3VZV
| Crystal structure of human mdm2 with a dihydroimidazothiazole inhibitor | Descriptor: | 1-{[(5R,6S)-5,6-bis(4-chlorophenyl)-6-methyl-3-(propan-2-yl)-5,6-dihydroimidazo[2,1-b][1,3]thiazol-2-yl]carbonyl}-N,N-dimethyl-L-prolinamide, E3 ubiquitin-protein ligase Mdm2 | Authors: | Shimizu, H, Katakura, S, Miyazaki, M, Naito, H, Sugimoto, Y, Kawato, H, Okayama, T, Soga, T. | Deposit date: | 2012-10-16 | Release date: | 2013-02-06 | Last modified: | 2024-03-20 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Lead optimization of novel p53-MDM2 interaction inhibitors possessing dihydroimidazothiazole scaffold Bioorg.Med.Chem.Lett., 23, 2013
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3W69
| Crystal structure of human mdm2 with a dihydroimidazothiazole inhibitor | Descriptor: | (5R,6S)-2-[((2S,5R)-2-{[(3R)-4-acetyl-3-methylpiperazin-1-yl]carbonyl}-5-ethylpyrrolidin-1-yl)carbonyl]-5,6-bis(4-chlorophenyl)-3-isopropyl-6-methyl-5,6-dihydroimidazo[2,1-b][1,3]thiazole, E3 ubiquitin-protein ligase Mdm2, SULFATE ION | Authors: | Shimizu, H, Katakura, S, Miyazaki, M, Naito, H, Sugimoto, Y, Kawato, H, Okayama, T, Soga, T. | Deposit date: | 2013-02-12 | Release date: | 2013-06-05 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Synthesis and evaluation of novel orally active p53-MDM2 interaction inhibitors Bioorg.Med.Chem., 21, 2013
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1T4F
| Structure of human MDM2 in complex with an optimized p53 peptide | Descriptor: | SULFATE ION, Ubiquitin-protein ligase E3 Mdm2, optimized p53 peptide | Authors: | 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. | Deposit date: | 2004-04-29 | Release date: | 2005-02-08 | Last modified: | 2023-08-23 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells J.Med.Chem., 48, 2005
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8EBK
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8F13
| Structure of the MDM2 P53 binding domain in complex with H103, an all-D Helicon Polypeptide, alternative C-terminus | Descriptor: | 1,2-ETHANEDIOL, DIMETHYL SULFOXIDE, E3 ubiquitin-protein ligase Mdm2, ... | Authors: | Li, K, Callahan, A.J, Travaline, T.L, Tokareva, O.S, Swiecicki, J.-M, Verdine, G.L, Pentelute, B.L, McGee, J.H. | Deposit date: | 2022-11-04 | Release date: | 2023-02-15 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (1.4 Å) | Cite: | Single-Shot Flow Synthesis of D-Proteins for Mirror-Image Phage Display Chemrxiv, 2023
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8F12
| Structure of the MDM2 P53 binding domain in complex with H103, an all-D Helicon Polypeptide | Descriptor: | CHLORIDE ION, E3 ubiquitin-protein ligase Mdm2, H103, ... | Authors: | Li, K, Callahan, A.J, Travaline, T.L, Tokareva, O.S, Swiecicki, J.-M, Verdine, G.L, Pentelute, B.L, McGee, J.H. | Deposit date: | 2022-11-04 | Release date: | 2023-02-15 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (1.86 Å) | Cite: | Single-Shot Flow Synthesis of D-Proteins for Mirror-Image Phage Display Chemrxiv, 2023
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8F10
| Structure of the MDM2 P53 binding domain in complex with H102, an all-D Helicon Polypeptide | Descriptor: | 1,2-ETHANEDIOL, CHLORIDE ION, E3 ubiquitin-protein ligase Mdm2, ... | Authors: | Li, K, Callahan, A.J, Travaline, T.L, Tokareva, O.S, Swiecicki, J.-M, Verdine, G.L, Pentelute, B.L, McGee, J.H. | Deposit date: | 2022-11-04 | Release date: | 2023-02-15 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (1.28 Å) | Cite: | Single-Shot Flow Synthesis of D-Proteins for Mirror-Image Phage Display Chemrxiv, 2023
