6TAC
 
 | | Human NAMPT deletion mutant in complex with nicotinamide mononucleotide, pyrophosphate, and Mg2+ | | 分子名称: | BETA-NICOTINAMIDE RIBOSE MONOPHOSPHATE, GLYCEROL, MAGNESIUM ION, ... | | 著者 | Houry, D, Raasakka, A, Kursula, P, Ziegler, M. | | 登録日 | 2019-10-29 | | 公開日 | 2020-11-18 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | | 主引用文献 | Identification of structural determinants of NAMPT activity and substrate selectivity
To Be Published
|
|
9BOL
 | | Crystal structure of the complex between VHL, ElonginB, ElonginC, and compound 5 | | 分子名称: | (4R)-1-[(2S)-2-(4-cyclopropyl-1H-1,2,3-triazol-1-yl)-3,3-dimethylbutanoyl]-4-hydroxy-N-{[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}-L-prolinamide, 1,2-ETHANEDIOL, CHLORIDE ION, ... | | 著者 | Murray, J.M, Wu, H, Fuhrmann, J, Fairbrother, W.J, DiPasquale, A. | | 登録日 | 2024-05-03 | | 公開日 | 2024-05-29 | | 実験手法 | X-RAY DIFFRACTION (1.99 Å) | | 主引用文献 | Potency-enhanced peptidomimetic VHL ligands with improved oral bioavailability
To Be Published
|
|
9BJU
 | | Crystal structure of the complex between VHL, ElonginB, ElonginC, and compound 5 | | 分子名称: | 1,2-ETHANEDIOL, 3-PYRIDIN-4-YL-2,4-DIHYDRO-INDENO[1,2-.C.]PYRAZOLE, ACETATE ION, ... | | 著者 | Murray, J.M, Wu, H, Fuhrmann, J, Fairbrother, W.J, DiPasquale, A. | | 登録日 | 2024-04-25 | | 公開日 | 2024-05-29 | | 実験手法 | X-RAY DIFFRACTION (2.47 Å) | | 主引用文献 | Potency-enhanced peptidomimetic VHL ligands with improved oral bioavailability
To Be Published
|
|
4W9I
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-((2S,4R)-1-acetyl-4-hydroxypyrrolidine-2-carbonyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 10) | | 分子名称: | (4R)-1-acetyl-4-hydroxy-L-prolyl-(4R)-4-hydroxy-N-[4-(4-methyl-1,3-thiazol-5-yl)benzyl]-L-prolinamide, Transcription elongation factor B polypeptide 1, Transcription elongation factor B polypeptide 2, ... | | 著者 | Gadd, M.S, Soares, P, Galdeano, C, van Molle, I, Ciulli, A. | | 登録日 | 2014-08-27 | | 公開日 | 2014-09-10 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Structure-Guided Design and Optimization of Small Molecules Targeting the Protein-Protein Interaction between the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities.
J.Med.Chem., 57, 2014
|
|
4W9C
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(oxazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 2) | | 分子名称: | (4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-[4-(1,3-oxazol-5-yl)benzyl]-L-prolinamide, Transcription elongation factor B polypeptide 1, Transcription elongation factor B polypeptide 2, ... | | 著者 | Gadd, M.S, Hewitt, S, Galdeano, C, van Molle, I, Ciulli, A. | | 登録日 | 2014-08-27 | | 公開日 | 2014-09-10 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Structure-Guided Design and Optimization of Small Molecules Targeting the Protein-Protein Interaction between the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities.
J.Med.Chem., 57, 2014
|
|
4W9D
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methyloxazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 3) | | 分子名称: | (4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-[4-(4-methyl-1,3-oxazol-5-yl)benzyl]-L-prolinamide, Transcription elongation factor B polypeptide 1, Transcription elongation factor B polypeptide 2, ... | | 著者 | Gadd, M.S, Hewitt, S, Galdeano, C, van Molle, I, Ciulli, A. | | 登録日 | 2014-08-27 | | 公開日 | 2014-09-10 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Structure-Guided Design and Optimization of Small Molecules Targeting the Protein-Protein Interaction between the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities.
J.Med.Chem., 57, 2014
|
|
4W9G
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-(3-methyl-4-(thiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 6) | | 分子名称: | (4R)-1-(3,3-dimethylbutanoyl)-4-hydroxy-N-[3-methyl-4-(1,3-thiazol-5-yl)benzyl]-L-prolinamide, Transcription elongation factor B polypeptide 1, Transcription elongation factor B polypeptide 2, ... | | 著者 | Gadd, M.S, Soares, P, Galdeano, C, van Molle, I, Ciulli, A. | | 登録日 | 2014-08-27 | | 公開日 | 2014-09-10 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Structure-Guided Design and Optimization of Small Molecules Targeting the Protein-Protein Interaction between the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities.
