タイトル | A structure-guided molecular chaperone approach for restoring the transcriptional activity of the p53 cancer mutant Y220C. |
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ジャーナル・号・ページ | Future Med Chem, Vol. 11, Page 2491-2504, Year 2019 |
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掲載日 | 2018年5月3日 (構造データの登録日) |
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著者 | Bauer, M.R. / Jones, R.N. / Tareque, R.K. / Springett, B. / Dingler, F.A. / Verduci, L. / Patel, K.J. / Fersht, A.R. / Joerger, A.C. / Spencer, J. |
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リンク | Future Med Chem / PubMed:31633398 |
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手法 | X線回折 |
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解像度 | 1.24 - 1.55000123008 Å |
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構造データ | PDB-6gga: p53 cancer mutant Y220C in complex with small-molecule stabilizer PK9284 手法: X-RAY DIFFRACTION / 解像度: 1.55000123008 Å PDB-6ggb: p53 cancer mutant Y220C in complex with small-molecule stabilizer PK9318 手法: X-RAY DIFFRACTION / 解像度: 1.32 Å PDB-6ggc: p53 cancer mutant Y220C in complex with small-molecule stabilizer PK9320 手法: X-RAY DIFFRACTION / 解像度: 1.24 Å PDB-6ggd: p53 cancer mutant Y220C in complex with small-molecule stabilizer PK9324 手法: X-RAY DIFFRACTION / 解像度: 1.4000088608 Å PDB-6gge: p53 cancer mutant Y220C in complex with small-molecule stabilizer PK9327 手法: X-RAY DIFFRACTION / 解像度: 1.25000506704 Å PDB-6ggf: Structure of the p53 cancer mutant Y220C in complex with small-molecule stabilizer PK9328 手法: X-RAY DIFFRACTION / 解像度: 1.32000022323 Å |
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化合物 | ChemComp-EY2: (7-bromanyl-9-ethyl-carbazol-3-yl)methyl-methyl-azanium
ChemComp-EXQ: [9-ethyl-7-(4-methylthiophen-2-yl)carbazol-3-yl]methyl-methyl-azanium
ChemComp-EPE: 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID / HEPES / pH緩衝剤*YM
ChemComp-EXN: [9-ethyl-7-(furan-2-yl)carbazol-3-yl]methyl-methyl-azanium
ChemComp-EYB: [9-ethyl-7-(1,2-oxazol-4-yl)carbazol-3-yl]methyl-methyl-azanium
ChemComp-EYE: [9-ethyl-7-(5-methylthiophen-2-yl)carbazol-3-yl]methyl-methyl-azanium
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由来 | - homo sapiens (ヒト)
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キーワード | DNA BINDING PROTEIN / p53 / transcription factor / tumor supressor / cancer therapy / oncogenic mutant / protein misfolding / small-molecule stabilizer / molecular chaperone |
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