2QV2
 
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3QIS
 | | Recognition of the F&H motif by the Lowe Syndrome protein OCRL | | 分子名称: | Inositol polyphosphate 5-phosphatase OCRL-1, Protein FAM109A | | 著者 | Pirruccello, M, Swan, L.E, Folta-Stogniew, E, De Camilli, P. | | 登録日 | 2011-01-27 | | 公開日 | 2011-06-15 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Recognition of the F&H motif by the Lowe syndrome protein OCRL.
Nat.Struct.Mol.Biol., 18, 2011
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2MBG
 | | Rlip76 (gap-gbd) | | 分子名称: | RalA-binding protein 1 | | 著者 | Rajasekar, K.V, Campbell, L.J, Nietlispach, D, Owen, D, Mott, H.R. | | 登録日 | 2013-07-30 | | 公開日 | 2013-12-04 | | 最終更新日 | 2024-05-15 | | 実験手法 | SOLUTION NMR | | 主引用文献 | The Structure of the RLIP76 RhoGAP-Ral Binding Domain Dyad: Fixed Position of the Domains Leads to Dual Engagement of Small G Proteins at the Membrane.
Structure, 21, 2013
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1AM4
 | | COMPLEX BETWEEN CDC42HS.GMPPNP AND P50 RHOGAP (H. SAPIENS) | | 分子名称: | CDC42HS, MAGNESIUM ION, P50-RHOGAP, ... | | 著者 | Rittinger, K, Walker, P, Gamblin, S.J, Smerdon, S.J. | | 登録日 | 1997-06-22 | | 公開日 | 1998-07-15 | | 最終更新日 | 2024-05-22 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Crystal structure of a small G protein in complex with the GTPase-activating protein rhoGAP.
Nature, 388, 1997
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1XA6
 | | Crystal Structure of the Human Beta2-Chimaerin | | 分子名称: | Beta2-chimaerin, ZINC ION | | 著者 | Canagarajah, B, Leskow, F.C, Ho, J.Y, Mischak, H, Saidi, L.F, Kazanietz, M.G, Hurley, J.H. | | 登録日 | 2004-08-25 | | 公開日 | 2004-11-23 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Structural mechanism for lipid activation of the Rac-specific GAP, beta2-chimaerin.
Cell(Cambridge,Mass.), 119, 2004
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6GVC
 | | Structure of ArhGAP12 bound to G-Actin | | 分子名称: | 1,2-ETHANEDIOL, ADENOSINE-5'-TRIPHOSPHATE, Actin, ... | | 著者 | Mouilleron, S, Treisman, R, Diring, J. | | 登録日 | 2018-06-20 | | 公開日 | 2019-03-27 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | RPEL-family rhoGAPs link Rac/Cdc42 GTP loading to G-actin availability.
Nat.Cell Biol., 21, 2019
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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 | | 最終更新日 | 2024-07-03 | | 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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6R3V
 | | Crystal Structure of RhoA-GDP-Pi in Complex with RhoGAP | | 分子名称: | 2,3-DIHYDROXY-1,4-DITHIOBUTANE, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, GUANOSINE-5'-DIPHOSPHATE, ... | | 著者 | Jin, Y. | | 登録日 | 2019-03-21 | | 公開日 | 2019-05-08 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (1.75 Å) | | 主引用文献 | A GAP-GTPase-GDP-PiIntermediate Crystal Structure Analyzed by DFT Shows GTP Hydrolysis Involves Serial Proton Transfers.
Chemistry, 25, 2019
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3MSX
 | | Crystal structure of RhoA.GDP.MgF3 in complex with GAP domain of ArhGAP20 | | 分子名称: | GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, Rho GTPase-activating protein 20, ... | | 著者 | Utepbergenov, D, Cooper, D.R, Derewenda, U, Derewenda, Z.S. | | 登録日 | 2010-04-29 | | 公開日 | 2011-03-16 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | Mechanism of molecular specificity of RhoGAP domains towards small GTPases of RhoA family.
To be Published
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7QSC
 | | GTPase IN COMPLEX WITH GDP.MGF3- | | 分子名称: | GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, Rho GTPase-activating protein 1, ... | | 著者 | Baumann, P, Jin, Y. | | 登録日 | 2022-01-13 | | 公開日 | 2023-01-25 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (1.91 Å) | | 主引用文献 | GTPase IN COMPLEX WITH GDP.MGF3-
To Be Published
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7QTM
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8TU6
 | | CryoEM structure of PI3Kalpha | | 分子名称: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | 著者 | Valverde, R, Shi, H, Holliday, M. | | 登録日 | 2023-08-15 | | 公開日 | 2023-11-15 | | 最終更新日 | 2024-02-21 | | 実験手法 | ELECTRON MICROSCOPY (3.12 Å) | | 主引用文献 | 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
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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 | 2024-05-29 | | 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 | 2024-05-29 | | 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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1TX4
 | | RHO/RHOGAP/GDP(DOT)ALF4 COMPLEX | | 分子名称: | GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, P50-RHOGAP, ... | | 著者 | Rittinger, K, Walker, P.A, Smerdon, S.J, Gamblin, S.J. | | 登録日 | 1997-07-29 | | 公開日 | 1998-09-16 | | 最終更新日 | 2024-05-22 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | Structure at 1.65 A of RhoA and its GTPase-activating protein in complex with a transition-state analogue.
