3EY4

Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11-hydroxysteroid dehydrogenase type 1 (11-HSD1) inhibitors: Reducing pregnane X receptor (PXR) activity and exploring activity in a monkey pharmacodynamic model

Summary for 3EY4

• Entry DOI: 10.2210/pdb3ey4/pdb
• Related: 2RBE 3BYZ
• Descriptor: 11-beta-Hydroxysteroid Dehydrogenase 1, NADPH DIHYDRO-NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE, (5S)-2-{[(1S)-1-(4-fluorophenyl)ethyl]amino}-5-(1-hydroxy-1-methylethyl)-5-methyl-1,3-thiazol-4(5H)-one (3 entities in total)
• Functional Keywords: endoplasmic reticulum, glycoprotein, lipid metabolism, membrane, nadp, oxidoreductase, polymorphism, signal-anchor, steroid metabolism, transmembrane, alpha beta, 3-layer(aba) sandwich, rossmann fold, nad(p)-binding rossmann-like domain, inhibitor, drug design
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 4
• Total formula weight: 126168.94

Authors

Zhang, J.D.,Jordan, S.R.,Li, V. (deposition date: 2008-10-17, release date: 2008-11-11, Last modification date: 2023-12-27)

• Primary citation: Christopher, F.,Bartberger, M.D.,Bercot, E.A.,Chen, M.,Cupples, R.,Emery, M.,Fretland, J.,Guram, A.,Hale, C.,Han, N.H.,Hickman, D.,Hungate, R.W.,Hayashi, M.,Komorowski, R.,Liu, Q.Y.,Matsumoto, G.,Jean, D.J.St.,Ursu, S.,Voniant, M.,Xu, G.F.,Ye, Q.P.,Yuan, C.,Zhang, J.D.,Zhang, X.P.,Tu, H.,Wang, M.H.; Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11-hydroxysteroid dehydrogenase type 1 (11-HSD1) inhibitors: Reducing pregnane X receptor (PXR) activity and exploring activity in a monkey pharmacodynamic model; To be Published, 2008

Experimental method

X-RAY DIFFRACTION (3 Å)