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Literature summary extracted from

  • Tu, H.; Powers, J.P.; Liu, J.; Ursu, S.; Sudom, A.; Yan, X.; Xu, H.; Meininger, D.; Degraffenreid, M.; He, X.; Jaen, J.C.; Sun, D.; Labelle, M.; Yamamoto, H.; Shan, B.; Walker, N.P.; Wang, Z.
    Distinctive molecular inhibition mechanisms for selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1 (2008), Bioorg. Med. Chem., 16, 8922-8931.
    View publication on PubMed

Application

EC Number Application Comment Organism
1.1.1.146 medicine inhibiting 11beta-HSD1 activity signifies a promising therapeutic strategy in the treatment of type 2 diabetes and related diseases Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.146 expressed in in Hi5 cells via a baculovirus protein expression system and in Escherichia coli Rosetta1(DE3) cells Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.1.1.146 sitting drop vapour diffusion method, using 16-18% (w/v) PEG3350 and 0.1 M MES buffer (pH 6.2-6.4) Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.146 1-(((R)-3-methyl-4-(4-((S)-1,1,1-trifluoro-2-hydroxypropan-2-yl)phenylsulfonyl)-piperazin-1-yl)methyl)-cyclopropanecarboxamide substrate competitive inhibitor, specific for 11beta-hydroxysteroid dehydrogenase type 1 Homo sapiens
1.1.1.146 3-(1-(4-fluorophenyl)cyclopropyl)-4-isopropyl-5-(4-(trifluoromethoxy)phenyl)-4H-1,2,4-triazole mixed-type inhibitor, specific for 11beta-hydroxysteroid dehydrogenase type 1 Homo sapiens
1.1.1.146 carbenoxolone specific for 11beta-hydroxysteroid dehydrogenase type 1 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.146 Homo sapiens P28845
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.1.1.146 purified in the presence of CHAPS by Ni+-NTA column chromatography and Superdex 200 gel filtration Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.146 cortisone + NADPH + H+
-
 Homo sapiens cortisol + NADP+
-
 r

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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.146 0.0000012
-
 in PBS buffer, at 37°C Homo sapiens 1-(((R)-3-methyl-4-(4-((S)-1,1,1-trifluoro-2-hydroxypropan-2-yl)phenylsulfonyl)-piperazin-1-yl)methyl)-cyclopropanecarboxamide
1.1.1.146 0.0000016
-
 in PBS buffer, at 37°C Homo sapiens 3-(1-(4-fluorophenyl)cyclopropyl)-4-isopropyl-5-(4-(trifluoromethoxy)phenyl)-4H-1,2,4-triazole