3BYZ
2-Amino-1,3-thiazol-4(5H)-ones as Potent and Selective 11-Hydroxysteroid Dehydrogenase Type 1 Inhibitors
3BYZ の概要
エントリーDOI | 10.2210/pdb3byz/pdb |
関連するPDBエントリー | 2RBE |
分子名称 | Corticosteroid 11-beta-dehydrogenase isozyme 1, NADPH DIHYDRO-NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE, (5S)-2-(cyclooctylamino)-5-methyl-5-propyl-1,3-thiazol-4(5H)-one (3 entities in total) |
機能のキーワード | alpha beta, 3-layer (aba) sandwich, rossmann fold, nad(p)-binding rossmann-like domain. amino thiazole inhibitor, endoplasmic reticulum, glycoprotein, lipid metabolism, membrane, microsome, nadp, oxidoreductase, polymorphism, signal-anchor, steroid metabolism, transmembrane, ---- |
由来する生物種 | Homo sapiens (human) |
細胞内の位置 | Endoplasmic reticulum membrane; Single-pass type II membrane protein: P28845 |
タンパク質・核酸の鎖数 | 4 |
化学式量合計 | 126057.17 |
構造登録者 | |
主引用文献 | Johansson, L.,Fotsch, C.,Bartberger, M.D.,Castro, V.M.,Chen, M.,Emery, M.,Gustafsson, S.,Hale, C.,Hickman, D.,Homan, E.,Jordan, S.R.,Komorowski, R.,Li, A.,McRae, K.,Moniz, G.,Matsumoto, G.,Orihuela, C.,Palm, G.,Veniant, M.,Wang, M.,Williams, M.,Zhang, J. 2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice. J.Med.Chem., 51:2933-2943, 2008 Cited by PubMed: 18419108DOI: 10.1021/jm701551j 主引用文献が同じPDBエントリー |
実験手法 | X-RAY DIFFRACTION (2.69 Å) |
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