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Literature summary extracted from

  • Kim, K.W.; Wang, Z.; Busby, J.; Tsuruda, T.; Chen, M.; Hale, C.; Castro, V.M.; Svensson, S.; Nybo, R.; Xiong, F.; Wang, M.
    The role of tyrosine 177 in human 11beta-hydroxysteroid dehydrogenase type 1 in substrate and inhibitor binding: an unlikely hydrogen bond donor for the substrate (2006), Biochim. Biophys. Acta, 1764, 824-830.
    View publication on PubMed

Protein Variants

EC Number Protein Variants Comment Organism
1.1.1.146 Y177A site-directed mutagenesis, the mutant shows increased Km for cortisone compared to the wild-type enzyme, the mutation reduces the sensitivity to glycyrrhetinic acid inhibition 6-10fold, but not to carbenoxolone Homo sapiens
1.1.1.146 Y177F site-directed mutagenesis, the mutant shows kinetics similar to the wild-type enzyme Homo sapiens
1.1.1.146 Y177Q site-directed mutagenesis, the mutant shows increased Km for cortisone compared to the wild-type enzyme, the mutation reduces the sensitivity to glycyrrhetinic acid inhibition 6-10fold, but not to carbenoxolone Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.146 carbenoxolone
-
 Homo sapiens
1.1.1.146 glycyrrhetinic acid isozyme 11beta-HSD1 inhibitor, residue Tyr177 is important in binding, molecular modeling Homo sapiens

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+
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.146 Homo sapiens
-
 isozyme 11beta-HSD1
-

Reaction

EC Number Reaction Comment Organism Reaction ID
1.1.1.146 an 11beta-hydroxysteroid + NADP+ = an 11-oxosteroid + NADPH + H+ substrate binding and active site structure, isozyme 11beta-HSD1 contains the conserved catalytic motif YSASK, Tyr177 is not a hydrogen bond donor in substrate binding but is involved via hydrophobic interaction, Tyr177 is not involved in determination of substrate specificity Homo sapiens
a

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.146 11-dehydrocorticosterone + NADPH isozyme 11beta-HSD1 Homo sapiens corticosterone + NADP+
-
 ?
1.1.1.146 cortisone + NADPH + H+ isozyme 11beta-HSD1 Homo sapiens cortisol + NADP+
-
 ?

Subunits

EC Number Subunits Comment Organism
1.1.1.146 More comparison of active site structure of isozyme 11beta-HSD1 from different species, overview Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
1.1.1.146 11beta-HSD1
-
 Homo sapiens
1.1.1.146 11beta-hydroxysteroid dehydrogenase type 1
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.146 NADPH
-
 Homo sapiens