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8F0Z
| Structure of the MDM2 P53 binding domain in complex with H101, an all-D Helicon Polypeptide | Descriptor: | CHLORIDE ION, E3 ubiquitin-protein ligase Mdm2, H101, ... | Authors: | Li, K, Callahan, A.J, Travaline, T.L, Tokareva, O.S, Swiecicki, J.-M, Verdine, G.L, Pentelute, B.L, McGee, J.H. | Deposit date: | 2022-11-04 | Release date: | 2023-02-15 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (1.61 Å) | Cite: | Single-Shot Flow Synthesis of D-Proteins for Mirror-Image Phage Display Chemrxiv, 2023
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8GJS
| Stapled Peptide ALRN-6924 Bound to MDMX | Descriptor: | ACE-LEU-THR-PHE-ALA-GLU-TYR-TRP-ALA-GLN-LEU-DAL-ALA-ALA-ALA-ALA-ALA-DAL, Protein Mdm4 | Authors: | Graves, B.J, Janson, C, Lukacs, C. | Deposit date: | 2023-03-16 | Release date: | 2023-07-26 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (1.75 Å) | Cite: | Discovery of Sulanemadlin (ALRN-6924), the First Cell-Permeating, Stabilized alpha-Helical Peptide in Clinical Development. J.Med.Chem., 66, 2023
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4MDQ
| Structure of a novel submicromolar MDM2 inhibitor | Descriptor: | 3-[(1R)-2-(benzylamino)-1-{[(2S)-1-(hydroxyamino)-4-methyl-1-oxopentan-2-yl]amino}-2-oxoethyl]-6-chloro-N-hydroxy-1H-indole-2-carboxamide, E3 ubiquitin-protein ligase Mdm2 | Authors: | Bista, M, Popowicz, G, Holak, T.A. | Deposit date: | 2013-08-23 | Release date: | 2013-11-13 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.119 Å) | Cite: | Transient Protein States in Designing Inhibitors of the MDM2-p53 Interaction. Structure, 21, 2013
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4LWU
| The 1.14A Crystal Structure of Humanized Xenopus MDM2 with RO5499252 | Descriptor: | (2'S,3R,4'S,5'R)-N-(4-carbamoylphenyl)-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-2-oxo-1,2-dihydrospiro[indole-3,3'-pyrrolidine]-5'-carboxamide, E3 ubiquitin-protein ligase Mdm2, SULFATE ION | Authors: | Graves, B.J, Lukacs, C, Janson, C.A. | Deposit date: | 2013-07-28 | Release date: | 2014-07-16 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (1.14 Å) | Cite: | Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. Bioorg.Med.Chem., 22, 2014
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4OAS
| co-crystal structure of MDM2 (17-111) in complex with compound 25 | Descriptor: | E3 ubiquitin-protein ligase Mdm2, SULFATE ION, [(3R,5R,6S)-1-[(2S)-1-(tert-butylsulfonyl)butan-2-yl]-5-(3-chlorophenyl)-6-(4-chlorophenyl)-3-methyl-2-oxopiperidin-3-yl]acetic acid | Authors: | Huang, X. | Deposit date: | 2014-01-06 | Release date: | 2014-02-19 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (1.7 Å) | Cite: | Discovery of AMG 232, a Potent, Selective, and Orally Bioavailable MDM2-p53 Inhibitor in Clinical Development. J.Med.Chem., 57, 2014
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4ODE
| Co-Crystal Structure of MDM2 with Inhibitor Compound 4 | Descriptor: | (2-{[(3R,5R,6S)-1-[(1S)-2-(tert-butylsulfonyl)-1-cyclopropylethyl]-6-(4-chloro-3-fluorophenyl)-5-(3-chlorophenyl)-3-methyl-2-oxopiperidin-3-yl]methyl}-1,3-thiazol-5-yl)acetic acid, E3 ubiquitin-protein ligase Mdm2, SULFATE ION | Authors: | Shaffer, P.L, Huang, X, Yakowec, P, Long, A.M. | Deposit date: | 2014-01-10 | Release date: | 2014-04-02 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Novel Inhibitors of the MDM2-p53 Interaction Featuring Hydrogen Bond Acceptors as Carboxylic Acid Isosteres. J.Med.Chem., 57, 2014