J.Med.Chem., 57, 2014
|
|
5N7D
 | | MAGI-1 complexed with a RSK1 peptide | | 分子名称: | CALCIUM ION, GLYCEROL, Membrane-associated guanylate kinase, ... | | 著者 | Gogl, G, Nyitray, L. | | 登録日 | 2017-02-20 | | 公開日 | 2017-11-08 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Dynamic control of RSK complexes by phosphoswitch-based regulation.
FEBS J., 285, 2018
|
|
5W3G
 | |
7T1Z
 | | Structure of the Fbw7-Skp1-MycNdegron complex | | 分子名称: | F-box/WD repeat-containing protein 7, Myc proto-oncogene N terminal degron, S-phase kinase-associated protein 1, ... | | 著者 | Wang, B, Rusnac, D.V, Clurman, B.E, Zheng, N. | | 登録日 | 2021-12-02 | | 公開日 | 2022-02-16 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.77 Å) | | 主引用文献 | Two diphosphorylated degrons control c-Myc degradation by the Fbw7 tumor suppressor.
Sci Adv, 8, 2022
|
|
4WQO
 | | Structure of VHL-EloB-EloC-Cul2 | | 分子名称: | Cullin-2, Transcription elongation factor B polypeptide 1, Transcription elongation factor B polypeptide 2, ... | | 著者 | Nguyen, H.C, Xiong, Y. | | 登録日 | 2014-10-22 | | 公開日 | 2015-03-04 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Insights into Cullin-RING E3 Ubiquitin Ligase Recruitment: Structure of the VHL-EloBC-Cul2 Complex.
Structure, 23, 2015
|
|
8CQE
 | | pVHL:EloB:EloC in complex with (2S,4R)-1-((S)-2-(1-Fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(2-methyl-4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide (Compound 37) | | 分子名称: | (2~{S},4~{R})-1-[(2~{S})-2-[(1-fluoranylcyclopropyl)carbonylamino]-3,3-dimethyl-butanoyl]-~{N}-[(1~{S})-7-fluoranyl-6-(4-methyl-1,3-thiazol-5-yl)-1,2,3,4-tetrahydronaphthalen-1-yl]-4-oxidanyl-pyrrolidine-2-carboxamide, Elongin-B, Elongin-C, ... | | 著者 | Casement, R, Phuong Vu, L, Ciulli, A, Gutschow, M. | | 登録日 | 2023-03-06 | | 公開日 | 2023-09-27 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.85 Å) | | 主引用文献 | Expanding the Structural Diversity at the Phenylene Core of Ligands for the von Hippel-Lindau E3 Ubiquitin Ligase: Development of Highly Potent Hypoxia-Inducible Factor-1 alpha Stabilizers.
J.Med.Chem., 66, 2023
|
|
7P15
 | |
7OZW
 | |
6P59
 | | Crystal structure of SIVrcm Vif-CBFbeta-ELOB-ELOC complex | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, Core-binding factor subunit beta, Elongin-B, ... | | 著者 | Binning, J.M, Chesarino, N.M, Emerman, M, Gross, J.D. | | 登録日 | 2019-05-29 | | 公開日 | 2019-12-25 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.942214 Å) | | 主引用文献 | Structural Basis for a Species-Specific Determinant of an SIV Vif Protein toward Hominid APOBEC3G Antagonism.
Cell Host Microbe, 26, 2019
|
|
6O22
 | | Structure of Asf1-H3:H4-Rtt109-Vps75 histone chaperone-lysine acetyltransferase complex with the histone substrate. | | 分子名称: | Histone H3.2, Histone H4, Histone acetyltransferase RTT109, ... | | 著者 | Danilenko, N, Carlomagno, T, Kirkpatrick, J.P. | | 登録日 | 2019-02-22 | | 公開日 | 2019-07-31 | | 最終更新日 | 2024-05-01 | | 実験手法 | SOLUTION NMR, SOLUTION SCATTERING | | 主引用文献 | Histone chaperone exploits intrinsic disorder to switch acetylation specificity.
Nat Commun, 10, 2019
|
|
7ZVX
 | | Crystal structure of human Annexin A2 in complex with full phosphorothioate 5-10 2'-methoxyethyl DNA gapmer antisense oligonucleotide solved at 2.4 A resolution | | 分子名称: | 1,2-ETHANEDIOL, 2'-methoxyethyl DNA gapmer antisense oligonucleotide, Annexin A2, ... | | 著者 | Hyjek-Skladanowska, M, Anderson, B, Mykhaylyk, V, Orr, C, Wagner, A, Skowronek, K, Seth, P, Nowotny, M. | | 登録日 | 2022-05-17 | | 公開日 | 2022-09-14 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Structures of annexin A2-PS DNA complexes show dominance of hydrophobic interactions in phosphorothioate binding.
