4YKN
 
 | | Pi3K alpha lipid kinase with Active Site Inhibitor | | Descriptor: | 3-(6-methoxypyridin-3-yl)-5-[({4-[(5-methyl-1,3,4-thiadiazol-2-yl)sulfamoyl]phenyl}amino)methyl]benzoic acid, Phosphatidylinositol 3-kinase regulatory subunit alpha,Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform fusion protein | | Authors: | Elkins, P.A. | | Deposit date: | 2015-03-04 | | Release date: | 2015-06-17 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Discovery of a Potent Class of PI3K alpha Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).
Acs Med.Chem.Lett., 6, 2015
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4ZOP
 | | Co-crystal Structure of Lipid Kinase PI3K alpha with a selective phosphatidylinositol-3 kinase alpha inhibitor | | Descriptor: | (2S,3R)-N~1~-(8-tert-butyl-4,5-dihydro[1,3]thiazolo[4,5-h]quinazolin-2-yl)-3-methylpyrrolidine-1,2-dicarboxamide, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | Authors: | Knapp, M.S, Elling, R.A. | | Deposit date: | 2015-05-06 | | Release date: | 2016-05-18 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.62 Å) | | Cite: | Co-crystal Structure of the Lipid Kinase PI3K alpha with a selective phosphatidylinositol-3 kinase alpha inhibitorCo-crystal Structure of the Lipid Kinase PI3K alpha with a selective phosphatidylinositol-3 kinase alpha inhibitor
To Be Published
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6NCT
 | | Structure of p110alpha/niSH2 - vector data collection | | Descriptor: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, SULFATE ION, ... | | Authors: | Miller, M.S, Maheshwari, S, Amzel, L.M, Gabelli, S.B. | | Deposit date: | 2018-12-12 | | Release date: | 2019-02-06 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.35 Å) | | Cite: | Getting the Most Out of Your Crystals: Data Collection at the New High-Flux, Microfocus MX Beamlines at NSLS-II.
Molecules, 24, 2019
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5XGI
 | | Crystal structure of PI3K complex with an inhibitor | | Descriptor: | 3-azanyl-5-(4-morpholin-4-ylthieno[3,2-d]pyrimidin-2-yl)phenol, GLYCEROL, HEXAETHYLENE GLYCOL, ... | | Authors: | Song, K, Yang, X, Zhao, Y, Jian, Z. | | Deposit date: | 2017-04-13 | | Release date: | 2018-04-25 | | Last modified: | 2024-03-27 | | Method: | X-RAY DIFFRACTION (2.56 Å) | | Cite: | Crystal structure of PI3K complex with an inhibitor
To Be Published
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5Y81
 | | NuA4 TEEAA sub-complex | | Descriptor: | Actin, Actin-related protein 4, Chromatin modification-related protein EAF1, ... | | Authors: | Wang, X, Cai, G. | | Deposit date: | 2017-08-18 | | Release date: | 2018-04-18 | | Last modified: | 2019-11-06 | | Method: | ELECTRON MICROSCOPY (4.7 Å) | | Cite: | Architecture of the Saccharomyces cerevisiae NuA4/TIP60 complex
Nat Commun, 9, 2018
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5H64
 | | Cryo-EM structure of mTORC1 | | Descriptor: | Regulatory-associated protein of mTOR, Serine/threonine-protein kinase mTOR, Target of rapamycin complex subunit LST8 | | Authors: | Yang, H, Wang, J, Liu, M, Chen, X, Huang, M, Tan, D, Dong, M, Wong, C.C.L, Wang, J, Xu, Y, Wang, H. | | Deposit date: | 2016-11-10 | | Release date: | 2017-01-25 | | Last modified: | 2019-11-06 | | Method: | ELECTRON MICROSCOPY (4.4 Å) | | Cite: | 4.4 angstrom Resolution Cryo-EM structure of human mTOR Complex 1
Protein Cell, 7, 2016
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5ZCS
 | | 4.9 Angstrom Cryo-EM structure of human mTOR complex 2 | | Descriptor: | Rapamycin-insensitive companion of mTOR, Serine/threonine-protein kinase mTOR, Target of rapamycin complex 2 subunit MAPKAP1, ... | | Authors: | Chen, X, Liu, M, Tian, Y, Wang, H, Wang, J, Xu, Y. | | Deposit date: | 2018-02-20 | | Release date: | 2018-03-21 | | Last modified: | 2024-03-27 | | Method: | ELECTRON MICROSCOPY (4.9 Å) | | Cite: | Cryo-EM structure of human mTOR complex 2.
