6I4X
| Crystal structure of SOCS2:Elongin C:Elongin B in complex with erythropoietin receptor peptide | 分子名称: | DI(HYDROXYETHYL)ETHER, Elongin-B, Elongin-C, ... | 著者 | Kung, W.W, Ramachandran, S, Makukhin, N, Bruno, E, Ciulli, A. | 登録日 | 2018-11-12 | 公開日 | 2019-05-29 | 最終更新日 | 2019-06-19 | 実験手法 | X-RAY DIFFRACTION (2.69 Å) | 主引用文献 | Structural insights into substrate recognition by the SOCS2 E3 ubiquitin ligase. Nat Commun, 10, 2019
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6I5N
| Crystal structure of SOCS2:Elongin C:Elongin B in complex with growth hormone receptor peptide | 分子名称: | COBALT (II) ION, Elongin-B, Elongin-C, ... | 著者 | Kung, W.W, Ramachandran, S, Makukhin, N, Bruno, E, Ciulli, A. | 登録日 | 2018-11-14 | 公開日 | 2019-05-29 | 最終更新日 | 2019-06-19 | 実験手法 | X-RAY DIFFRACTION (1.98 Å) | 主引用文献 | Structural insights into substrate recognition by the SOCS2 E3 ubiquitin ligase. Nat Commun, 10, 2019
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6I5J
| Crystal structure of SOCS2:Elongin C:Elongin B in complex with growth hormone receptor peptide | 分子名称: | COBALT (II) ION, Elongin-B, Elongin-C, ... | 著者 | Kung, W.W, Ramachandran, S, Makukhin, N, Bruno, E, Ciulli, A. | 登録日 | 2018-11-13 | 公開日 | 2019-05-29 | 最終更新日 | 2019-11-20 | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | 主引用文献 | Structural insights into substrate recognition by the SOCS2 E3 ubiquitin ligase. Nat Commun, 10, 2019
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7M6T
| Crystal structure of SOCS2/ElonginB/ElonginC bound to a non-canonical peptide that enhances phospho-peptide binding | 分子名称: | Elongin-B, Elongin-C, Non-canonical peptide F3, ... | 著者 | Kershaw, N.J, Li, K, Linossi, E.M, Nicholson, S.E. | 登録日 | 2021-03-26 | 公開日 | 2021-10-13 | 最終更新日 | 2023-10-18 | 実験手法 | X-RAY DIFFRACTION (3.194 Å) | 主引用文献 | Discovery of an exosite on the SOCS2-SH2 domain that enhances SH2 binding to phosphorylated ligands. Nat Commun, 12, 2021
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7MYN
| Cryo-EM Structure of p110alpha in complex with p85alpha | 分子名称: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | 著者 | Liu, X, Yang, S, Hart, J.R, Xu, Y, Zou, X, Zhang, H, Zhou, Q, Xia, T, Zhang, Y, Yang, D, Wang, M.-W, Vogt, P.K. | 登録日 | 2021-05-21 | 公開日 | 2021-11-10 | 最終更新日 | 2021-11-17 | 実験手法 | ELECTRON MICROSCOPY (2.79 Å) | 主引用文献 | Cryo-EM structures of PI3K alpha reveal conformational changes during inhibition and activation. Proc.Natl.Acad.Sci.USA, 118, 2021
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7MYO
| Cryo-EM structure of p110alpha in complex with p85alpha inhibited by BYL-719 | 分子名称: | (2S)-N~1~-{4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl}pyrrolidine-1,2-dicarboxamide, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | 著者 | Liu, X, Yang, S, Hart, J.R, Xu, Y, Zou, X, Zhang, H, Zhou, Q, Xia, T, Zhang, Y, Yang, D, Wang, M.-W, Vogt, P.K. | 登録日 | 2021-05-21 | 公開日 | 2021-11-10 | 最終更新日 | 2021-11-24 | 実験手法 | ELECTRON MICROSCOPY (2.92 Å) | 主引用文献 | Cryo-EM structures of PI3K alpha reveal conformational changes during inhibition and activation. Proc.Natl.Acad.Sci.USA, 118, 2021
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6JMF
