4DIJ
| |
4HBM
| Ordering of the N Terminus of Human MDM2 by Small Molecule Inhibitors | 分子名称: | E3 ubiquitin-protein ligase Mdm2, {(3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-[(2S)-1-hydroxybutan-2-yl]-2-oxopiperidin-3-yl}acetic acid | 著者 | Huang, X. | 登録日 | 2012-09-28 | 公開日 | 2012-10-17 | 最終更新日 | 2024-02-28 | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | 主引用文献 | Ordering of the N-terminus of human MDM2 by small molecule inhibitors. J.Am.Chem.Soc., 134, 2012
|
|
1T4F
| Structure of human MDM2 in complex with an optimized p53 peptide | 分子名称: | SULFATE ION, Ubiquitin-protein ligase E3 Mdm2, optimized p53 peptide | 著者 | Grasberger, B.L, Schubert, C, Koblish, H.K, Carver, T.E, Franks, C.F, Zhao, S.Y, Lu, T, LaFrance, L.V, Parks, D.J. | 登録日 | 2004-04-29 | 公開日 | 2005-02-08 | 最終更新日 | 2023-08-23 | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | 主引用文献 | Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells J.Med.Chem., 48, 2005
|
|
4JRG
| The 1.9A crystal structure of humanized Xenopus MDM2 with RO5313109 - a pyrrolidine MDM2 inhibitor | 分子名称: | (3R,4R,5S)-3-(3-chlorophenyl)-4-(4-chlorophenyl)-4-cyano-N-[(3S)-3,4-dihydroxybutyl]-5-(2,2-dimethylpropyl)-D-prolinamide, E3 ubiquitin-protein ligase Mdm2 | 著者 | Graves, B.J, Janson, C.A, Lukacs, C. | 登録日 | 2013-03-21 | 公開日 | 2013-07-24 | 最終更新日 | 2024-02-28 | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | 主引用文献 | Discovery of RG7388, a Potent and Selective p53-MDM2 Inhibitor in Clinical Development. J.Med.Chem., 56, 2013
|
|
4MDN
| Structure of a novel submicromolar MDM2 inhibitor | 分子名称: | 3-{(1S)-2-(tert-butylamino)-1-[{4-[(4-chlorobenzyl)oxy]benzyl}(formyl)amino]-2-oxoethyl}-6-chloro-1H-indole-2-carboxylic acid, E3 ubiquitin-protein ligase Mdm2, SULFATE ION | 著者 | Bista, M, Popowicz, G, Holak, T.A. | 登録日 | 2013-08-23 | 公開日 | 2013-11-13 | 最終更新日 | 2024-02-28 | 実験手法 | X-RAY DIFFRACTION (1.905 Å) | 主引用文献 | Transient Protein States in Designing Inhibitors of the MDM2-p53 Interaction. Structure, 21, 2013
|
|
4J3E
| The 1.9A crystal structure of humanized Xenopus Mdm2 with nutlin-3a | 分子名称: | 4-({(4S,5R)-4,5-bis(4-chlorophenyl)-2-[4-methoxy-2-(propan-2-yloxy)phenyl]-4,5-dihydro-1H-imidazol-1-yl}carbonyl)piperazin-2-one, E3 ubiquitin-protein ligase Mdm2, SULFATE ION | 著者 | Graves, B.J, Lukacs, C.M, Kammlott, R.U, Crowther, R. | 登録日 | 2013-02-05 | 公開日 | 2013-04-24 | 最終更新日 | 2024-02-28 | 実験手法 | X-RAY DIFFRACTION (1.91 Å) | 主引用文献 | Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. ACS Med Chem Lett, 4, 2013
|
|
5SWK
| |
3IWY
| |
3LNZ
| |
4ZYC
| |
4UMN
| Structure of a stapled peptide antagonist bound to Nutlin-resistant Mdm2. | 分子名称: | E3 ubiquitin-protein ligase Mdm2, M06 | 著者 | Chee, S, Wongsantichon, J, Quah, S, Robinson, R.C, Verma, C, Lane, D.P, Brown, C.J, Ghadessy, F.J. | 登録日 | 2014-05-20 | 公開日 | 2014-05-28 | 最終更新日 | 2024-02-07 | 実験手法 | X-RAY DIFFRACTION (1.99 Å) | 主引用文献 | Structure of a stapled peptide antagonist bound to nutlin-resistant Mdm2. PLoS ONE, 9, 2014
|
|
6GGN
