| タイトル | Discovery of Acylsulfonohydrazide-Derived Inhibitors of the Lysine Acetyltransferase, KAT6A, as Potent Senescence-Inducing Anti-Cancer Agents. |
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| ジャーナル・号・ページ | J. Med. Chem., Vol. 63, Page 4655-4684, Year 2020 |
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| 掲載日 | 2019年5月9日 (構造データの登録日) |
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著者 | Priebbenow, D.L. / Leaver, D.J. / Nguyen, N. / Cleary, B. / Lagiakos, H.R. / Sanchez, J. / Xue, L. / Huang, F. / Sun, Y. / Mujumdar, P. ...Priebbenow, D.L. / Leaver, D.J. / Nguyen, N. / Cleary, B. / Lagiakos, H.R. / Sanchez, J. / Xue, L. / Huang, F. / Sun, Y. / Mujumdar, P. / Mudududdla, R. / Varghese, S. / Teguh, S. / Charman, S.A. / White, K.L. / Shackleford, D.M. / Katneni, K. / Cuellar, M. / Strasser, J.M. / Dahlin, J.L. / Walters, M.A. / Street, I.P. / Monahan, B.J. / Jarman, K.E. / Jousset Sabroux, H. / Falk, H. / Chung, M.C. / Hermans, S.J. / Downer, N.L. / Parker, M.W. / Voss, A.K. / Thomas, T. / Baell, J.B. |
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リンク | J. Med. Chem. / PubMed:32118427 |
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| 手法 | X線回折 |
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| 解像度 | 1.75 - 2.8 Å |
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| 構造データ | PDB-6owh: Crystal structure of MYST acetyltransferase domain in complex with inhibitor 92 手法: X-RAY DIFFRACTION / 解像度: 2 Å PDB-6owi: Crystal structure of MYST acetyltransferase domain in complex with inhibitor 85 手法: X-RAY DIFFRACTION / 解像度: 1.75 Å PDB-6pd8: Crystal structure of MYST acetyltransferase domain in complex with inhibitor 39 手法: X-RAY DIFFRACTION / 解像度: 2.738 Å PDB-6pd9: Crystal structure of MYST acetyltransferase domain in complex with inhibitor 60 手法: X-RAY DIFFRACTION / 解像度: 2.8 Å PDB-6pda: Crystal structure of MYST acetyltransferase domain in complex with inhibitor 74 手法: X-RAY DIFFRACTION / 解像度: 2.448 Å PDB-6pdb: Crystal structure of MYST acetyltransferase domain in complex with inhibitor 80 手法: X-RAY DIFFRACTION / 解像度: 2.42 Å PDB-6pdc: Crystal structure of MYST acetyltransferase domain in complex with inhibitor 42 手法: X-RAY DIFFRACTION / 解像度: 1.96 Å PDB-6pdd: Crystal structure of MYST acetyltransferase domain in complex with inhibitor 41 手法: X-RAY DIFFRACTION / 解像度: 2.15 Å PDB-6pde: Crystal structure of MYST acetyltransferase domain in complex with inhibitor 40 手法: X-RAY DIFFRACTION / 解像度: 2.22 Å PDB-6pdf: Crystal structure of MYST acetyltransferase domain in complex with inhibitor 55 手法: X-RAY DIFFRACTION / 解像度: 2.22 Å PDB-6pdg: Crystal structure of MYST acetyltransferase domain in complex with inhibitor 83 手法: X-RAY DIFFRACTION / 解像度: 1.919 Å |
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| 化合物 | ChemComp-NBJ: N'-[(2-fluorophenyl)sulfonyl]-3-iodobenzohydrazide
ChemComp-NB7: N'-[(2-fluorophenyl)sulfonyl]benzohydrazide
ChemComp-O9D: 5-ethoxy-2-fluoro-3-methyl-N'-(phenylsulfonyl)benzohydrazide
ChemComp-O9G: 2-fluoro-3-methyl-N'-(phenylsulfonyl)-5-(1H-pyrazol-1-yl)benzohydrazide
ChemComp-O9J: 2-fluoro-3-methyl-N'-(phenylsulfonyl)-5-(pyridin-2-yl)benzohydrazide
ChemComp-O9M: 2-fluoro-3-methyl-N'-(phenylsulfonyl)-5-(pyrimidin-2-yl)benzohydrazide
ChemComp-O9P: 2-fluoro-3-methyl-N'-(phenylsulfonyl)-5-[(prop-2-en-1-yl)oxy]benzohydrazide
ChemComp-O9S: 2-fluoro-3-methyl-N'-(phenylsulfonyl)-5-[(propan-2-yl)oxy]benzohydrazide
ChemComp-O9V: 2-fluoro-3-methyl-N'-(phenylsulfonyl)-5-propoxybenzohydrazide
ChemComp-O9Y: 2-fluoro-3-methyl-N'-(phenylsulfonyl)-5-(2H-1,2,3-triazol-2-yl)benzohydrazide
ChemComp-O9A: 5-ethoxy-2-fluoro-3-methyl-N'-[(naphthalen-2-yl)sulfonyl]benzohydrazide
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| 由来 | homo sapiens (ヒト)
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キーワード | TRANSFERASE/TRANSFERASE INHIBITOR / Inhibitor / Complex / MYST / TRANSFERASE / TRANSFERASE-TRANSFERASE INHIBITOR complex / TRANSFERASE/TRANSERASE INHIBITOR / TRANSFERASE-TRANSERASE INHIBITOR complex |
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