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4OGV
| Co-Crystal Structure of MDM2 with Inhibitor Compound 49 | Descriptor: | E3 ubiquitin-protein ligase Mdm2, [(2S,5R,6R)-4-[(2S)-1-(tert-butylsulfonyl)butan-2-yl]-6-(3-chlorophenyl)-5-(4-chlorophenyl)-3-oxomorpholin-2-yl]acetic acid | Authors: | Shaffer, P.L, Huang, X, Yakowec, P, Long, A.M. | Deposit date: | 2014-01-16 | Release date: | 2014-04-02 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.197 Å) | Cite: | Novel Inhibitors of the MDM2-p53 Interaction Featuring Hydrogen Bond Acceptors as Carboxylic Acid Isosteres. J.Med.Chem., 57, 2014
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4OGN
| Co-Crystal Structure of MDM2 with Inhbitor Compound 3 | Descriptor: | 6-{[(3R,5R,6S)-1-[(1S)-2-(tert-butylsulfonyl)-1-cyclopropylethyl]-5-(3-chlorophenyl)-6-(4-chlorophenyl)-3-methyl-2-oxopiperidin-3-yl]methyl}pyridine-3-carboxylic acid, E3 ubiquitin-protein ligase Mdm2, SULFATE ION | Authors: | Shaffer, P.L, Huang, X, Yakowec, P, Long, A.M. | Deposit date: | 2014-01-16 | Release date: | 2014-04-02 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (1.377 Å) | Cite: | Novel Inhibitors of the MDM2-p53 Interaction Featuring Hydrogen Bond Acceptors as Carboxylic Acid Isosteres. J.Med.Chem., 57, 2014
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4OGT
| Co-Crystal Structure of MDM2 with Inhbitor Compound 46 | Descriptor: | 6-{[(2R,5R,6R)-4-[(1S)-2-(tert-butylsulfonyl)-1-cyclopropylethyl]-6-(3-chlorophenyl)-5-(4-chlorophenyl)-2-methyl-3-oxomorpholin-2-yl]methyl}pyridine-3-carboxylic acid, E3 ubiquitin-protein ligase Mdm2, SULFATE ION | Authors: | Shaffer, P.L, Huang, X, Yakowec, P, Long, A.M. | Deposit date: | 2014-01-16 | Release date: | 2014-04-02 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (1.5361 Å) | Cite: | Novel Inhibitors of the MDM2-p53 Interaction Featuring Hydrogen Bond Acceptors as Carboxylic Acid Isosteres. J.Med.Chem., 57, 2014
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4LWT
| The 1.6A Crystal Structure of Humanized Xenopus MDM2 with RO5027344 | Descriptor: | (3S)-3-[(3R)-1-acetylpiperidin-3-yl]-6-chloro-3-(3-chlorobenzyl)-1,3-dihydro-2H-indol-2-one, E3 ubiquitin-protein ligase Mdm2, SULFATE ION | Authors: | Graves, B.J, Lukacs, C, Kammlott, U. | Deposit date: | 2013-07-28 | Release date: | 2014-07-16 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (1.6 Å) | Cite: | Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. Bioorg.Med.Chem., 22, 2014
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4N5T
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4OBA
| Co-crystal structure of MDM2 with Inhibitor Compound 4 | Descriptor: | E3 ubiquitin-protein ligase Mdm2, [(2R,5R,6R)-4-[(1S)-2-(tert-butylsulfonyl)-1-cyclopropylethyl]-6-(3-chlorophenyl)-5-(4-chlorophenyl)-3-oxomorpholin-2-yl]acetic acid | Authors: | Shaffer, P.L, Huang, X, Yakowec, P, Long, A.M. | Deposit date: | 2014-01-07 | Release date: | 2014-03-19 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (1.602 Å) | Cite: | Selective and Potent Morpholinone Inhibitors of the MDM2-p53 Protein-Protein Interaction. J.Med.Chem., 57, 2014