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8GUB
| Cryo-EM structure of cancer-specific PI3Kalpha mutant H1047R in complex with BYL-719 | 分子名称: | (2S)-N~1~-{4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl}pyrrolidine-1,2-dicarboxamide, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | 著者 | Liu, X, Zhou, Q, Hart, J.R, Xu, Y, Yang, S, Yang, D, Vogt, P.K, Wang, M.-W. | 登録日 | 2022-09-11 | 公開日 | 2022-11-23 | 実験手法 | ELECTRON MICROSCOPY (2.73 Å) | 主引用文献 | Cryo-EM structures of cancer-specific helical and kinase domain mutations of PI3K alpha. Proc.Natl.Acad.Sci.USA, 119, 2022
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8GMB
| Crystal structure of the full-length Bruton's tyrosine kinase (PH-TH domain not visible) | 分子名称: | 2-[3'-(hydroxymethyl)-1-methyl-5-({5-[(2S)-2-methyl-4-(oxetan-3-yl)piperazin-1-yl]pyridin-2-yl}amino)-6-oxo[1,6-dihydro[3,4'-bipyridine]]-2'-yl]-7,7-dimethyl-3,4,7,8-tetrahydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one, Tyrosine-protein kinase BTK | 著者 | Lin, D.Y, Andreotti, A.H. | 登録日 | 2023-03-24 | 公開日 | 2023-08-16 | 最終更新日 | 2024-01-31 | 実験手法 | X-RAY DIFFRACTION (3.4 Å) | 主引用文献 | Conformational heterogeneity of the BTK PHTH domain drives multiple regulatory states. Elife, 12, 2024
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8GWW
| Small-molecule Allosteric Regulation Mechanism of SHP2 | 分子名称: | 2-[4-(aminomethyl)-4-methyl-piperidin-1-yl]-5-[2,3-bis(chloranyl)phenyl]-3-methyl-pyrrolo[2,1-f][1,2,4]triazin-4-one, Tyrosine-protein phosphatase non-receptor type 11 | 著者 | Luo, Y, Zhu, J, Yu, K, Liu, B. | 登録日 | 2022-09-17 | 公開日 | 2023-09-20 | 実験手法 | X-RAY DIFFRACTION (3 Å) | 主引用文献 | Small-molecule Allosteric Regulation Mechanism of SHP2 To Be Published
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8H36
| Cryo-EM Structure of the KBTBD2-CUL3-Rbx1-p85a dimeric complex | 分子名称: | Cullin-3, E3 ubiquitin-protein ligase RBX1, Kelch repeat and BTB domain-containing protein 2, ... | 著者 | Hu, Y, Mao, Q, Chen, Z, Sun, L. | 登録日 | 2022-10-08 | 公開日 | 2023-10-11 | 最終更新日 | 2024-03-20 | 実験手法 | ELECTRON MICROSCOPY (4.6 Å) | 主引用文献 | Dynamic molecular architecture and substrate recruitment of cullin3-RING E3 ligase CRL3 KBTBD2. Nat.Struct.Mol.Biol., 31, 2024
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8H37
| Cryo-EM Structure of the KBTBD2-CUL3-Rbx1-p85a tetrameric complex | 分子名称: | Cullin-3, E3 ubiquitin-protein ligase RBX1, Kelch repeat and BTB domain-containing protein 2, ... | 著者 | Hu, Y, Mao, Q, Chen, Z, Sun, L. | 登録日 | 2022-10-08 | 公開日 | 2023-10-11 | 最終更新日 | 2024-03-20 | 実験手法 | ELECTRON MICROSCOPY (7.52 Å) | 主引用文献 | Dynamic molecular architecture and substrate recruitment of cullin3-RING E3 ligase CRL3 KBTBD2. Nat.Struct.Mol.Biol., 31, 2024
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8ILV
| Cryo-EM structure of PI3Kalpha in complex with compound 18 | 分子名称: | N-[(2R)-1-(ethylamino)-1-oxidanylidene-3-[3-(2-quinoxalin-6-ylethynyl)phenyl]propan-2-yl]-2,3-dimethyl-quinoxaline-6-carboxamide, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | 著者 | Zhou, Q, Liu, X, Neri, D, Li, W, Favalli, N, Bassi, G, Yang, S, Yang, D, Vogt, P.K, Wang, M.-W. | 登録日 | 2023-03-04 | 公開日 | 2023-09-06 | 実験手法 | ELECTRON MICROSCOPY (3.19 Å) | 主引用文献 | Structural insights into the interaction of three Y-shaped ligands with PI3K alpha. Proc.Natl.Acad.Sci.USA, 120, 2023
