki Value [mM]

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