8PWC
| Crystal structure of MDM2 with Brigimadlin | Descriptor: | Brigimadlin, E3 ubiquitin-protein ligase Mdm2 | Authors: | Bader, G, Wolkerstorfer, B. | Deposit date: | 2023-07-20 | Release date: | 2024-10-02 | Method: | X-RAY DIFFRACTION (1.461 Å) | Cite: | Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2-p53 Antagonist Suitable for Intermittent Dose Schedules. Mol.Cancer Ther., 2024
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8J81
| MDM2 bound with a peptoid | Descriptor: | (2S)-2-[[(2S)-2-[(6-chloranyl-1H-indol-3-yl)methyl-[(2S)-2-[[(2S)-2-[ethanoyl-(phenylmethyl)amino]propanoyl]-methyl-amino]propanoyl]amino]propanoyl]-methyl-amino]-N-(3,3-dimethylbutyl)-N-[(2S)-1-oxidanylidene-1-piperazin-1-yl-propan-2-yl]propanamide, CHLORIDE ION, E3 ubiquitin-protein ligase Mdm2 | Authors: | Yokomine, M, Fukuda, Y, Ago, H, Matsuura, H, Ueno, G, Nagatoishi, S, Yamamoto, M, Tsumoto, K, Jumpei, M, Sando, S. | Deposit date: | 2023-04-28 | Release date: | 2024-05-01 | Method: | X-RAY DIFFRACTION (1.35 Å) | Cite: | A structural and physicochemical study of how a peptoid binds to a protein To Be Published
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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: | 2024-10-09 | 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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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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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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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: | 2024-10-16 | 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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8BGU
| human MDM2-5S RNP | Descriptor: | 5S rRNA, 60S ribosomal protein L11, 60S ribosomal protein L5, ... | Authors: | Castillo, N, Thoms, M, Flemming, D, Hammaren, H.M, Buschauer, R, Ameismeier, M, Bassler, J, Beck, M, Beckmann, R, Hurt, E. | Deposit date: | 2022-10-28 | Release date: | 2023-06-14 | Last modified: | 2023-08-30 | Method: | ELECTRON MICROSCOPY (4.1 Å) | Cite: | Structure of nascent 5S RNPs at the crossroad between ribosome assembly and MDM2-p53 pathways. Nat.Struct.Mol.Biol., 30, 2023
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8EIC
| Crystal structure of beta-catenin and the MDM2 p53-binding domain in complex with H330, a Helicon Polypeptide | Descriptor: | Catenin beta-1, E3 ubiquitin-protein ligase Mdm2, H330, ... | Authors: | Li, K, Travaline, T.L, Swiecicki, J.-M, Tokareva, O.S, Thomson, T.M, Verdine, G.L, McGee, J.H. | Deposit date: | 2022-09-14 | Release date: | 2023-10-25 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.62 Å) | Cite: | Recognition and reprogramming of E3 ubiquitin ligase surfaces by alpha-helical peptides. Nat Commun, 14, 2023
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8EIB
| Crystal structure of beta-catenin and the MDM2 p53-binding domain in complex with H329, a Helicon Polypeptide | Descriptor: | Catenin beta-1, E3 ubiquitin-protein ligase Mdm2, H329, ... | Authors: | Li, K, Travaline, T.L, Swiecicki, J.-M, Tokareva, O.S, Thomson, T.M, Verdine, G.L, McGee, J.H. | Deposit date: | 2022-09-14 | Release date: | 2023-10-25 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (3.76 Å) | Cite: | Recognition and reprogramming of E3 ubiquitin ligase surfaces by alpha-helical peptides. Nat Commun, 14, 2023
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8EI9
