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Literature summary for 1.1.1.146 extracted from

  • Ganjoo, A.; Tripathi, A.; Chetti, P.
    Structural assessment and identification of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors (2020), J. Biomol. Struct. Dyn., 38, 4928-4937 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(3S)-1-(3-chloro-2-methylbenzene-1-sulfonyl)-N-cyclohexylpiperidine-3-carboxamide INCB-13739, selective inhibitor for isoform 11beta-HSD1 Homo sapiens
4-(cyclopentylsulfanyl)-3-[[1-(2,4-dichlorobenzamido)cyclopropyl]methoxy]-N-[(1R,2s,3S,5s,7s)-5-hydroxyadamantan-2-yl]-1,2-oxazole-5-carboxamide
-
Homo sapiens
AZD-4017 selective inhibitor for isoform 11beta-HSD1 Homo sapiens
INCB-13739 selective inhibitor for isoform 11beta-HSD1 Homo sapiens
UE2343 selective inhibitor for isoform 11beta-HSD1 Homo sapiens
[(1R,3r,5S)-3-hydroxy-3-(pyrimidin-2-yl)-8-azabicyclo[3.2.1]octan-8-yl][5-(1H-pyrazol-4-yl)thiophen-3-yl]methanone selective inhibitor for isoform 11beta-HSD1 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
corticosterone + NADP+ Homo sapiens
-
11-dehydrocorticosterone + NADPH + H+
-
?
cortisol + NADP+ Homo sapiens
-
cortisone + NADPH + H+
-
r
cortisone + NADPH + H+ Homo sapiens preferred direction of reaction cortisol + NADP+
-
r

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
corticosterone + NADP+
-
Homo sapiens 11-dehydrocorticosterone + NADPH + H+
-
?
cortisol + NADP+
-
Homo sapiens cortisone + NADPH + H+
-
r
cortisone + NADPH + H+ preferred direction of reaction Homo sapiens cortisol + NADP+
-
r

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
NADP+
-
Homo sapiens
NADPH
-
Homo sapiens