Nature, 389, 1997
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8W9A
 | | CryoEM structure of human PI3K-alpha (P85/P110-H1047R) with QR-7909 binding at an allosteric site | | 分子名称: | 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 | | 著者 | Huang, X, Ren, X, Zhong, W. | | 登録日 | 2023-09-05 | | 公開日 | 2024-04-17 | | 最終更新日 | 2024-05-08 | | 実験手法 | ELECTRON MICROSCOPY (2.7 Å) | | 主引用文献 | Cryo-EM structures reveal two allosteric inhibition modes of PI3K alpha H1047R involving a re-shaping of the activation loop.
Structure, 2024
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1OW3
 | | Crystal Structure of RhoA.GDP.MgF3-in Complex with RhoGAP | | 分子名称: | GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, Rho-GTPase-activating protein 1, ... | | 著者 | Graham, D.L, Lowe, P.N, Grime, G.W, Marsh, M, Rittinger, K, Smerdon, S.J, Gamblin, S.J, Eccleston, J.F. | | 登録日 | 2003-03-28 | | 公開日 | 2003-05-06 | | 最終更新日 | 2023-08-16 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | MgF(3)(-) as a Transition State Analog of Phosphoryl Transfer
Chem.Biol., 9, 2002
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1GRN
 | | CRYSTAL STRUCTURE OF THE CDC42/CDC42GAP/ALF3 COMPLEX. | | 分子名称: | ALUMINUM FLUORIDE, GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, ... | | 著者 | Nassar, N, Hoffman, G.R, Clardy, J.C, Cerione, R.A. | | 登録日 | 1998-07-30 | | 公開日 | 1999-12-22 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Structures of Cdc42 bound to the active and catalytically compromised forms of Cdc42GAP.
Nat.Struct.Biol., 5, 1998
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5C2K
 | | Crystal structure of the fusion protein linked by RhoA and the GAP domain of MgcRacGAP | | 分子名称: | ALUMINUM FLUORIDE, GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, ... | | 著者 | Murayama, K, Kato-Murayama, M, Hosaka, T, Kitamura, T, Yokoyama, S, Shirouzu, M. | | 登録日 | 2015-06-16 | | 公開日 | 2016-06-22 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (1.42 Å) | | 主引用文献 | Structural basis of G-protein target alternation of MgcRacGAP by phospholylation
To Be Published
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3CXL
 | | Crystal structure of human chimerin 1 (CHN1) | | 分子名称: | N-chimerin, UNKNOWN ATOM OR ION, ZINC ION | | 著者 | Shen, L, Buck, M, Tong, Y, Tempel, W, MacKenzie, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Wilkstrom, M, Bochkarev, A, Park, H, Structural Genomics Consortium (SGC) | | 登録日 | 2008-04-24 | | 公開日 | 2008-08-05 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Crystal structure of human chimerin 1 (CHN1).
To be Published
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5C2J
 | | Complex structure of the GAP domain of MgcRacGAP and Cdc42 | | 分子名称: | ALUMINUM FLUORIDE, Cell division control protein 42 homolog, GUANOSINE-5'-DIPHOSPHATE, ... | | 著者 | Murayama, K, Kato-Murayama, M, Hosaka, T, Kitamura, T, Yokoyama, S, Shirouzu, M. | | 登録日 | 2015-06-16 | | 公開日 | 2016-06-22 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Structural basis of G-protein target alternation of MgcRacGAP by phospholylation
To Be Published
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5M70
 | | Crystal Structure of human RhoGAP mutated in its arginin finger (R85A) in complex with RhoA.GDP.AlF4- human | | 分子名称: | GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, Rho GTPase-activating protein 1, ... | | 著者 | Pellegrini, E, Bowler, M.W. | | 登録日 | 2016-10-26 | | 公開日 | 2017-05-17 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Assessing the Influence of Mutation on GTPase Transition States by Using X-ray Crystallography, (19) F NMR, and DFT Approaches.
Angew. Chem. Int. Ed. Engl., 56, 2017
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5M6U
 | | HUMAN PI3KDELTA IN COMPLEX WITH LASW1579 | | 分子名称: | 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 | | 著者 | Segarra, V, Hernandez, B, Lozoya, E, Blaesse, M, Hoeppner, S, Jestel, A. | | 登録日 | 2016-10-26 | | 公開日 | 2017-02-01 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.85 Å) | | 主引用文献 | 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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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 | | 最終更新日 | 2024-06-12 | | 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 | | 最終更新日 | 2024-06-12 | | 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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