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8W9A
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BU of 8w9a by Molmil
CryoEM structure of human PI3K-alpha (P85/P110-H1047R) with QR-7909 binding at an allosteric site
Descriptor: 6-chloranyl-3-[[(1R)-1-[2-(1,3-dihydropyrrolo[3,4-c]pyridin-2-yl)-3,6-dimethyl-4-oxidanylidene-quinazolin-8-yl]ethyl]amino]pyridine-2-carboxylic acid, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Authors:Huang, X, Ren, X, Zhong, W.
Deposit date:2023-09-05
Release date:2024-04-17
Last modified:2024-07-24
Method:ELECTRON MICROSCOPY (2.7 Å)
Cite:Cryo-EM structures reveal two allosteric inhibition modes of PI3K alpha H1047R involving a re-shaping of the activation loop.
Structure, 32, 2024
8TU6
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BU of 8tu6 by Molmil
CryoEM structure of PI3Kalpha
Descriptor: Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Authors:Valverde, R, Shi, H, Holliday, M.
Deposit date:2023-08-15
Release date:2023-11-15
Last modified:2024-02-21
Method:ELECTRON MICROSCOPY (3.12 Å)
Cite:Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3K alpha Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia.
Cancer Discov, 14, 2024
8ILR
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BU of 8ilr by Molmil
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
8ILV
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BU of 8ilv by Molmil
Cryo-EM structure of PI3Kalpha in complex with compound 18
Descriptor: 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
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:2023-09-06
Method:ELECTRON MICROSCOPY (3.19 Å)
Cite:Structural insights into the interaction of three Y-shaped ligands with PI3K alpha.
Proc.Natl.Acad.Sci.USA, 120, 2023
8ILS
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BU of 8ils by Molmil
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
8H36
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BU of 8h36 by Molmil
Cryo-EM Structure of the KBTBD2-CUL3-Rbx1-p85a dimeric complex
Descriptor: Cullin-3, E3 ubiquitin-protein ligase RBX1, Kelch repeat and BTB domain-containing protein 2, ...
Authors:Hu, Y, Mao, Q, Chen, Z, Sun, L.
Deposit date:2022-10-08
Release date:2023-10-11
Last modified:2024-03-20
Method:ELECTRON MICROSCOPY (4.6 Å)
Cite:Dynamic molecular architecture and substrate recruitment of cullin3-RING E3 ligase CRL3 KBTBD2.
Nat.Struct.Mol.Biol., 31, 2024
8H37
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BU of 8h37 by Molmil
Cryo-EM Structure of the KBTBD2-CUL3-Rbx1-p85a tetrameric complex
Descriptor: Cullin-3, E3 ubiquitin-protein ligase RBX1, Kelch repeat and BTB domain-containing protein 2, ...
Authors:Hu, Y, Mao, Q, Chen, Z, Sun, L.
Deposit date:2022-10-08
Release date:2023-10-11
Last modified:2024-03-20
Method:ELECTRON MICROSCOPY (7.52 Å)
Cite:Dynamic molecular architecture and substrate recruitment of cullin3-RING E3 ligase CRL3 KBTBD2.
Nat.Struct.Mol.Biol., 31, 2024
8GUB
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BU of 8gub by Molmil
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
Last modified:2024-07-03
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
8DCP
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BU of 8dcp by Molmil
PI 3-kinase alpha with nanobody 3-126
Descriptor: Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Authors: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.
Deposit date:2022-06-17
Release date:2022-09-21
Last modified:2024-06-12
Method:ELECTRON MICROSCOPY (2.41 Å)
Cite:Nanobodies and chemical cross-links advance the structural and functional analysis of PI3K alpha.
Proc.Natl.Acad.Sci.USA, 119, 2022
8DD4
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BU of 8dd4 by Molmil
PI 3-kinase alpha with nanobody 3-142
Descriptor: Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Authors: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.
Deposit date:2022-06-17
Release date:2022-09-21
Last modified:2024-06-12
Method:ELECTRON MICROSCOPY (3.1 Å)
Cite:Nanobodies and chemical cross-links advance the structural and functional analysis of PI3K alpha.
