8ILR
 
 | | Cryo-EM structure of PI3Kalpha in complex with compound 16 | | Descriptor: | 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 | | Authors: | Zhou, Q, Liu, X, Neri, D, Li, W, Favalli, N, Bassi, G, Yang, S, Yang, D, Vogt, P.K, Wang, M.-W. | | Deposit date: | 2023-03-04 | | Release date: | 2023-08-30 | | Method: | ELECTRON MICROSCOPY (3.05 Å) | | Cite: | 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 | | Descriptor: | 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 | | Authors: | Zhou, Q, Liu, X, Neri, D, Li, W, Favalli, N, Bassi, G, Yang, S, Yang, D, Vogt, P.K, Wang, M.-W. | | Deposit date: | 2023-03-04 | | Release date: | 2023-09-13 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Structural insights into the interaction of three Y-shaped ligands with PI3K alpha.
Proc.Natl.Acad.Sci.USA, 120, 2023
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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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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: | 2024-05-15 | | 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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4OVV
 | | Crystal Structure of PI3Kalpha in complex with diC4-PIP2 | | Descriptor: | (2R)-3-{[(R)-HYDROXY{[(1R,2R,3S,4R,5R,6S)-2,3,6-TRIHYDROXY-4,5-BIS(PHOSPHONOOXY)CYCLOHEXYL]OXY}PHOSPHORYL]OXY}PROPANE-1 ,2-DIYL DIBUTANOATE, PHOSPHATE ION, Phosphatidylinositol 3-kinase regulatory subunit alpha, ... | | Authors: | Gabelli, S.B, Vogelstein, B, Miller, M, Amzel, L.M. | | Deposit date: | 2014-01-14 | | Release date: | 2014-09-03 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Structural basis of nSH2 regulation and lipid binding in PI3K alpha.
Oncotarget, 5, 2014
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4OVU
 | | Crystal Structure of p110alpha in complex with niSH2 of p85alpha | | Descriptor: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | Authors: | Gabelli, S.B, Vogelstein, B, Miller, M.S, Amzel, L.M. | | Deposit date: | 2014-01-14 | | Release date: | 2014-09-03 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.96 Å) | | Cite: | Structural basis of nSH2 regulation and lipid binding in PI3K alpha.
Oncotarget, 5, 2014
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5M6U
 | | HUMAN PI3KDELTA IN COMPLEX WITH LASW1579 | | Descriptor: | 4-azanyl-6-[[(1~{S})-1-(4-oxidanylidene-3-phenyl-pyrrolo[2,1-f][1,2,4]triazin-2-yl)ethyl]amino]pyrimidine-5-carbonitrile, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform | | Authors: | Segarra, V, Hernandez, B, Lozoya, E, Blaesse, M, Hoeppner, S, Jestel, A. | | Deposit date: | 2016-10-26 | | Release date: | 2017-02-01 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.85 Å) | | Cite: | Discovery of a Potent, Selective, and Orally Available PI3K delta Inhibitor for the Treatment of Inflammatory Diseases.
ACS Med Chem Lett, 8, 2017
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1HE8
 | | Ras G12V - PI 3-kinase gamma complex | | Descriptor: | MAGNESIUM ION, PHOSPHATIDYLINOSITOL 3-KINASE CATALYTIC SUBUNIT, GAMMA ISOFORM, ... | | Authors: | Pacold, M.E, Suire, S, Perisic, O, Lara-Gonzalez, S, Davis, C.T, Hawkins, P.T, Walker, E.H, Stephens, L, Eccleston, J.F, Williams, R.L. | | Deposit date: | 2000-11-20 | | Release date: | 2001-01-08 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Crystal Structure and Functional Analysis of Ras Binding to its Effector Phosphoinositide 3-Kinase Gamma
Cell(Cambridge,Mass.), 103, 2000
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6EMK
 | | Cryo-EM Structure of Saccharomyces cerevisiae Target of Rapamycin Complex 2 | | Descriptor: | Serine/threonine-protein kinase TOR2, Target of rapamycin complex 2 subunit AVO1, Target of rapamycin complex 2 subunit AVO2, ... | | Authors: | Karuppasamy, M, Kusmider, B, Oliveira, T.M, Gaubitz, C, Prouteau, M, Loewith, R, Schaffitzel, C. | | Deposit date: | 2017-10-02 | | Release date: | 2017-12-06 | | Last modified: | 2024-05-15 | | Method: | ELECTRON MICROSCOPY (7.9 Å) | | Cite: | Cryo-EM structure of Saccharomyces cerevisiae target of rapamycin complex 2.
Nat Commun, 8, 2017
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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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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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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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5C46
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5C4G
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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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5WBU
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5WBY
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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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5XGJ
 | | Crystal structure of PI3K complex with an inhibitor | | Descriptor: | 3-(4-morpholin-4-ylfuro[3,2-d]pyrimidin-2-yl)-5-[(phenylmethyl)amino]phenol, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, ... | | 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 (2.97 Å) | | Cite: | Crystal structure of PI3K complex with an inhibitor
To Be Published
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5XGH
 | | Crystal structure of PI3K complex with an inhibitor | | Descriptor: | 3-[(4-fluorophenyl)methylamino]-5-(4-morpholin-4-ylthieno[3,2-d]pyrimidin-2-yl)phenol, GLYCEROL, Phosphatidylinositol 3-kinase regulatory subunit alpha, ... | | 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 (2.97 Å) | | Cite: | New Insights into PI3K Inhibitor Design using X-ray Structures of PI3K alpha Complexed with a Potent Lead Compound.
Sci Rep, 7, 2017
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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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