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Literature summary for 1.1.1.B40 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)

Cloned (Comment) Organism
stable expression of isozymes 11beta-HSD1 and 11beta-HSD2 in CHO cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
BVT-14225 isozyme 11beta-HSD1 IC50: 52 nM, 1000fold less potent against isozyme 11beta-HSD2 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
cortisol + NAD+ Homo sapiens isozyme 11beta-HSD2 catalyzes the reverse reaction of 11-beta-HSD1 with cofactor NAD+ cortisone + NADH
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ir

Organism

Organism UniProt Comment Textmining
Homo sapiens
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isozymes 11beta-HSD1 and 11beta-HSD2
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
cortisol + NAD+ isozyme 11beta-HSD2 catalyzes the reverse reaction of 11-beta-HSD1 with cofactor NAD+ Homo sapiens cortisone + NADH
-
ir

Cofactor

Cofactor Comment Organism Structure
NAD+
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
isozyme 11beta-HSD1 IC50: 52 nM, 1000fold less potent against isozyme 11beta-HSD2 Homo sapiens BVT-14225