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8ILR
| Cryo-EM structure of PI3Kalpha in complex with compound 16 | 分子名称: | N-[(2S)-1-(ethylamino)-1-oxidanylidene-3-[4-(2-quinoxalin-6-ylethynyl)phenyl]propan-2-yl]-2,3-dimethyl-quinoxaline-6-carboxamide, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | 著者 | Zhou, Q, Liu, X, Neri, D, Li, W, Favalli, N, Bassi, G, Yang, S, Yang, D, Vogt, P.K, Wang, M.-W. | 登録日 | 2023-03-04 | 公開日 | 2023-08-30 | 実験手法 | ELECTRON MICROSCOPY (3.05 Å) | 主引用文献 | Structural insights into the interaction of three Y-shaped ligands with PI3K alpha. Proc.Natl.Acad.Sci.USA, 120, 2023
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8ILS
| Cryo-EM structure of PI3Kalpha in complex with compound 17 | 分子名称: | N-[(2R)-1-(ethylamino)-1-oxidanylidene-3-[4-(2-quinoxalin-6-ylethynyl)phenyl]propan-2-yl]-2,3-dimethyl-quinoxaline-6-carboxamide, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | 著者 | Zhou, Q, Liu, X, Neri, D, Li, W, Favalli, N, Bassi, G, Yang, S, Yang, D, Vogt, P.K, Wang, M.-W. | 登録日 | 2023-03-04 | 公開日 | 2023-09-13 | 実験手法 | ELECTRON MICROSCOPY (3.1 Å) | 主引用文献 | Structural insights into the interaction of three Y-shaped ligands with PI3K alpha. Proc.Natl.Acad.Sci.USA, 120, 2023
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2Y3A
| Crystal structure of p110beta in complex with icSH2 of p85beta and the drug GDC-0941 | 分子名称: | 2-(1H-indazol-4-yl)-6-{[4-(methylsulfonyl)piperazin-1-yl]methyl}-4-morpholin-4-yl-thieno[3,2-d]pyrimidine, PHOSPHATIDYLINOSITOL 3-KINASE REGULATORY SUBUNIT BETA, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT BETA ISOFORM | 著者 | Zhang, X, Vadas, O, Perisic, O, Williams, R.L. | 登録日 | 2010-12-20 | 公開日 | 2011-03-16 | 最終更新日 | 2023-12-20 | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | 主引用文献 | Structure of Lipid Kinase P110Beta-P85Beta Elucidates an Unusual Sh2-Domain-Mediated Inhibitory Mechanism. Mol.Cell, 41, 2011
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8CBH
| SHP2 in complex with a novel allosteric inhibitor | 分子名称: | Tyrosine-protein phosphatase non-receptor type 11, [(1~{S},6~{R},7~{S})-3-[3-[2,3-bis(chloranyl)phenyl]-2~{H}-pyrazolo[3,4-b]pyrazin-6-yl]-7-(4-methyl-1,3-thiazol-2-yl)-3-azabicyclo[4.1.0]heptan-7-yl]methanamine | 著者 | di Fabio, R, Petrocchi, A. | 登録日 | 2023-01-25 | 公開日 | 2023-04-26 | 実験手法 | X-RAY DIFFRACTION (2.24 Å) | 主引用文献 | Discovery of a Novel Series of Imidazopyrazine Derivatives as Potent SHP2 Allosteric Inhibitors. Acs Med.Chem.Lett., 14, 2023
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8D3F
| Crystal structure of human STAT1 in complex with the repeat region from Toxoplasma protein TgIST | 分子名称: | Signal transducer and activator of transcription 1-alpha/beta,Inhibitor of STAT1-dependent transcription TgIST | 著者 | Huang, Z, Liu, H, Nix, J.C, Amarasinghe, G.K, Sibley, L.D. | 登録日 | 2022-06-01 | 公開日 | 2022-07-06 | 最終更新日 | 2023-10-25 | 実験手法 | X-RAY DIFFRACTION (2.97 Å) | 主引用文献 | The intrinsically disordered protein TgIST from Toxoplasma gondii inhibits STAT1 signaling by blocking cofactor recruitment. Nat Commun, 13, 2022