| Crystal structure of beta-catenin and the MDM2 p53-binding domain in complex with H332, a Helicon Polypeptide | Descriptor: | Catenin beta-1, E3 ubiquitin-protein ligase Mdm2, H332, ... | Authors: | Li, K, Travaline, T.L, Swiecicki, J.-M, Tokareva, O.S, Thomson, T.M, Verdine, G.L, McGee, J.H. | Deposit date: | 2022-09-14 | Release date: | 2023-10-25 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (3.9 Å) | Cite: | Recognition and reprogramming of E3 ubiquitin ligase surfaces by alpha-helical peptides. Nat Commun, 14, 2023
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8EIA
| Crystal structure of beta-catenin and the MDM2 p53-binding domain in complex with H333, a Helicon Polypeptide | Descriptor: | Catenin beta-1, E3 ubiquitin-protein ligase Mdm2, H333, ... | Authors: | Li, K, Travaline, T.L, Swiecicki, J.-M, Tokareva, O.S, Thomson, T.M, Verdine, G.L, McGee, J.H. | Deposit date: | 2022-09-14 | Release date: | 2023-10-25 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (3.6 Å) | Cite: | Recognition and reprogramming of E3 ubiquitin ligase surfaces by alpha-helical peptides. Nat Commun, 14, 2023
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8EBK
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8AEU
| Structure of hMDM2 in complex with Nutlin-3a-aa | Descriptor: | 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 | Authors: | Labuzek, B, Golik, P, Magiera-Mularz, K, Berg, T. | Deposit date: | 2022-07-13 | Release date: | 2023-01-18 | Last modified: | 2024-02-07 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Nutlin-3a-aa: Improving the Bioactivity of a p53/MDM2 Interaction Inhibitor by Introducing a Solvent-Exposed Methylene Group. Chembiochem, 24, 2023
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7Y8R
| The nucleosome-bound human PBAF complex | Descriptor: | ACTB protein (Fragment), ADENOSINE-5'-DIPHOSPHATE, AT-rich interactive domain-containing protein 2, ... | Authors: | Wang, L, Yu, J, Yu, Z, Wang, Q, He, S, Xu, Y. | Deposit date: | 2022-06-24 | Release date: | 2022-12-07 | Last modified: | 2024-07-03 | Method: | ELECTRON MICROSCOPY (4.4 Å) | Cite: | Structure of nucleosome-bound human PBAF complex. Nat Commun, 13, 2022
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7Z0O
| Structure of transcription factor UAF in complex with TBP and 35S rRNA promoter DNA | Descriptor: | Histone H3, Histone H4, Non-template DNA, ... | Authors: | Baudin, F, Murciano, B, Fung, H.K.H, Fromm, S.A, Mueller, C.W. | Deposit date: | 2022-02-23 | Release date: | 2022-04-27 | Last modified: | 2024-07-17 | Method: | ELECTRON MICROSCOPY (2.8 Å) | Cite: | Mechanism of RNA polymerase I selection by transcription factor UAF. Sci Adv, 8, 2022
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7QDQ
| Crystal Structure of HDM2 in complex with Caylin-1 | Descriptor: | CHLORIDE ION, Caylin-1, DIMETHYL SULFOXIDE, ... | Authors: | Finke, A.D, Walti, M.A, Marsh, M.E, Orts, J. | Deposit date: | 2021-11-29 | Release date: | 2022-10-05 | Last modified: | 2024-02-07 | Method: | X-RAY DIFFRACTION (1.26 Å) | Cite: | Elucidation of a nutlin-derivative-HDM2 complex structure at the interaction site by NMR molecular replacement: A straightforward derivation J Magn Reson Open, 10-11, 2022
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7VDV
| The overall structure of human chromatin remodeling PBAF-nucleosome complex | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, AT-rich interactive domain-containing protein 2,AT-rich interactive domain-containing protein 2, Actin, ... | Authors: | Chen, Z.C, Chen, K.J, Yuan, J.J. | Deposit date: | 2021-09-07 | Release date: | 2022-05-18 | Method: | ELECTRON MICROSCOPY (3.4 Å) | Cite: | Structure of human chromatin-remodelling PBAF complex bound to a nucleosome. Nature, 605, 2022