| In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor | 分子名称: | (4~{S})-4-(4-chloranyl-2-methyl-phenyl)-5-(5-chloranyl-2-methyl-phenyl)-2-(2,4-dimethoxypyrimidin-5-yl)-3-propan-2-yl-4~{H}-pyrrolo[3,4-d]imidazol-6-one, CHLORIDE ION, E3 ubiquitin-protein ligase Mdm2 | 著者 | Kallen, J. | 登録日 | 2018-05-03 | 公開日 | 2018-09-26 | 最終更新日 | 2024-01-17 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor. Bioorg. Med. Chem. Lett., 28, 2018
|
|
4ZFI
| Structure of Mdm2 with low molecular weight inhibitor | 分子名称: | (5S)-3,5-bis(4-chlorobenzyl)-4-(6-chloro-1H-indol-3-yl)-5-hydroxy-1-methyl-1,5-dihydro-2H-pyrrol-2-one, E3 ubiquitin-protein ligase Mdm2 | 著者 | Zak, K.M, Twarda-Clapa, A, Wrona, E.M, Grudnik, P, Dubin, G, Holak, T.A. | 登録日 | 2015-04-21 | 公開日 | 2016-10-19 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | A Unique Mdm2-Binding Mode of the 3-Pyrrolin-2-one- and 2-Furanone-Based Antagonists of the p53-Mdm2 Interaction. ACS Chem. Biol., 11, 2016
|
|
6Q9H
| |
7BJ0
| Inhibitor of MDM2-p53 Interaction | 分子名称: | (3~{R})-4-chloranyl-3-(4-chlorophenyl)-3-[[1-(hydroxymethyl)cyclopropyl]methoxy]-2-[(4-nitrophenyl)methyl]isoindol-1-one, E3 ubiquitin-protein ligase Mdm2 | 著者 | Williams, P.A. | 登録日 | 2021-01-13 | 公開日 | 2021-04-07 | 最終更新日 | 2021-04-21 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein-Protein Interaction. J.Med.Chem., 64, 2021
|
|
4ZGK
| Structure of Mdm2 with low molecular weight inhibitor. | 分子名称: | (5R)-3,5-bis(4-chlorobenzyl)-4-(6-chloro-1H-indol-3-yl)-5-hydroxyfuran-2(5H)-one, E3 ubiquitin-protein ligase Mdm2 | 著者 | Twarda-Clapa, A, Zak, K.M, Wrona, E.M, Grudnik, P, Dubin, G, Holak, T.A. | 登録日 | 2015-04-23 | 公開日 | 2016-10-19 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | A Unique Mdm2-Binding Mode of the 3-Pyrrolin-2-one- and 2-Furanone-Based Antagonists of the p53-Mdm2 Interaction. ACS Chem. Biol., 11, 2016
|
|
6AAW
| Mdm2 in complex with a D amino Acid Containing Stapled Peptide | 分子名称: | ACE-LEU-THR-PHE-STQ-GLU-TYR-DTR-GLN-LEU-CBA-MK8-SER-ALA-ALA, E3 ubiquitin-protein ligase Mdm2 | 著者 | Brown, C.J, Partridge, A.W. | 登録日 | 2018-07-19 | 公開日 | 2019-07-24 | 最終更新日 | 2023-11-29 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | A Model System to Explore Macrocyclic Peptide Structural and Chirality Relationships: Tolerance of helix-breaking residues within the context of a stapled peptide. To Be Published
|
|
5J7F
| Structure of MDM2 with low molecular weight inhibitor with aliphatic linker. | 分子名称: | 4-({6-[(6-chloro-3-{1-[(4-chlorophenyl)methyl]-4-(4-fluorophenyl)-1H-imidazol-5-yl}-1H-indole-2-carbonyl)oxy]hexyl}amino)-4-oxobutanoic acid, E3 ubiquitin-protein ligase Mdm2 | 著者 | Twarda-Clapa, A, Kubica, K, Guzik, K, Dubin, G, Holak, T.A. | 登録日 | 2016-04-06 | 公開日 | 2017-05-17 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers. J. Med. Chem., 60, 2017
|
|
3V3B
| Structure of the Stapled p53 Peptide Bound to Mdm2 | 分子名称: | CHLORIDE ION, E3 ubiquitin-protein ligase Mdm2, SAH-p53-8 stapled-peptide | 著者 | Baek, S, Kutchukian, P.S, Verdine, G.L, Huber, R, Holak, T.A, Ki Won, L, Popowicz, G.M. | 登録日 | 2011-12-13 | 公開日 | 2012-01-18 | 最終更新日 | 2023-11-15 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Structure of the stapled p53 peptide bound to Mdm2. J.Am.Chem.Soc., 134, 2012
|
|
5OAI