Cell Res., 28, 2018
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3HHM
 | | Crystal structure of p110alpha H1047R mutant in complex with niSH2 of p85alpha and the drug wortmannin | | Descriptor: | (1S,6BR,9AS,11R,11BR)-9A,11B-DIMETHYL-1-[(METHYLOXY)METHYL]-3,6,9-TRIOXO-1,6,6B,7,8,9,9A,10,11,11B-DECAHYDRO-3H-FURO[4, 3,2-DE]INDENO[4,5-H][2]BENZOPYRAN-11-YL ACETATE, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, ... | | Authors: | Amzel, L.M, Vogelstein, B, Gabelli, S.B, Mandelker, D. | | Deposit date: | 2009-05-15 | | Release date: | 2009-09-29 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | A frequent kinase domain mutation that changes the interaction between PI3K{alpha} and the membrane.
Proc.Natl.Acad.Sci.USA, 106, 2009
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3HIZ
 | | Crystal structure of p110alpha H1047R mutant in complex with niSH2 of p85alpha | | Descriptor: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | Authors: | Amzel, L.M, Vogelstein, B, Gabelli, S.B, Mandelker, D. | | Deposit date: | 2009-05-20 | | Release date: | 2009-09-29 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (3.3 Å) | | Cite: | A frequent kinase domain mutation that changes the interaction between PI3K{alpha} and the membrane.
Proc.Natl.Acad.Sci.USA, 106, 2009
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5ITD
 | | Crystal structure of PI3K alpha with PI3K delta inhibitor | | Descriptor: | 5-{4-[3-(4-acetylpiperazine-1-carbonyl)phenyl]quinazolin-6-yl}-2-methoxypyridine-3-carbonitrile, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | Authors: | Knapp, M.S, Elling, R.A. | | Deposit date: | 2016-03-16 | | Release date: | 2016-09-07 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (3.02 Å) | | Cite: | Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.
Acs Med.Chem.Lett., 7, 2016
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5KC2
 | | Negative stain structure of Vps15/Vps34 complex | | Descriptor: | Phosphatidylinositol 3-kinase VPS34, Serine/threonine-protein kinase VPS15 | | Authors: | Kirsten, M.L, Zhang, L, Ohashi, Y, Perisic, O, Williams, R.L, Sachse, C. | | Deposit date: | 2016-06-04 | | Release date: | 2016-10-05 | | Last modified: | 2019-11-13 | | Method: | ELECTRON MICROSCOPY (28 Å) | | Cite: | Characterization of Atg38 and NRBF2, a fifth subunit of the autophagic Vps34/PIK3C3 complex.
Autophagy, 12, 2016
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6BCX
 | | mTORC1 structure refined to 3.0 angstroms | | Descriptor: | ADENOSINE-5'-TRIPHOSPHATE, Eukaryotic translation initiation factor 4E-binding protein 1, MAGNESIUM ION, ... | | Authors: | Pavletich, N.P, Yang, H. | | Deposit date: | 2017-10-20 | | Release date: | 2017-12-20 | | Last modified: | 2024-03-13 | | Method: | ELECTRON MICROSCOPY (3.23 Å) | | Cite: | Mechanisms of mTORC1 activation by RHEB and inhibition by PRAS40.
Nature, 552, 2017
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6BCU
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8ESC
 | | Structure of the Yeast NuA4 Histone Acetyltransferase Complex | | Descriptor: | ADENOSINE-5'-TRIPHOSPHATE, Actin, Actin-related protein 4, ... | | Authors: | Patel, A.B, Zukin, S.A, Nogales, E. | | Deposit date: | 2022-10-13 | | Release date: | 2022-11-16 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Structure and flexibility of the yeast NuA4 histone acetyltransferase complex.
Elife, 11, 2022
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4A55
 | | Crystal structure of p110alpha in complex with iSH2 of p85alpha and the inhibitor PIK-108 | | Descriptor: | PHOSPHATIDYLINOSITOL 3-KINASE REGULATORY SUBUNIT ALPHA, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT ALPHA ISOFORM, PIK-108 | | Authors: | Hon, W.-C, Berndt, A, Williams, R.L. | | Deposit date: | 2011-10-24 | | Release date: | 2011-12-28 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Regulation of Lipid Binding Underlies the Activation Mechanism of Class Ia Pi3-Kinases.
Oncogene, 31, 2012
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7TZ7
 | | PI3K alpha in complex with an inhibitor | | Descriptor: | (4S,5R)-3-[2'-amino-2-(morpholin-4-yl)-4'-(trifluoromethyl)[4,5'-bipyrimidin]-6-yl]-4-(hydroxymethyl)-5-methyl-1,3-oxazolidin-2-one, Isoform 3 of Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | Authors: | Knapp, M.S, Tang, J. | | Deposit date: | 2022-02-15 | | Release date: | 2022-05-18 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.41 Å) | | Cite: | Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.
