Application | Comment | Organism |
---|---|---|
medicine | inhibiting 11beta-HSD1 activity signifies a promising therapeutic strategy in the treatment of type 2 diabetes and related diseases | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
expressed in in Hi5 cells via a baculovirus protein expression system and in Escherichia coli Rosetta1(DE3) cells | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
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 | Comment | Organism | Structure |
---|---|---|---|
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 | |
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 | |
carbenoxolone | specific for 11beta-hydroxysteroid dehydrogenase type 1 | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P28845 | - |
- |
Purification (Comment) | Organism |
---|---|
purified in the presence of CHAPS by Ni+-NTA column chromatography and Superdex 200 gel filtration | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
cortisone + NADPH + H+ | - |
Homo sapiens | cortisol + NADP+ | - |
r |
Synonyms | Comment | Organism |
---|---|---|
11beta-HSD1 | - |
Homo sapiens |
11beta-hydroxysteroid dehydrogenase type 1 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
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 | |
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 |