| Structure of MDM2 with low molecular weight inhibitor | 分子名称: | 3-[(1~{R})-2-(~{tert}-butylamino)-1-[methanoyl-[[3,4,5-tris(fluoranyl)phenyl]methyl]amino]-2-oxidanylidene-ethyl]-6-chloranyl-1~{H}-indole-2-carboxylic acid, E3 ubiquitin-protein ligase Mdm2 | 著者 | Twarda-Clapa, A, Neochoritis, C.G, Grudnik, P, Dubin, G, Domling, A, Holak, T.A. | 登録日 | 2017-06-22 | 公開日 | 2019-02-13 | 最終更新日 | 2024-01-17 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | A fluorinated indole-based MDM2 antagonist selectively inhibits the growth of p53wtosteosarcoma cells. Febs J., 286, 2019
|
|
8AEU
| Structure of hMDM2 in complex with Nutlin-3a-aa | 分子名称: | 4-[[(4~{S},5~{R})-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxy-phenyl)-4,5-dihydroimidazol-1-yl]carbonyl]-3-methylidene-piperazin-2-one, BETA-MERCAPTOETHANOL, E3 ubiquitin-protein ligase Mdm2 | 著者 | Labuzek, B, Golik, P, Magiera-Mularz, K, Berg, T. | 登録日 | 2022-07-13 | 公開日 | 2023-01-18 | 最終更新日 | 2024-02-07 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Nutlin-3a-aa: Improving the Bioactivity of a p53/MDM2 Interaction Inhibitor by Introducing a Solvent-Exposed Methylene Group. Chembiochem, 24, 2023
|
|
4ERF
| crystal structure of MDM2 (17-111) in complex with compound 29 (AM-8553) | 分子名称: | E3 ubiquitin-protein ligase Mdm2, {(3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-[(2S,3S)-2-hydroxypentan-3-yl]-3-methyl-2-oxopiperidin-3-yl}acetic acid | 著者 | Huang, X. | 登録日 | 2012-04-20 | 公開日 | 2012-05-23 | 最終更新日 | 2024-02-28 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Structure-based design of novel inhibitors of the MDM2-p53 interaction. J.Med.Chem., 55, 2012
|
|
6H22
| Crystal structure of Mdm2 bound to a stapled peptide | 分子名称: | 12-(dimethylamino)-3,10-diethyl-N,N,N-trimethyl-3,10-dihydrodibenzo[3,4:7,8]cycloocta[1,2-d:5,6-d']bis([1,2,3]triazole)-5-aminium, E3 ubiquitin-protein ligase Mdm2, Stapled peptide | 著者 | Wang, X, Sharma, K, Spring, D.R, Hyvonen, M. | 登録日 | 2018-07-12 | 公開日 | 2019-07-31 | 最終更新日 | 2019-09-11 | 実験手法 | X-RAY DIFFRACTION (2.006 Å) | 主引用文献 | Water-soluble, stable and azide-reactive strained dialkynes for biocompatible double strain-promoted click chemistry. Org.Biomol.Chem., 17, 2019
|
|
7BIR
| Inhibitor of MDM2-p53 Interaction | 分子名称: | 1-[[(1~{R})-2-[(5-chloranylpyridin-2-yl)methyl]-1-(4-chlorophenyl)-7-fluoranyl-3-oxidanylidene-5-(2-oxidanylpropan-2-yl)isoindol-1-yl]oxymethyl]cyclopropane-1-carboxamide, E3 ubiquitin-protein ligase Mdm2, SULFATE ION | 著者 | Williams, P.A. | 登録日 | 2021-01-13 | 公開日 | 2021-04-07 | 最終更新日 | 2021-04-21 | 実験手法 | X-RAY DIFFRACTION (2.02 Å) | 主引用文献 | Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein-Protein Interaction. J.Med.Chem., 64, 2021
|
|
7AD0
| X-ray structure of Mdm2 with modified p53 peptide | 分子名称: | E3 ubiquitin-protein ligase Mdm2, Modified p53 peptide | 著者 | Twarda-Clapa, A, Fortuna, P, Grudnik, P, Dubin, G, Berlicki, L, Holak, T.A. | 登録日 | 2020-09-13 | 公開日 | 2020-10-28 | 最終更新日 | 2024-01-31 | 実験手法 | X-RAY DIFFRACTION (2.07 Å) | 主引用文献 | Systematic ""foldamerization"" of peptide inhibiting p53-MDM2/X interactions by the incorporation of trans- or cis-2-aminocyclopentanecarboxylic acid residues Eur.J.Med.Chem., 208, 2020
|
|