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4WT2
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CO-CRYSTAL STRUCTURE OF MDM2 IN COMPLEX WITH AM-7209
Descriptor:E3 ubiquitin-protein ligase Mdm2, 4-({[(3R,5R,6S)-1-[(1S)-2-(tert-butylsulfonyl)-1-cyclopropylethyl]-6-(4-chloro-3-fluorophenyl)-5-(3-chlorophenyl)-3-methyl-2-oxopiperidin-3-yl]acetyl}amino)-2-methoxybenzoic acid, SULFATE ION
Authors:Shaffer, P.L., Huang, X., Yakowec, P., Long, A.M.
Deposit date:2014-10-30
Release date:2014-12-03
Last modified:2017-11-22
Method:X-RAY DIFFRACTION (1.42 Å)
Cite:Discovery of AM-7209, a Potent and Selective 4-Amidobenzoic Acid Inhibitor of the MDM2-p53 Interaction.
J.Med.Chem., 57, 2014
4ZFI
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STRUCTURE OF MDM2 WITH LOW MOLECULAR WEIGHT INHIBITOR
Descriptor:E3 ubiquitin-protein ligase Mdm2, (5S)-3,5-bis(4-chlorobenzyl)-4-(6-chloro-1H-indol-3-yl)-5-hydroxy-1-methyl-1,5-dihydro-2H-pyrrol-2-one
Authors:Zak, K.M., Twarda-Clapa, A., Wrona, E.M., Grudnik, P., Dubin, G., Holak, T.A.
Deposit date:2015-04-21
Release date:2016-10-19
Last modified:2016-12-28
Method:X-RAY DIFFRACTION (2 Å)
Cite: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
5HMI
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HDM2 IN COMPLEX WITH A 3,3-DISUBSTITUTED PIPERIDINE
Descriptor:E3 ubiquitin-protein ligase Mdm2, {4-[2-(2-hydroxyethoxy)phenyl]piperazin-1-yl}[(2R,3S)-2-propyl-1-{[4-(trifluoromethyl)pyridin-3-yl]carbonyl}-3-{[5-(trifluoromethyl)thiophen-3-yl]oxy}piperidin-3-yl]methanone, SULFATE ION
Authors:Scapin, G.
Deposit date:2016-01-16
Release date:2016-04-06
Last modified:2017-11-22
Method:X-RAY DIFFRACTION (1.74 Å)
Cite:Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.
Acs Med.Chem.Lett., 7, 2016
5HMK
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HDM2 IN COMPLEX WITH A 3,3-DISUBSTITUTED PIPERIDINE
Descriptor:E3 ubiquitin-protein ligase Mdm2, {4-[2-(2-hydroxyethoxy)phenyl]piperazin-1-yl}[(2R,3S)-2-propyl-3-[4-(trifluoromethyl)phenoxy]-1-{[4-(trifluoromethyl)pyridin-3-yl]carbonyl}piperidin-3-yl]methanone
Authors:Scapin, G.
Deposit date:2016-01-16
Release date:2016-04-06
Method:X-RAY DIFFRACTION (2.17 Å)
Cite:Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.
Acs Med.Chem.Lett., 7, 2016
5LAW
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NOVEL SPIRO[3H-INDOLE-3,2 -PYRROLIDIN]-2(1H)-ONE INHIBITORS OF THE MDM2-P53 INTERACTION: HDM2 (MDM2) IN COMPLEX WITH COMPOUND 14
Descriptor:E3 ubiquitin-protein ligase Mdm2, 2-[(3~{S},3'~{a}~{S},6'~{S},6'~{a}~{S})-6-chloranyl-6'-(3-chlorophenyl)-4'-(cyclopropylmethyl)-2-oxidanylidene-spiro[1~{H}-indole-3,5'-3,3~{a},6,6~{a}-tetrahydro-2~{H}-pyrrolo[3,2-b]pyrrole]-1'-yl]ethanoic acid, SULFATE ION
Authors:KESSLER, D., GOLLNER, A.
Deposit date:2016-06-15
Release date:2016-11-02
Last modified:2016-12-21
Method:X-RAY DIFFRACTION (1.64 Å)
Cite:Discovery of Novel Spiro[3H-indole-3,2'-pyrrolidin]-2(1H)-one Compounds as Chemically Stable and Orally Active Inhibitors of the MDM2-p53 Interaction.
J. Med. Chem., 59, 2016
5LN2
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DISCOVERY OF A NOVEL CLASS OF HIGHLY POTENT INHIBITORS OF THE P53-MDM2 INTERACTION BY STRUCTURE-BASED DESIGN STARTING FROM A CONFORMATIONAL ARGUMENT
Descriptor:E3 ubiquitin-protein ligase Mdm2, (4~{S})-5-[5-chloranyl-2-[2-(dimethylamino)ethoxy]phenyl]-4-(4-chloranyl-2-methyl-phenyl)-2-(2-methoxyphenyl)-3-propan-2-yl-4~{H}-pyrrolo[3,4-c]pyrazol-6-one, SULFATE ION, ...
Authors:Kallen, J.
Deposit date:2016-08-02
Release date:2016-09-07
Last modified:2016-09-21
Method:X-RAY DIFFRACTION (1.58 Å)
Cite:Discovery of a novel class of highly potent inhibitors of the p53-MDM2 interaction by structure-based design starting from a conformational argument.
Bioorg.Med.Chem.Lett., 26, 2016
5OC8
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HDM2 (17-111, WILD TYPE) COMPLEXED WITH NVP-HDM201 AT 1.56A
Descriptor:E3 ubiquitin-protein ligase Mdm2, (4~{S})-5-(5-chloranyl-1-methyl-2-oxidanylidene-pyridin-3-yl)-4-(4-chlorophenyl)-2-(2,4-dimethoxypyrimidin-5-yl)-3-propan-2-yl-4~{H}-pyrrolo[3,4-d]imidazol-6-one, CHLORIDE ION
Authors:Kallen, J.
Deposit date:2017-06-29
Release date:2018-08-22
Last modified:2018-11-14
Method:X-RAY DIFFRACTION (1.56 Å)
Cite:Dose and Schedule Determine Distinct Molecular Mechanisms Underlying the Efficacy of the p53-MDM2 Inhibitor HDM201.
Cancer Res., 78, 2018
1RV1
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CRYSTAL STRUCTURE OF HUMAN MDM2 WITH AN IMIDAZOLINE INHIBITOR
Descriptor:Ubiquitin-protein ligase E3 Mdm2, CIS-[4,5-BIS-(4-BROMOPHENYL)-2-(2-ETHOXY-4-METHOXYPHENYL)-4,5-DIHYDROIMIDAZOL-1-YL]-[4-(2-HYDROXYETHYL)PIPERAZIN-1-YL]METHANONE
Authors:Lukacs, C., Kammlott, U., Graves, B.
Deposit date:2003-12-12
Release date:2004-01-20
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.3 Å)
Cite:In vivo activation of the p53 pathway by small-molecule antagonists of MDM2.
Science, 303, 2004
1T4E
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STRUCTURE OF HUMAN MDM2 IN COMPLEX WITH A BENZODIAZEPINE INHIBITOR
Descriptor:Ubiquitin-protein ligase E3 Mdm2, (4-CHLOROPHENYL)[3-(4-CHLOROPHENYL)-7-IODO-2,5-DIOXO-1,2,3,5-TETRAHYDRO-4H-1,4-BENZODIAZEPIN-4-YL]ACETIC ACID
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:2018-01-31
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells
J.Med.Chem., 48, 2005
1T4F
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STRUCTURE OF HUMAN MDM2 IN COMPLEX WITH AN OPTIMIZED P53 PEPTIDE
Descriptor:Ubiquitin-protein ligase E3 Mdm2, optimized p53 peptide, SULFATE ION
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:2011-07-13
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
1YCR
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MDM2 BOUND TO THE TRANSACTIVATION DOMAIN OF P53
Descriptor:MDM2, P53
Authors:Kussie, P.H., Pavletich, N.P.
Deposit date:1996-09-30
Release date:1997-11-19
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:Structure of the MDM2 oncoprotein bound to the p53 tumor suppressor transactivation domain.
Science, 274, 1996
1Z1M
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NMR STRUCTURE OF UNLIGANDED MDM2
Descriptor:Ubiquitin-protein ligase E3 Mdm2
Authors:Uhrinova, S., Uhrin, D., Powers, H., Watt, K., Zheleva, D., Fischer, P., McInnes, C., Barlow, P.N.
Deposit date:2005-03-04
Release date:2005-06-28
Last modified:2011-07-13
Method:SOLUTION NMR
Cite:Structure of Free MDM2 N-terminal Domain Reveals Conformational Adjustments that Accompany p53-binding
J.Mol.Biol., 350, 2005
2C6A
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SOLUTION STRUCTURE OF THE C4 ZINC-FINGER DOMAIN OF HDM2
Descriptor:UBIQUITIN-PROTEIN LIGASE E3 MDM2, ZINC ION
Authors:Yu, G.W., Allen, M.D., Andreeva, A., Fersht, A.R., Bycroft, M.
Deposit date:2005-11-08
Release date:2006-01-04
Last modified:2018-01-24
Method:SOLUTION NMR
Cite:Solution Structure of the C4 Zinc Finger Domain of Hdm2.
Protein Sci., 15, 2006
2C6B
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SOLUTION STRUCTURE OF THE C4 ZINC-FINGER DOMAIN OF HDM2
Descriptor:UBIQUITIN-PROTEIN LIGASE E3 MDM2, ZINC ION
Authors:Yu, G.W., Allen, M.D., Andreeva, A., Fersht, A.R., Bycroft, M.
Deposit date:2005-11-08
Release date:2006-01-04
Last modified:2018-01-24
Method:SOLUTION NMR
Cite:Solution Structure of the C4 Zinc Finger Domain of Hdm2.
Protein Sci., 15, 2006
2HDP
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SOLUTION STRUCTURE OF HDM2 RING FINGER DOMAIN
Descriptor:Ubiquitin-protein ligase E3 Mdm2, ZINC ION
Authors:Kostic, M., Matt, T., Yamout-Martinez, M., Dyson, H.J., Wright, P.E.
Deposit date:2006-06-20
Release date:2006-11-21
Last modified:2011-07-13
Method:SOLUTION NMR
Cite:Solution structure of the Hdm2 C2H2C4 RING, a domain critical for ubiquitination of p53.
J.Mol.Biol., 363, 2006
2LZG
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NMR STRUCTURE OF MDM2 (6-125) WITH PIP-1
Descriptor:E3 ubiquitin-protein ligase Mdm2, [(3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-(cyclopropylmethyl)-2-oxopiperidin-3-yl]acetic acid
Authors:Michelsen, K.B., Jordan, J.B., Lewis, J., Long, A.M., Yang, E., Rew, Y., Zhou, J., Yakowec, P., Schnier, P.D., Huang, X., Poppe, L.
Deposit date:2012-10-02
Release date:2012-11-07
Method:SOLUTION NMR
Cite:Ordering of the N-Terminus of Human MDM2 by Small Molecule Inhibitors.
J.Am.Chem.Soc., 134, 2012
2M86
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SOLUTION STRUCTURE OF HDM2 WITH ENGINEERED CYCLOTIDE
Descriptor:MCo-PMI, E3 ubiquitin-protein ligase Mdm2
Authors:Majumder, S., Ji, Y., Millard, M., Borra, R., Bi, T., Elnagar, A.Y., Neamati, N., Camarero, J.A.
Deposit date:2013-05-07
Release date:2013-07-31
Last modified:2013-08-21
Method:SOLUTION NMR
Cite:In Vivo Activation of the p53 Tumor Suppressor Pathway by an Engineered Cyclotide.
J.Am.Chem.Soc., 135, 2013
2MPS
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STRUCTURE OF COMPLEX OF MDM2(3-109) AND P73 TAD(10-25)
Descriptor:E3 ubiquitin-protein ligase Mdm2, Tumor protein p73
Authors:Shin, J.S., Ha, J.H., Chi, S.W.
Deposit date:2014-06-02
Release date:2015-06-03
Method:SOLUTION NMR
Cite:Structural convergence of unstructured p53 family transactivation domains in MDM2 recognition
Cell Cycle, 14, 2015
2RUH
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CHEMICAL SHIFT ASSIGNMENTS FOR MIP AND MDM2 IN BOUND STATE
Descriptor:E3 ubiquitin-protein ligase Mdm2
Authors:Nagata, T., Shirakawa, K., Kobayashi, N., Shiheido, H., Horisawa, K., Katahira, M., Doi, N., Yanagawa, H.
