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Literature summary for 1.1.1.146 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

Protein Variants Comment Organism
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
Y177F site-directed mutagenesis, the mutant shows kinetics similar to the wild-type enzyme Homo sapiens
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

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

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+
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isozyme 11beta-HSD1
-

Reaction

Reaction Comment Organism Reaction ID
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

Substrates and Products (Substrate)

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

Subunits

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

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens