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5M2N
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Crystal Structure of Elongator subunit Elp2
Descriptor: Elongator complex protein 2
Authors:Glatt, S, Mueller, C.W.
Deposit date:2016-10-13
Release date:2016-12-28
Last modified:2017-09-06
Method:X-RAY DIFFRACTION (2.812 Å)
Cite:Architecture of the yeast Elongator complex.
EMBO Rep., 18, 2017
5M23
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Modulation of MLL1 Methyltransferase Activity
Descriptor: 4-[(~{E})-[4-[[[(2~{S})-2-[[(2~{S})-2-[[(2~{S})-2-[[(2~{S})-2-azanyl-3-oxidanyl-propanoyl]amino]propanoyl]amino]-5-carbamimidamido-pentanoyl]amino]propanoyl]amino]methyl]phenyl]diazenyl]-~{N}-[(2~{S})-3-methyl-1-oxidanylidene-butan-2-yl]benzamide, WD repeat-containing protein 5
Authors:Srinivasan, V.
Deposit date:2016-10-11
Release date:2017-06-28
Last modified:2024-01-17
Method:X-RAY DIFFRACTION (1.97 Å)
Cite:Controlled inhibition of methyltransferases using photoswitchable peptidomimetics: towards an epigenetic regulation of leukemia.
Chem Sci, 8, 2017
5M89
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Spliceosome component
Descriptor: Spliceosome WD40 Sc
Authors:Moura, T.R, Pena, V.
Deposit date:2016-10-28
Release date:2018-03-14
Last modified:2024-01-17
Method:X-RAY DIFFRACTION (1.605 Å)
Cite:Prp19/Pso4 Is an Autoinhibited Ubiquitin Ligase Activated by Stepwise Assembly of Three Splicing Factors.
Mol. Cell, 69, 2018
5MWJ
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Structure Enabled Discovery of a Stapled Peptide Inhibitor to Target the Oncogenic Transcriptional Repressor TLE1
Descriptor: DIMETHYL SULFOXIDE, Transducin-like enhancer protein 1, pepide inhibtor
Authors:McGrath, S, Tortorici, M, Vidler, L, Drouin, L, Westwood, I, Gimeson, P, Van Montfort, R, Hoelder, S.
Deposit date:2017-01-18
Release date:2017-04-05
Last modified:2024-01-17
Method:X-RAY DIFFRACTION (2.04 Å)
Cite:Structure-Enabled Discovery of a Stapled Peptide Inhibitor to Target the Oncogenic Transcriptional Repressor TLE1.
Chemistry, 23, 2017
5N4A
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Crystal structure of Chlamydomonas IFT80
Descriptor: GLYCEROL, Intraflagellar transport protein 80, OXALATE ION
Authors:Taschner, M, Mourao, A.
Deposit date:2017-02-10
Release date:2018-02-28
Last modified:2019-03-13
Method:X-RAY DIFFRACTION (1.79 Å)
Cite:Crystal structure of intraflagellar transport protein 80 reveals a homo-dimer required for ciliogenesis.
Elife, 7, 2018
5MZH
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Crystal structure of ODA16 from Chlamydomonas reinhardtii
Descriptor: Dynein assembly factor with WDR repeat domains 1, SULFATE ION
Authors:Lorentzen, E, Taschner, M, Basquin, J, Mourao, A.
Deposit date:2017-01-31
Release date:2017-03-22
Last modified:2024-01-17
Method:X-RAY DIFFRACTION (2.398 Å)
Cite:Structural basis of outer dynein arm intraflagellar transport by the transport adaptor protein ODA16 and the intraflagellar transport protein IFT46.
J. Biol. Chem., 292, 2017
5N1A
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Crystal structure of Utp4 from Chaetomium thermophilum
Descriptor: utp4
Authors:Calvino, F.R, Ahmed, Y.L, Wild, K, Sinning, I.
Deposit date:2017-02-05
Release date:2017-06-14
Last modified:2019-10-16
Method:X-RAY DIFFRACTION (2.15 Å)
Cite:Structural basis for 5'-ETS recognition by Utp4 at the early stages of ribosome biogenesis.
PLoS ONE, 12, 2017
5NAF
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Co-crystal structure of an MeCP2 peptide with TBLR1 WD40 domain
Descriptor: F-box-like/WD repeat-containing protein TBL1XR1, GLYCEROL, Methyl-CpG-binding protein 2
Authors:Kruusvee, V, Cook, A.G.
Deposit date:2017-02-27
Release date:2017-03-29
Last modified:2024-01-17
Method:X-RAY DIFFRACTION (2.493 Å)
Cite:Structure of the MeCP2-TBLR1 complex reveals a molecular basis for Rett syndrome and related disorders.
Proc. Natl. Acad. Sci. U.S.A., 114, 2017
5NNZ
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Crystal structure of human ODA16
Descriptor: Dynein assembly factor with WDR repeat domains 1
Authors:Lorentzen, E, Taschner, T, Basquin, J.
Deposit date:2017-04-10
Release date:2017-06-07
Last modified:2024-01-31
Method:X-RAY DIFFRACTION (2.651 Å)
Cite:Purification and crystal structure of human ODA16: Implications for ciliary import of outer dynein arms by the intraflagellar transport machinery.
Protein Sci., 29, 2020
5NUV
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Structure of the WD40-domain of human ATG16L1
Descriptor: (R,R)-2,3-BUTANEDIOL, Autophagy-related protein 16-1
Authors:Bajagic, M, Scrima, A.
Deposit date:2017-05-02
Release date:2017-07-19
Last modified:2024-01-17
Method:X-RAY DIFFRACTION (1.55 Å)
Cite:Structure of the WD40-domain of human ATG16L1.
Protein Sci., 26, 2017
6DY7
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WDR5 in complex with a WIN site inhibitor
Descriptor: DIMETHYL SULFOXIDE, N-[3-(2,4-dichlorophenoxy)propyl]-1H-imidazol-2-amine, SULFATE ION, ...
Authors:Phan, J, Wang, F, Fesik, S.W.
Deposit date:2018-07-01
Release date:2019-03-13
Last modified:2024-03-13
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity.
Cell Rep, 26, 2019
6E1Y
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Discovery of Potent 2-Aryl-6,7-Dihydro-5HPyrrolo[ 1,2-a]imidazoles as WDR5 WIN-site Inhibitors Using Fragment-Based Methods and Structure-Based Design
Descriptor: N-[(1S)-1-(3-chlorophenyl)ethyl]-3-{[(4,5-dihydro-1H-imidazol-2-yl)amino]methyl}benzamide, WD repeat-containing protein 5
Authors:Phan, J, Fesik, S.W.
Deposit date:2018-07-10
Release date:2019-03-13
Last modified:2023-10-11
Method:X-RAY DIFFRACTION (1.219 Å)
Cite:Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity.
Cell Rep, 26, 2019
6DYA
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WDR5 in complex with a WIN site inhibitor
Descriptor: DIMETHYL SULFOXIDE, N-[(3,5-dichlorophenyl)methyl]-3-[(1H-imidazol-1-yl)methyl]benzamide, SULFATE ION, ...
Authors:Phan, J, Wang, F, Fesik, S.W.
Deposit date:2018-07-01
Release date:2019-03-13
Last modified:2024-03-13
Method:X-RAY DIFFRACTION (2.56 Å)
Cite:Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity.
Cell Rep, 26, 2019
6E1Z
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Displacement of WDR5 from chromatin by a pharmacological WIN site inhibitor with picomolar affinity
Descriptor: 5-[(1H-imidazol-1-yl)methyl]furan-2-carboxylic acid, WD repeat-containing protein 5
Authors:Phan, J, Fesik, S.W.
Deposit date:2018-07-10
Release date:2019-03-13
Last modified:2023-10-11
Method:X-RAY DIFFRACTION (1.1 Å)
Cite:Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity.
Cell Rep, 26, 2019
6E23
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Displacement of WDR5 from chromatin by a pharmacological WIN site inhibitor with picomolar affinity
Descriptor: 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, N-[(3,4-dichlorophenyl)methyl]-3-(6-fluoro-2-methylpyridin-3-yl)-5-{[(2E)-2-imino-3-methyl-2,3-dihydro-1H-imidazol-1-yl]methyl}benzamide, WD repeat-containing protein 5
Authors:Phan, J, Fesik, S.W.
Deposit date:2018-07-10
Release date:2019-03-13
Last modified:2023-10-11
Method:X-RAY DIFFRACTION (1.66 Å)
Cite:Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity.
Cell Rep, 26, 2019
6E22
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Displacement of WDR5 from chromatin by a pharmacological WIN site inhibitor with picomolar affinity
Descriptor: 3-{[(4,5-dihydro-1H-imidazol-2-yl)amino]methyl}-N-[(3,5-dimethoxyphenyl)methyl]-4-fluorobenzamide, SULFATE ION, WD repeat-containing protein 5
Authors:Phan, J, Fesik, S.W.
Deposit date:2018-07-10
Release date:2019-03-13
Last modified:2023-10-11
Method:X-RAY DIFFRACTION (1.6 Å)
Cite:Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity.
Cell Rep, 26, 2019
6E29
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Crystal structure of Myceliophteria_thermophila Cps50 (Swd1) beta-propeller domain
Descriptor: SWD1-like protein
Authors:Joshi, M, Yang, Y, Brunzelle, J.S, Couture, J.F.
Deposit date:2018-07-10
Release date:2018-07-25
Last modified:2023-10-11
Method:X-RAY DIFFRACTION (1.818 Å)
Cite:Structure and Conformational Dynamics of a COMPASS Histone H3K4 Methyltransferase Complex.
Cell, 174, 2018
5TF2
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CRYSTAL STRUCTURE OF THE WD40 DOMAIN OF THE HUMAN PROLACTIN REGULATORY ELEMENT-BINDING PROTEIN
Descriptor: Prolactin regulatory element-binding protein, UNKNOWN ATOM OR ION
Authors:Walker, J.R, Zhang, Q, Dong, A, Wernimont, A, Li, Y, He, H, Tempel, W, Bountra, C, Edwards, A.M, Arrowsmith, C.H, Chen, Z, Tong, Y, Structural Genomics Consortium (SGC)
Deposit date:2016-09-23
Release date:2016-11-23
Last modified:2023-10-04
Method:X-RAY DIFFRACTION (2.8 Å)
Cite:CRYSTAL STRUCTURE OF THE WD40 DOMAIN OF THE HUMAN PROLACTIN REGULATORY ELEMENT-BINDING PROTEIN (CASP target)
To be published
5U8F
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Polycomb protein EED in complex with inhibitor: (3R,4S)-1-[(1S)-7-fluoro-2,3-dihydro-1H-inden-1-yl]-N,N-dimethyl-4-(1-methyl-1H-indol-3-yl)pyrrolidin-3-amine
Descriptor: (3R,4S)-1-[(1S)-7-fluoro-2,3-dihydro-1H-inden-1-yl]-N,N-dimethyl-4-(1-methyl-1H-indol-3-yl)pyrrolidin-3-amine, Polycomb protein EED
Authors:Jakob, C.G, Zhu, H.
Deposit date:2016-12-14
Release date:2017-03-15
Last modified:2023-10-04
Method:X-RAY DIFFRACTION (1.343 Å)
Cite:SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding.
Bioorg. Med. Chem. Lett., 27, 2017
5U5H
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Crystal structure of EED in complex with 6-(2-fluoro-5-methoxybenzyl)-1-isopropyl-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amine 6-(2-fluoro-5-methoxybenzyl)-1-isopropyl-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amine
Descriptor: (6S)-6-[(2-fluoro-5-methoxyphenyl)methyl]-1-(propan-2-yl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amine, GLYCEROL, Polycomb protein EED
Authors:Bussiere, D, Shu, W.
Deposit date:2016-12-06
Release date:2017-01-11
Last modified:2024-03-06
Method:X-RAY DIFFRACTION (1.8 Å)
Cite:Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase.
J. Med. Chem., 60, 2017
5U69
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Polycomb protein EED in complex with inhibitor: (3R,4S)-1-[(2-methoxyphenyl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amine
Descriptor: (3R,4S)-1-[(2-methoxyphenyl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amine, Polycomb protein EED
Authors:Jakob, C.G, Zhu, H.
Deposit date:2016-12-07
Release date:2017-03-15
Last modified:2023-10-04
Method:X-RAY DIFFRACTION (1.28 Å)
Cite:SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding.
Bioorg. Med. Chem. Lett., 27, 2017
5TTW
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Crystal Structure of EED in Complex with UNC4859
Descriptor: Polycomb protein EED, SULFATE ION, UNC4859, ...
Authors:The, J, Barnash, K.D, Brown, P.J, Edwards, A.M, Bountra, C, Frye, S.V, James, L.I, Arrowsmith, C.H.
Deposit date:2016-11-04
Release date:2017-01-11
Last modified:2023-10-04
Method:X-RAY DIFFRACTION (1.74 Å)
Cite:Discovery of Peptidomimetic Ligands of EED as Allosteric Inhibitors of PRC2.
ACS Comb Sci, 19, 2017
5U5K
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Crystal structure of EED in complex with 3-(3-methoxybenzyl)piperidine hydrochloride
Descriptor: (3R)-3-[(3-methoxyphenyl)methyl]piperidine, FORMIC ACID, Polycomb protein EED
Authors:Bussiere, D, Shu, W.
Deposit date:2016-12-06
Release date:2017-01-11
Last modified:2024-03-06
Method:X-RAY DIFFRACTION (2.33 Å)
Cite:Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase.
J. Med. Chem., 60, 2017
5U8A
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Polycomb protein EED in complex with inhibitor: (3R,4S)-1-[(2-bromo-6-fluorophenyl)methyl]-N,N-dimethyl-4-(1-methyl-1H-indol-3-yl)pyrrolidin-3-amine
Descriptor: (3R,4S)-1-[(2-bromo-6-fluorophenyl)methyl]-N,N-dimethyl-4-(1-methyl-1H-indol-3-yl)pyrrolidin-3-amine, Polycomb protein EED
Authors:Jakob, C.G, Zhu, H.
Deposit date:2016-12-14
Release date:2017-03-15
Last modified:2023-10-04
Method:X-RAY DIFFRACTION (1.45 Å)
Cite:SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding.
Bioorg. Med. Chem. Lett., 27, 2017
5U6D
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Polycomb protein EED in complex with inhibitor: 2-[4-(4-{(3S,4R)-4-(dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl}phenyl)-1H-pyrazol-1-yl]acetamide
Descriptor: 2-[4-(4-{(3S,4R)-4-(dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl}phenyl)-1H-pyrazol-1-yl]acetamide, Polycomb protein EED
Authors:Jakob, C.G, Zhu, H.
Deposit date:2016-12-07
Release date:2017-03-15
Last modified:2023-10-04
Method:X-RAY DIFFRACTION (1.64 Å)
Cite:SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding.
Bioorg. Med. Chem. Lett., 27, 2017

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