J.Med.Chem., 65, 2022
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7TZO
 | | The apo structure of human mTORC2 complex | | Descriptor: | Rapamycin-insensitive companion of mTOR, Serine/threonine-protein kinase mTOR, Target of rapamycin complex 2 subunit MAPKAP1, ... | | Authors: | Yu, Z, Chen, J, Pearce, D. | | Deposit date: | 2022-02-16 | | Release date: | 2023-01-11 | | Method: | ELECTRON MICROSCOPY (3.28 Å) | | Cite: | Interactions between mTORC2 core subunits Rictor and mSin1 dictate selective and context-dependent phosphorylation of substrate kinases SGK1 and Akt.
J.Biol.Chem., 298, 2022
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8GUB
 | | Cryo-EM structure of cancer-specific PI3Kalpha mutant H1047R in complex with BYL-719 | | Descriptor: | (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 | | Authors: | Liu, X, Zhou, Q, Hart, J.R, Xu, Y, Yang, S, Yang, D, Vogt, P.K, Wang, M.-W. | | Deposit date: | 2022-09-11 | | Release date: | 2022-11-23 | | Method: | ELECTRON MICROSCOPY (2.73 Å) | | Cite: | 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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8H7G
 | | Cryo-EM structure of the human SAGA complex | | Descriptor: | Ataxin-7, STAGA complex 65 subunit gamma, Splicing factor 3B subunit 3, ... | | Authors: | Huang, J, Zhang, Y. | | Deposit date: | 2022-10-20 | | Release date: | 2022-12-14 | | Method: | ELECTRON MICROSCOPY (3.7 Å) | | Cite: | Cryo-EM structure of human SAGA transcriptional coactivator complex.
Cell Discov, 8, 2022
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7UXC
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7UXH
 | | cryo-EM structure of the mTORC1-TFEB-Rag-Ragulator complex | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, INOSITOL HEXAKISPHOSPHATE, ... | | Authors: | Cui, Z, Hurley, J. | | Deposit date: | 2022-05-05 | | Release date: | 2022-11-30 | | Last modified: | 2023-03-01 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Structure of the lysosomal mTORC1-TFEB-Rag-Ragulator megacomplex.
Nature, 614, 2023
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7VVY
 | | TRA module of NuA4 | | Descriptor: | ADENOSINE-5'-TRIPHOSPHATE, Actin, Actin-related protein 4, ... | | Authors: | Chen, Z, Qu, K. | | Deposit date: | 2021-11-09 | | Release date: | 2022-08-10 | | Last modified: | 2022-11-02 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Structure of the NuA4 acetyltransferase complex bound to the nucleosome.
Nature, 610, 2022
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7VVZ
 | | NuA4 bound to the nucleosome | | Descriptor: | ADENOSINE-5'-TRIPHOSPHATE, Actin, Actin-related protein 4, ... | | Authors: | Qu, K, Chen, Z. | | Deposit date: | 2021-11-09 | | Release date: | 2022-08-10 | | Last modified: | 2022-11-16 | | Method: | ELECTRON MICROSCOPY (8.8 Å) | | Cite: | Structure of the NuA4 acetyltransferase complex bound to the nucleosome.
Nature, 610, 2022
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4D0M
 | | Phosphatidylinositol 4-kinase III beta in a complex with Rab11a-GTP- gamma-S and the Rab-binding domain of FIP3 | | Descriptor: | 5'-GUANOSINE-DIPHOSPHATE-MONOTHIOPHOSPHATE, MAGNESIUM ION, N-(5-(4-CHLORO-3-(2-HYDROXY-ETHYLSULFAMOYL)- PHENYLTHIAZOLE-2-YL)-ACETAMIDE, ... | | Authors: | Burke, J.E, Inglis, A.J, Perisic, O, Masson, G.R, McLaughlin, S.H, Rutaganira, F, Shokat, K.M, Williams, R.L. | | Deposit date: | 2014-04-29 | | Release date: | 2014-05-28 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (6 Å) | | Cite: | Structures of Pi4Kiiibeta Complexes Show Simultaneous Recruitment of Rab11 and its Effectors.
Science, 344, 2014
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4D0L
 | | Phosphatidylinositol 4-kinase III beta-PIK93 in a complex with Rab11a- GTP gammaS | | Descriptor: | 5'-GUANOSINE-DIPHOSPHATE-MONOTHIOPHOSPHATE, MAGNESIUM ION, N-(5-(4-CHLORO-3-(2-HYDROXY-ETHYLSULFAMOYL)- PHENYLTHIAZOLE-2-YL)-ACETAMIDE, ... | | Authors: | Burke, J.E, Inglis, A.J, Perisic, O, Masson, G.R, McLaughin, S.H, Rutaganira, F, Shokat, K.M, Williams, R.L. | | Deposit date: | 2014-04-29 | | Release date: | 2014-05-28 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.94 Å) | | Cite: | Structures of Pi4Kiiibeta Complexes Show Simultaneous Recruitment of Rab11 and its Effectors.
Science, 344, 2014
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