タイトル | Structural Basis of Inhibitor Selectivity in the BRD7/9 Subfamily of Bromodomains. |
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ジャーナル・号・ページ | J. Med. Chem., Vol. 63, Page 3227-3237, Year 2020 |
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掲載日 | 2019年7月5日 (構造データの登録日) |
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著者 | Karim, R.M. / Chan, A. / Zhu, J.Y. / Schonbrunn, E. |
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リンク | J. Med. Chem. / PubMed:32091206 |
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手法 | X線回折 |
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解像度 | 1.35 - 2.4 Å |
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構造データ | PDB-6ppa: Crystal structure of the unliganded bromodomain of human BRD7 手法: X-RAY DIFFRACTION / 解像度: 1.77 Å PDB-6uzf: Crystal structure of the unliganded bromodomain of human BRD9 手法: X-RAY DIFFRACTION / 解像度: 1.75 Å PDB-6v0q: Crystal structure of the bromodomain of human BRD7 bound to TG003 手法: X-RAY DIFFRACTION / 解像度: 1.69 Å PDB-6v0s: Crystal structure of the bromodomain of human BRD9 bound to TG003 手法: X-RAY DIFFRACTION / 解像度: 2.4 Å PDB-6v0u: Crystal structure of the first bromodomain (BD1) of human BRD4 bound to bromosporine 手法: X-RAY DIFFRACTION / 解像度: 1.4 Å PDB-6v0x: Crystal structure of the bromodomain of human BRD9 bound to sunitinib 手法: X-RAY DIFFRACTION / 解像度: 1.5 Å PDB-6v14: Crystal structure of the bromodomain of human BRD9 bound to TP472 手法: X-RAY DIFFRACTION / 解像度: 1.7 Å PDB-6v16: Crystal structure of the bromodomain of human BRD7 bound to TP472 手法: X-RAY DIFFRACTION / 解像度: 1.9 Å PDB-6v17: Crystal structure of the bromodomain of human BRD7 bound to I-BRD9 手法: X-RAY DIFFRACTION / 解像度: 2.05 Å PDB-6v1b: Crystal structure of the bromodomain of human BRD9 bound to I-BRD9 手法: X-RAY DIFFRACTION / 解像度: 1.35 Å PDB-6v1e: Crystal structure of the bromodomain of human BRD7 bound to BI7273 手法: X-RAY DIFFRACTION / 解像度: 2.3 Å PDB-6v1f: Crystal structure of the bromodomain of human BRD7 bound to BI9564 手法: X-RAY DIFFRACTION / 解像度: 2 Å PDB-6v1h: Crystal structure of the bromodomain of human BRD7 bound to bromosporine 手法: X-RAY DIFFRACTION / 解像度: 1.93 Å PDB-6v1k: Crystal structure of the first bromodomain (BD1) of human BRD4 bound to BI7273 手法: X-RAY DIFFRACTION / 解像度: 1.75 Å PDB-6v1l: Crystal structure of the first bromodomain (BD1) of human BRD4 bound to BI9564 手法: X-RAY DIFFRACTION / 解像度: 2.1 Å PDB-6v1u: Crystal structure of the first bromodomain (BD1) of human BRD4 bound to TP-472 手法: X-RAY DIFFRACTION / 解像度: 1.73 Å |
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化合物 | ChemComp-EAE: (1~{Z})-1-(3-ethyl-5-methoxy-1,3-benzothiazol-2-ylidene)propan-2-one / TG-003
ChemComp-B49: N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carbo / スニチニブ / 薬剤, 抗がん剤, 阻害剤*YM
ChemComp-QMG: 3-(6-acetylpyrrolo[1,2-a]pyrimidin-8-yl)-N-cyclopropyl-4-methylbenzamide
ChemComp-5SW: 4-[4-[(dimethylamino)methyl]-3,5-dimethoxy-phenyl]-2-methyl-2,7-naphthyridin-1-one / BI-7273
ChemComp-5U6: 4-[4-[(dimethylamino)methyl]-2,5-dimethoxy-phenyl]-2-methyl-2,7-naphthyridin-1-one / BI-9564
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由来 | - homo sapiens (ヒト)
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キーワード | GENE REGULATION / BRD7 / PBAF / CELTIX-1 / mSWI/SNF / BP75 / BRD9 / BAF / TG003 / non-BET / BRD / Bromosporine / BRD4 / BET / Sunitinib / TP472 / TP-472 / bromodomain / CELTIX1 / Rhabdomyosarcoma antigen / I-BRD9 / IBRD9 / inhibitor / BI7273 / BI9564 / HUNK1 |
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