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4OCC
| co-crystal structure of MDM2(17-111) in complex with compound 48 | Descriptor: | E3 ubiquitin-protein ligase Mdm2, [(2R,5R,6R)-4-[(2S)-1-(tert-butylsulfonyl)butan-2-yl]-6-(3-chlorophenyl)-5-(4-chlorophenyl)-3-oxomorpholin-2-yl]acetic acid | Authors: | Huang, X. | Deposit date: | 2014-01-08 | Release date: | 2014-04-02 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Novel Inhibitors of the MDM2-p53 Interaction Featuring Hydrogen Bond Acceptors as Carboxylic Acid Isosteres. J.Med.Chem., 57, 2014
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4ODF
| Co-Crystal Structure of MDM2 with Inhibitor Compound 47 | Descriptor: | 6-{[(2S,5R,6R)-4-[(1S)-2-(tert-butylsulfonyl)-1-cyclopropylethyl]-6-(3-chlorophenyl)-5-(4-chlorophenyl)-2-methyl-3-oxomorpholin-2-yl]methyl}pyridine-3-carboxylic acid, E3 ubiquitin-protein ligase Mdm2 | Authors: | Shaffer, P.L, Huang, X, Yakowec, P, Long, A.M. | Deposit date: | 2014-01-10 | Release date: | 2014-04-02 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.2006 Å) | Cite: | Novel Inhibitors of the MDM2-p53 Interaction Featuring Hydrogen Bond Acceptors as Carboxylic Acid Isosteres. J.Med.Chem., 57, 2014
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4OQ3
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4JSC
| The 2.5A crystal structure of humanized Xenopus MDM2 with RO5316533 - a pyrrolidine MDM2 inhibitor | Descriptor: | (3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-N-[(3S)-3,4-dihydroxybutyl]-5-(2,2-dimethylpropyl)-D-prolinamide, E3 ubiquitin-protein ligase Mdm2 | Authors: | Janson, C.A, Lukacs, C, Graves, B. | Deposit date: | 2013-03-22 | Release date: | 2013-07-24 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Discovery of RG7388, a Potent and Selective p53-MDM2 Inhibitor in Clinical Development. J.Med.Chem., 56, 2013
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4JV7
| Co-crystal structure of MDM2 with inhibitor (2S,5R,6S)-2-benzyl-5,6-bis(4-bromophenyl)-4-methylmorpholin-3-one | Descriptor: | (2S,5R,6S)-2-benzyl-5,6-bis(4-bromophenyl)-4-methylmorpholin-3-one, E3 ubiquitin-protein ligase Mdm2, SULFATE ION | Authors: | Huang, X, Gonzalez-Lopez de Turiso, F, Sun, D, Yosup, R, Bartberger, M.D, Beck, H.P, Cannon, J, Shaffer, P, Oliner, J.D, Olson, S.H, Medina, J.C. | Deposit date: | 2013-03-25 | Release date: | 2013-05-01 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Rational Design and Binding Mode Duality of MDM2-p53 Inhibitors. J.Med.Chem., 56, 2013
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4JVR
| Co-crystal structure of MDM2 with inhibitor (2'S,3R,4'S,5'R)-N-(2-aminoethyl)-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-2-oxo-1,2-dihydrospiro[indole-3,3'-pyrrolidine]-5'-carboxamide | Descriptor: | (2'S,3R,4'S,5'R)-N-(2-aminoethyl)-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-2-oxo-1,2-dihydrospiro[indole-3,3'-pyrrolidine]-5'-carboxamide, E3 ubiquitin-protein ligase Mdm2 | Authors: | Huang, X, Gonzalez-Lopez de Turiso, F, Sun, D, Yosup, R, Bartberger, M.D, Beck, H.P, Cannon, J, Shaffer, P, Oliner, J.D, Olson, S.H, Medina, J.C. | Deposit date: | 2013-03-26 | Release date: | 2013-05-01 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (1.7 Å) | Cite: | Rational Design and Binding Mode Duality of MDM2-p53 Inhibitors. J.Med.Chem., 56, 2013
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