Proc.Natl.Acad.Sci.USA, 119, 2022
8DD8
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BU of 8dd8 by Molmil
PI 3-kinase alpha with nanobody 3-142, crosslinked with DSG
Descriptor: Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Authors: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.
Deposit date:2022-06-17
Release date:2022-09-21
Last modified:2024-06-12
Method:ELECTRON MICROSCOPY (3.4 Å)
Cite:Nanobodies and chemical cross-links advance the structural and functional analysis of PI3K alpha.
Proc.Natl.Acad.Sci.USA, 119, 2022
8DCX
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BU of 8dcx by Molmil
PI 3-kinase alpha with nanobody 3-159
Descriptor: Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Authors: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.
Deposit date:2022-06-17
Release date:2022-09-21
Last modified:2024-06-12
Method:ELECTRON MICROSCOPY (2.8 Å)
Cite:Nanobodies and chemical cross-links advance the structural and functional analysis of PI3K alpha.
Proc.Natl.Acad.Sci.USA, 119, 2022
7TPB
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BU of 7tpb by Molmil
p120RasGAP SH3 domain in complex with DLC1 RhoGAP domain
Descriptor: Ras GTPase-activating protein 1, Rho GTPase-activating protein 7
Authors:Stiegler, A.L, Boggon, T.J, Chau, J.E, Vish, K.J.
Deposit date:2022-01-25
Release date:2022-08-03
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (3.2 Å)
Cite:SH3 domain regulation of RhoGAP activity: Crosstalk between p120RasGAP and DLC1 RhoGAP.
Nat Commun, 13, 2022
7QTM
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BU of 7qtm by Molmil
Transition state analogue of small G protein in complex with relevant GAP
Descriptor: GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, Rho GTPase-activating protein 1, ...
Authors:Baumann, P, Jin, Y.
Deposit date:2022-01-14
Release date:2023-01-25
Last modified:2024-01-31
Method:X-RAY DIFFRACTION (2.25 Å)
Cite:Transition state analogue of small G protein in complex with relevant GAP
To Be Published
7QSC
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BU of 7qsc by Molmil
GTPase IN COMPLEX WITH GDP.MGF3-
Descriptor: GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, Rho GTPase-activating protein 1, ...
Authors:Baumann, P, Jin, Y.
Deposit date:2022-01-13
Release date:2023-01-25
Last modified:2024-02-07
Method:X-RAY DIFFRACTION (1.91 Å)
Cite:GTPase IN COMPLEX WITH GDP.MGF3-
To Be Published
7MYN
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BU of 7myn by Molmil
Cryo-EM Structure of p110alpha in complex with p85alpha
Descriptor: Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Authors: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.
Deposit date:2021-05-21
Release date:2021-11-10
Last modified:2024-05-29
Method:ELECTRON MICROSCOPY (2.79 Å)
Cite:Cryo-EM structures of PI3K alpha reveal conformational changes during inhibition and activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
7MYO
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BU of 7myo by Molmil
Cryo-EM structure of p110alpha in complex with p85alpha inhibited by 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, 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.
Deposit date:2021-05-21
Release date:2021-11-10
Last modified:2024-05-29
Method:ELECTRON MICROSCOPY (2.92 Å)
Cite:Cryo-EM structures of PI3K alpha reveal conformational changes during inhibition and activation.
Proc.Natl.Acad.Sci.USA, 118, 2021
6R3V
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BU of 6r3v by Molmil
Crystal Structure of RhoA-GDP-Pi in Complex with RhoGAP
Descriptor: 2,3-DIHYDROXY-1,4-DITHIOBUTANE, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, GUANOSINE-5'-DIPHOSPHATE, ...
Authors:Jin, Y.
Deposit date:2019-03-21
Release date:2019-05-08
Last modified:2024-01-24
Method:X-RAY DIFFRACTION (1.75 Å)
Cite:A GAP-GTPase-GDP-PiIntermediate Crystal Structure Analyzed by DFT Shows GTP Hydrolysis Involves Serial Proton Transfers.
