Literature summary for 1.1.1.146 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.

Search for more literature for 1.1.1.146

Application

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(Commentary)

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

Crystallization (Commentary)

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

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

Organism	UniProt	Comment	Textmining
Homo sapiens	P28845	-	-

Purification (Commentary)

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

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
cortisone + NADPH + H+	-	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
NADPH	-	Homo sapiens

IC50 Value

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

Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.

Release 2023.1 (January 2023)