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Literature summary extracted from

  • Xiang, J.; Ipek, M.; Suri, V.; Massefski, W.; Pan, N.; Ge, Y.; Tam, M.; Xing, Y.; Tobin, J.F.; Xu, X.; Tam, S.
    Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I (2005), Bioorg. Med. Chem. Lett., 15, 2865-2869.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.B40 stable expression of isozymes 11beta-HSD1 and 11beta-HSD2 in CHO cells Homo sapiens
1.1.1.146 stable expression of isozymes 11beta-HSD1 and 11beta-HSD2 in CHO cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.B40 BVT-14225 isozyme 11beta-HSD1 IC50: 52 nM, 1000fold less potent against isozyme 11beta-HSD2 Homo sapiens
1.1.1.146 1-(5-oxo-2,5-dihydrofuran-3-yl)urea specific for isozyme 11beta-HSD1 Homo sapiens
1.1.1.146 arylsulfonamidothiazole derivatives specific for isozyme 11beta-HSD1 Homo sapiens
1.1.1.146 BVT-14225 isozyme 11beta-HSD1 IC50: 52 nM, 1000fold less potent against isozyme 11beta-HSD2 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.B40 cortisol + NAD+ Homo sapiens isozyme 11beta-HSD2 catalyzes the reverse reaction of 11-beta-HSD1 with cofactor NAD+ cortisone + NADH
-
 ir
1.1.1.146 cortisone + NADPH + H+ Homo sapiens isozyme 11beta-HSD1 catalyzes the forward reaction with cofactor NADPH cortisol + NADP+
-
 ir

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.B40 Homo sapiens
-
 isozymes 11beta-HSD1 and 11beta-HSD2
-
1.1.1.146 Homo sapiens
-
 isozymes 11beta-HSD1 and 11beta-HSD2
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.B40 cortisol + NAD+ isozyme 11beta-HSD2 catalyzes the reverse reaction of 11-beta-HSD1 with cofactor NAD+ Homo sapiens cortisone + NADH
-
 ir
1.1.1.146 cortisone + NADPH + H+ isozyme 11beta-HSD1 catalyzes the forward reaction with cofactor NADPH Homo sapiens cortisol + NADP+
-
 ir

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.B40 NAD+
-
 Homo sapiens
1.1.1.146 NADPH
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.B40 additional information
-
 isozyme 11beta-HSD1 IC50: 52 nM, 1000fold less potent against isozyme 11beta-HSD2 Homo sapiens BVT-14225
1.1.1.146 0.000052
-
 isozyme 11beta-HSD1 IC50: 52 nM, 1000fold less potent against isozyme 11beta-HSD2, pH and temperature not specified in the publication Homo sapiens BVT-14225