Nucleic Acids Res., 51, 2023
|
|
7ZVN
 | | Crystal structure of human Annexin A2 in complex with full phosphorothioate 5-10 2'-methoxyethyl DNA gapmer antisense oligonucleotide solved at 1.87 A resolution | | 分子名称: | 2'-methoxyethyl DNA gapmer antisense oligonucleotide, Annexin A2, CALCIUM ION, ... | | 著者 | Hyjek-Skladanowska, M, Anderson, B, Mykhaylyk, V, Orr, C, Wagner, A, Skowronek, K, Seth, P, Nowotny, M. | | 登録日 | 2022-05-16 | | 公開日 | 2022-09-14 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (1.87 Å) | | 主引用文献 | Structures of annexin A2-PS DNA complexes show dominance of hydrophobic interactions in phosphorothioate binding.
Nucleic Acids Res., 51, 2023
|
|
7AOA
 | | Structure of the extended MTA1/HDAC1/MBD2/RBBP4 NURD deacetylase complex | | 分子名称: | Histone deacetylase 1, Histone-binding protein RBBP4, INOSITOL HEXAKISPHOSPHATE, ... | | 著者 | Millard, C.J, Fairall, L, Ragan, T.J, Savva, C.G, Schwabe, J.W.R. | | 登録日 | 2020-10-14 | | 公開日 | 2020-11-11 | | 最終更新日 | 2024-05-01 | | 実験手法 | ELECTRON MICROSCOPY (19.4 Å) | | 主引用文献 | The topology of chromatin-binding domains in the NuRD deacetylase complex.
Nucleic Acids Res., 48, 2020
|
|
8CDK
 | |
8CDJ
 | |
7AO9
 | | Structure of the core MTA1/HDAC1/MBD2 NURD deacetylase complex | | 分子名称: | Histone deacetylase 1, INOSITOL HEXAKISPHOSPHATE, Metastasis-associated protein MTA1, ... | | 著者 | Millard, C.J, Fairall, L, Ragan, T.J, Savva, C.G, Schwabe, J.W.R. | | 登録日 | 2020-10-14 | | 公開日 | 2020-11-11 | | 最終更新日 | 2024-05-01 | | 実験手法 | ELECTRON MICROSCOPY (6.1 Å) | | 主引用文献 | The topology of chromatin-binding domains in the NuRD deacetylase complex.
Nucleic Acids Res., 48, 2020
|
|
8C2D
 | | 14-3-3 in complex with Pyrin pS208 | | 分子名称: | 14-3-3 protein sigma, MAGNESIUM ION, Pyrin pS208 peptide | | 著者 | Lau, R, Ottmann, C, Hann, M. | | 登録日 | 2022-12-22 | | 公開日 | 2023-07-26 | | 実験手法 | X-RAY DIFFRACTION (2.15 Å) | | 主引用文献 | Crystal structure and ligandability of the 14-3-3/pyrin interface.
Biochem.Biophys.Res.Commun., 651, 2023
|
|
8BZW
 | | Co-soaked stabilizers for ERa - 14-3-3 interaction (844_AZ210) | | 分子名称: | 14-3-3 protein sigma, 2-(4-chloranylphenoxy)-2-methyl-~{N}-(2-sulfanylethyl)propanamide, 4-[(2~{R})-3-azanyl-2-methyl-propyl]-7-methoxy-1-benzothiophene-2-carboximidamide, ... | | 著者 | Visser, E.J, Sijbesma, E, Ottmann, C. | | 登録日 | 2022-12-15 | | 公開日 | 2023-08-02 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.1 Å) | | 主引用文献 | From Tethered to Freestanding Stabilizers of 14-3-3 Protein-Protein Interactions through Fragment Linking.
Angew.Chem.Int.Ed.Engl., 62, 2023
|
|
8C4G
 | | Small molecule amidine soak in 14-3-3/ERa (AZ132) | | 分子名称: | 14-3-3 protein sigma, ERalpha peptide, MAGNESIUM ION, ... | | 著者 | Visser, E.J, Sijbesma, E, Ottmann, C. | | 登録日 | 2023-01-03 | | 公開日 | 2023-08-02 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.46 Å) | | 主引用文献 | From Tethered to Freestanding Stabilizers of 14-3-3 Protein-Protein Interactions through Fragment Linking.
Angew.Chem.Int.Ed.Engl., 62, 2023
|
|