Chemistry, 25, 2019
6MRP
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BU of 6mrp by Molmil
Structure of the Bovine p85a BH domain R228E mutant
Descriptor: Phosphatidylinositol 3-kinase regulatory subunit alpha
Authors:Moore, S.A, Marshall, J.D, Anderson, D.H.
Deposit date:2018-10-15
Release date:2019-01-30
Last modified:2024-04-03
Method:X-RAY DIFFRACTION (2.403 Å)
Cite:Insight into the PTEN - p85 alpha interaction and lipid binding properties of the p85 alpha BH domain.
Oncotarget, 9, 2018
6GVC
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BU of 6gvc by Molmil
Structure of ArhGAP12 bound to G-Actin
Descriptor: 1,2-ETHANEDIOL, ADENOSINE-5'-TRIPHOSPHATE, Actin, ...
Authors:Mouilleron, S, Treisman, R, Diring, J.
Deposit date:2018-06-20
Release date:2019-03-27
Last modified:2024-01-17
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:RPEL-family rhoGAPs link Rac/Cdc42 GTP loading to G-actin availability.
Nat.Cell Biol., 21, 2019
6D85
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BU of 6d85 by Molmil
Structure of the Bovine p85a BH domain E217K mutant
Descriptor: Phosphatidylinositol 3-kinase regulatory subunit alpha, SULFATE ION
Authors:Moore, S.A, Marshall, J.D, Anderson, D.H.
Deposit date:2018-04-25
Release date:2018-05-23
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (2.203 Å)
Cite:Patient-derived mutations within the N-terminal domains of p85 alpha impact PTEN or Rab5 binding and regulation.
Sci Rep, 8, 2018
6D81
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BU of 6d81 by Molmil
Structure of the Bovine p85a BH domain
Descriptor: Phosphatidylinositol 3-kinase regulatory subunit alpha, SULFATE ION
Authors:Moore, S.A, Marshall, J.D, Anderson, D.H.
Deposit date:2018-04-25
Release date:2018-05-23
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (2.248 Å)
Cite:Patient-derived mutations within the N-terminal domains of p85 alpha impact PTEN or Rab5 binding and regulation.
Sci Rep, 8, 2018
6D82
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BU of 6d82 by Molmil
Structure of the Bovine p85a BH domain
Descriptor: Phosphatidylinositol 3-kinase regulatory subunit alpha, SULFATE ION
Authors:Moore, S.A, Marshall, J.D, Anderson, D.H.
Deposit date:2018-04-25
Release date:2018-05-23
Last modified:2020-01-08
Method:X-RAY DIFFRACTION (2.407 Å)
Cite:Patient-derived mutations within the N-terminal domains of p85 alpha impact PTEN or Rab5 binding and regulation.
Sci Rep, 8, 2018
6D86
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BU of 6d86 by Molmil
Structure of the Bovine p85a BH domain
Descriptor: Phosphatidylinositol 3-kinase regulatory subunit alpha, SULFATE ION
Authors:Moore, S.A, Marshall, J.D, Anderson, D.H.
Deposit date:2018-04-25
Release date:2018-05-23
Last modified:2020-01-08
Method:X-RAY DIFFRACTION (2.301 Å)
Cite:Patient-derived mutations within the N-terminal domains of p85 alpha impact PTEN or Rab5 binding and regulation.
Sci Rep, 8, 2018
6D87
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BU of 6d87 by Molmil
Structure of the Bovine p85alpha BH domain, R262T mutant
Descriptor: Phosphatidylinositol 3-kinase regulatory subunit alpha, SULFATE ION
Authors:Moore, S.A, Marshall, J.D, Anderson, D.H.
Deposit date:2018-04-25
Release date:2018-05-23
Last modified:2023-11-15
Method:X-RAY DIFFRACTION (2.7 Å)
Cite:Patient-derived mutations within the N-terminal domains of p85 alpha impact PTEN or Rab5 binding and regulation.
Sci Rep, 8, 2018

 

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