| タイトル | Enhanced cellular death in liver and breast cancer cells by dual BET/BRPF1 inhibitors. |
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| ジャーナル・号・ページ | Protein Sci., Vol. 33, Page e5191-e5191, Year 2024 |
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| 掲載日 | 2023年8月23日 (構造データの登録日) |
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著者 | Cazzanelli, G. / Dalle Vedove, A. / Sbardellati, N. / Valer, L. / Caflisch, A. / Lolli, G. |
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リンク | Protein Sci. / PubMed:39473021 |
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| 手法 | X線回折 |
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| 解像度 | 1.25 - 1.5 Å |
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| 構造データ | PDB-8qal: Crystal Structure of the first bromodomain of BRD4 in complex with acetyl-pyrrole derivative compound 83 手法: X-RAY DIFFRACTION / 解像度: 1.3 Å PDB-8qan: Crystal Structure of the first bromodomain of BRD4 in complex with acetyl-pyrrole derivative compound 79 手法: X-RAY DIFFRACTION / 解像度: 1.25 Å PDB-8qap: Crystal Structure of the first bromodomain of BRD4 in complex with acetyl-pyrrole derivative compound 2 手法: X-RAY DIFFRACTION / 解像度: 1.4 Å PDB-8qar: Crystal Structure of the first bromodomain of BRD4 in complex with acetyl-pyrrole derivative compound 98 手法: X-RAY DIFFRACTION / 解像度: 1.5 Å PDB-8qaz: Crystal Structure of BRPF1 bromodomain in complex with acetyl-pyrrole derivative compound 3 手法: X-RAY DIFFRACTION / 解像度: 1.4 Å PDB-8qb0: Crystal Structure of BRPF1 bromodomain in complex with acetyl-pyrrole derivative compound 2 手法: X-RAY DIFFRACTION / 解像度: 1.45 Å PDB-8qb2: Crystal Structure of BRPF1 bromodomain in complex with acetyl-pyrrole derivative compound 79 手法: X-RAY DIFFRACTION / 解像度: 1.42 Å |
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| 化合物 | ChemComp-GQX: 2-[4-(3-methyl-4-oxidanylidene-2,5,6,7-tetrahydroisoindol-1-yl)-1,3-thiazol-2-yl]guanidine
ChemComp-GKI: 1-[2-methyl-4-(3-methylbutyl)-5-(2-piperazin-1-yl-1,3-thiazol-4-yl)-1~{H}-pyrrol-3-yl]ethanone
ChemComp-GI0: 3-methyl-1-[2-[4-[(4-methyl-1~{H}-pyrazol-3-yl)methyl]piperazin-1-yl]-1,3-thiazol-4-yl]-2,5,6,7-tetrahydroisoindol-4-one
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| 由来 | homo sapiens (ヒト)
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キーワード | TRANSCRIPTION / four helical bundle |
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