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7NA3
| HDM2 in complex with compound 62 | Descriptor: | 3-[4-(5-chloropyridin-3-yl)-2-[(2S)-1-methoxypropan-2-yl]-3-{(1R)-1-[(1r,4R)-4-methylcyclohexyl]ethyl}-3H-imidazo[4,5-c]pyridin-6-yl]-1,2,4-oxadiazol-5(4H)-one, Isoform 11 of E3 ubiquitin-protein ligase Mdm2, SULFATE ION | Authors: | Scapin, G. | Deposit date: | 2021-06-19 | Release date: | 2021-11-10 | Last modified: | 2024-05-22 | Method: | X-RAY DIFFRACTION (2.21 Å) | Cite: | Discovery of MK-4688 : an Efficient Inhibitor of the HDM2-p53 Protein-Protein Interaction. J.Med.Chem., 64, 2021
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7NA4
| HDM2 in complex with compound 63 | Descriptor: | 3-[4-(5-chloropyridin-3-yl)-2-[(R)-cyclopropyl(ethoxy)methyl]-3-{(1R)-1-[(1r,4R)-4-methylcyclohexyl]ethyl}-3H-imidazo[4,5-c]pyridin-6-yl]-1,2,4-oxadiazol-5(4H)-one, CHLORIDE ION, GLYCEROL, ... | Authors: | Scapin, G. | Deposit date: | 2021-06-19 | Release date: | 2021-11-10 | Last modified: | 2024-05-22 | Method: | X-RAY DIFFRACTION (1.84 Å) | Cite: | Discovery of MK-4688 : an Efficient Inhibitor of the HDM2-p53 Protein-Protein Interaction. J.Med.Chem., 64, 2021
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7NA2
| HDM2 in complex with compound 56 | Descriptor: | 3-[4-(5-chloropyridin-3-yl)-2-[(4aR,7aR)-hexahydrocyclopenta[b][1,4]oxazin-4(4aH)-yl]-3-{[(1r,4R)-4-methylcyclohexyl]methyl}-3H-imidazo[4,5-c]pyridin-6-yl]-1,2,4-oxadiazol-5(4H)-one, Isoform 11 of E3 ubiquitin-protein ligase Mdm2 | Authors: | Scapin, G. | Deposit date: | 2021-06-19 | Release date: | 2021-11-10 | Last modified: | 2024-05-22 | Method: | X-RAY DIFFRACTION (1.86 Å) | Cite: | Discovery of MK-4688 : an Efficient Inhibitor of the HDM2-p53 Protein-Protein Interaction. J.Med.Chem., 64, 2021
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7NA1
| HDM2 in complex with compound 2 | Descriptor: | 8-(1-benzothiophen-5-yl)-7-[(4-chlorophenyl)methyl]-6-{[(1R)-1-cyclopropylethyl]amino}-7H-purine-2-carboxylic acid, CITRIC ACID, E3 ubiquitin-protein ligase Mdm2, ... | Authors: | Scapin, G. | Deposit date: | 2021-06-19 | Release date: | 2021-11-10 | Last modified: | 2024-05-22 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Discovery of MK-4688 : an Efficient Inhibitor of the HDM2-p53 Protein-Protein Interaction. J.Med.Chem., 64, 2021
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7NUS
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7BMG
| Inhibitor of MDM2-p53 Interaction | Descriptor: | (3~{R})-3-(4-chlorophenyl)-2-[(4-ethynylphenyl)methyl]-3-[[1-(hydroxymethyl)cyclopropyl]methoxy]-6-(2-oxidanylpropan-2-yl)isoindol-1-one, 1,2-ETHANEDIOL, E3 ubiquitin-protein ligase Mdm2 | Authors: | Williams, P.A. | Deposit date: | 2021-01-20 | Release date: | 2021-04-07 | Last modified: | 2024-05-15 | Method: | X-RAY DIFFRACTION (1.83 Å) | Cite: | Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein-Protein Interaction. J.Med.Chem., 64, 2021
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7BJ6
| Inhibitor of MDM2-p53 Interaction | Descriptor: | (3~{R})-2-[(5-chloranylpyridin-2-yl)methyl]-3-(4-chlorophenyl)-4-fluoranyl-3-[[1-(hydroxymethyl)cyclopropyl]methoxy]-6-(2-oxidanylpropan-2-yl)isoindol-1-one, 1,2-ETHANEDIOL, DIMETHYL SULFOXIDE, ... | Authors: | Williams, P.A. | Deposit date: | 2021-01-14 | Release date: | 2021-04-07 | Last modified: | 2024-05-15 | Method: | X-RAY DIFFRACTION (1.59 Å) | Cite: | Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein-Protein Interaction. J.Med.Chem., 64, 2021
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