| タイトル | Quantitative structural assessment of graded receptor agonism. |
|---|
| ジャーナル・号・ページ | Proc. Natl. Acad. Sci. USA, Vol. 116, Page 22179-22188, Year 2019 |
|---|
| 掲載日 | 2018年5月17日 (構造データの登録日) |
|---|
著者 | Shang, J. / Brust, R. / Griffin, P.R. / Kamenecka, T.M. / Kojetin, D.J. |
|---|
リンク | Proc. Natl. Acad. Sci. USA / PubMed:31611383 |
|---|
| 手法 | X線回折 |
|---|
| 解像度 | 1.95 - 3.1 Å |
|---|
| 構造データ | PDB-6dgl: Crystal Structure of Human PPARgamma Ligand Binding Domain in Complex with Darglitazone 手法: X-RAY DIFFRACTION / 解像度: 1.95 Å PDB-6dgo: Crystal Structure of Human PPARgamma Ligand Binding Domain in Complex with Troglitazone 手法: X-RAY DIFFRACTION / 解像度: 3.1 Å PDB-6dgq: Crystal Structure of Human PPARgamma Ligand Binding Domain in Complex with CAY10506 手法: X-RAY DIFFRACTION / 解像度: 2.45 Å PDB-6dgr: Crystal Structure of Human PPARgamma Ligand Binding Domain in Complex with CAY10638 手法: X-RAY DIFFRACTION / 解像度: 2.15 Å PDB-6o67: Crystal Structure of Human PPARgamma Ligand Binding Domain in Complex with Mitoglitazone 手法: X-RAY DIFFRACTION / 解像度: 2.52 Å PDB-6o68: Crystal Structure of Human PPARgamma Ligand Binding Domain in Complex with Ciglitazone 手法: X-RAY DIFFRACTION / 解像度: 2.78 Å |
|---|
| 化合物 | ChemComp-GEV: (5Z)-5-({4-[3-(5-methyl-2-phenyl-1,3-oxazol-4-yl)propanoyl]phenyl}methylidene)-1,3-thiazolidine-2,4-dione / アゴニスト*YM
ChemComp-GD4: (5S)-5-[(4-{[(2R)-6-hydroxy-2,5,7,8-tetramethyl-3,4-dihydro-2H-1-benzopyran-2-yl]methoxy}phenyl)methyl]-1,3-thiazolidine-2,4-dione / (2R,5S)-トログリタゾン
ChemComp-GBV: N-(2-{4-[(2,4-dioxo-3,4-dihydro-2H-1lambda~4~,3-thiazol-5-yl)methyl]phenoxy}ethyl)-5-[(3R)-1,2-dithiolan-3-yl]pentanamide
ChemComp-GDY: (5Z)-5-({4-[2-(thiophen-2-yl)ethoxy]phenyl}methylidene)-1,3-thiazolidine-2,4-dione
|
|---|
| 由来 | homo sapiens (ヒト)
|
|---|
キーワード | TRANSCRIPTION/TRANSCRIPTION INHIBITOR / Nuclear receptors / TZDs / Drug design / Therapeutic targets / TRANSCRIPTION / TRANSCRIPTION-TRANSCRIPTION INHIBITOR complex |
|---|