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8DCX
| PI 3-kinase alpha with nanobody 3-159 | 分子名称: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | 著者 | Hart, J.R, Liu, X, Pan, C, Liang, A, Ueno, L, Xu, Y, Quezada, A, Zou, X, Yang, S, Zhou, Q, Schoonooghe, S, Hassanzadeh-Ghassabeh, G, Xia, T, Shui, W, Yang, D, Vogt, P.K, Wang, M.-W. | 登録日 | 2022-06-17 | 公開日 | 2022-09-21 | 実験手法 | ELECTRON MICROSCOPY (2.8 Å) | 主引用文献 | Nanobodies and chemical cross-links advance the structural and functional analysis of PI3K alpha. Proc.Natl.Acad.Sci.USA, 119, 2022
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8DCP
| PI 3-kinase alpha with nanobody 3-126 | 分子名称: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | 著者 | Hart, J.R, Liu, X, Pan, C, Liang, A, Ueno, L, Xu, Y, Quezada, A, Zou, X, Yang, S, Zhou, Q, Schoonooghe, S, Hassanzadeh-Ghassabeh, G, Xia, T, Shui, W, Yang, D, Vogt, P.K, Wang, M.-W. | 登録日 | 2022-06-17 | 公開日 | 2022-09-21 | 実験手法 | ELECTRON MICROSCOPY (2.41 Å) | 主引用文献 | Nanobodies and chemical cross-links advance the structural and functional analysis of PI3K alpha. Proc.Natl.Acad.Sci.USA, 119, 2022
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8DD4
| PI 3-kinase alpha with nanobody 3-142 | 分子名称: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | 著者 | Hart, J.R, Liu, X, Pan, C, Liang, A, Ueno, L, Xu, Y, Quezada, A, Zou, X, Yang, S, Zhou, Q, Schoonooghe, S, Hassanzadeh-Ghassabeh, G, Xia, T, Shui, W, Yang, D, Vogt, P.K, Wang, M.-W. | 登録日 | 2022-06-17 | 公開日 | 2022-09-21 | 実験手法 | ELECTRON MICROSCOPY (3.1 Å) | 主引用文献 | Nanobodies and chemical cross-links advance the structural and functional analysis of PI3K alpha. Proc.Natl.Acad.Sci.USA, 119, 2022
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8DD8
| PI 3-kinase alpha with nanobody 3-142, crosslinked with DSG | 分子名称: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | 著者 | Hart, J.R, Liu, X, Pan, C, Liang, A, Ueno, L, Xu, Y, Quezada, A, Zou, X, Yang, S, Zhou, Q, Schoonooghe, S, Hassanzadeh-Ghassabeh, G, Xia, T, Shui, W, Yang, D, Vogt, P.K, Wang, M.-W. | 登録日 | 2022-06-17 | 公開日 | 2022-09-21 | 実験手法 | ELECTRON MICROSCOPY (3.4 Å) | 主引用文献 | Nanobodies and chemical cross-links advance the structural and functional analysis of PI3K alpha. Proc.Natl.Acad.Sci.USA, 119, 2022
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8DGQ
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8DGO
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3BKB
| Crystal structure of human Feline Sarcoma Viral Oncogene Homologue (v-FES) | 分子名称: | 1,2-ETHANEDIOL, Proto-oncogene tyrosine-protein kinase Fes/Fps, STAUROSPORINE, ... | 著者 | Filippakopoulos, P, Salah, E, Fedorov, O, Cooper, C, Ugochukwu, E, Pike, A.C.W, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Knapp, S, Structural Genomics Consortium (SGC) | 登録日 | 2007-12-06 | 公開日 | 2007-12-25 | 最終更新日 | 2023-08-30 | 実験手法 | X-RAY DIFFRACTION (1.78 Å) | 主引用文献 | Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation Cell(Cambridge,Mass.), 134, 2008
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