Deposit date:2014-06-03
Release date:2014-10-15
Method:SOLUTION NMR
Cite:Structural Basis for Inhibition of the MDM2:p53 Interaction by an Optimized MDM2-Binding Peptide Selected with mRNA Display
Plos One, 9, 2014
2VJE
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CRYSTAL STRUCTURE OF THE MDM2-MDMX RING DOMAIN HETERODIMER
Descriptor:E3 UBIQUITIN-PROTEIN LIGASE MDM2, MDM4 PROTEIN, ZINC ION, ...
Authors:Mace, P.D., Linke, K., Smith, C.A., Day, C.L.
Deposit date:2007-12-10
Release date:2008-05-13
Last modified:2018-06-06
Method:X-RAY DIFFRACTION (2.2 Å)
Cite:Structure of the MDM2/MDMX RING domain heterodimer reveals dimerization is required for their ubiquitylation in trans.
Cell Death Differ., 15, 2008
2VJF
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CRYSTAL STRUCTURE OF THE MDM2-MDMX RING DOMAIN HETERODIMER
Descriptor:E3 UBIQUITIN-PROTEIN LIGASE MDM2, MDM4 PROTEIN, ZINC ION, ...
Authors:Mace, P.D., Linke, K., Smith, C.A., Day, C.L.
Deposit date:2007-12-10
Release date:2008-05-13
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.3 Å)
Cite:Structure of the Mdm2/Mdmx Ring Domain Heterodimer Reveals Dimerization is Required for Their Ubiquitylation in Trans.
Cell Death Differ., 15, 2008
3EQS
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CRYSTAL STRUCTURE OF HUMAN MDM2 IN COMPLEX WITH A 12-MER PEPTIDE INHIBITOR
Descriptor:E3 ubiquitin-protein ligase Mdm2, 12-mer peptide inhibitor, GUANIDINE
Authors:Pazgier, M., Lu, W.
Deposit date:2008-10-01
Release date:2009-03-17
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (1.65 Å)
Cite:Structural basis for high-affinity peptide inhibition of p53 interactions with MDM2 and MDMX.
Proc.Natl.Acad.Sci.USA, 106, 2009
3G03
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STRUCTURE OF HUMAN MDM2 IN COMPLEX WITH HIGH AFFINITY PEPTIDE
Descriptor:E3 ubiquitin-protein ligase Mdm2, High affinity synthetic peptide
Authors:Czarna, A.L., Popowicz, G.M., Holak, T.A.
Deposit date:2009-01-27
Release date:2009-04-14
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (1.8 Å)
Cite:High affinity interaction of the p53 peptide-analogue with human Mdm2 and Mdmx
Cell Cycle, 8, 2009
3IUX
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CRYSTAL STRUCTURE OF HUMAN MDM2 IN COMPLEX WITH A POTENT MINIATURE PROTEIN INHIBITOR (18-RESIDUES)
Descriptor:E3 ubiquitin-protein ligase Mdm2, miniature protein inhibitor, ACETATE ION, ...
Authors:Pazgier, M., Lu, W.
Deposit date:2009-08-31
Release date:2009-10-27
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (1.65 Å)
Cite:Apamin as a template for structure-based rational design of potent peptide activators of p53.
Angew.Chem.Int.Ed.Engl., 48, 2009
3IWY
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CRYSTAL STRUCTURE OF HUMAN MDM2 COMPLEXED WITH D-PEPTIDE (12 RESIDUES)
Descriptor:D-peptide inhibitor, E3 ubiquitin-protein ligase Mdm2
Authors:Pazgier, M., Lu, W.
Deposit date:2009-09-03
Release date:2010-04-21
Last modified:2012-12-12
Method:X-RAY DIFFRACTION (1.93 Å)
Cite:D-peptide inhibitors of the p53-MDM2 interaction for targeted molecular therapy of malignant neoplasms.
Proc.Natl.Acad.Sci.USA, 398, 2010
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