2NCK
 
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1RBB
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1NLK
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1LMK
 | | THE STRUCTURE OF A BIVALENT DIABODY | | Descriptor: | ANTI-PHOSPHATIDYLINOSITOL SPECIFIC PHOSPHOLIPASE C DIABODY | | Authors: | Williams, R.L. | | Deposit date: | 1994-08-29 | | Release date: | 1995-03-31 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Crystal structure of a diabody, a bivalent antibody fragment.
Structure, 2, 1994
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1NQB
 | | TRIVALENT ANTIBODY FRAGMENT | | Descriptor: | SINGLE-CHAIN ANTIBODY FRAGMENT | | Authors: | Williams, R.L, Pei, X.Y. | | Deposit date: | 1997-04-04 | | Release date: | 1997-08-20 | | Last modified: | 2023-08-09 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | The 2.0-A resolution crystal structure of a trimeric antibody fragment with noncognate VH-VL domain pairs shows a rearrangement of VH CDR3.
Proc.Natl.Acad.Sci.USA, 94, 1997
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1NSK
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5OQ4
 | | PQR309 - a Potent, Brain-Penetrant, Orally Bioavailable, pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology | | Descriptor: | 5-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION | | Authors: | Williams, R.L, Zhang, X. | | Deposit date: | 2017-08-10 | | Release date: | 2017-09-06 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.
J. Med. Chem., 60, 2017
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7BL1
 | | human complex II-BATS bound to membrane-attached Rab5a-GTP | | Descriptor: | Beclin-1, GUANOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, ... | | Authors: | Tremel, S, Morado, D.R, Kovtun, O, Williams, R.L, Briggs, J.A.G, Munro, S, Ohashi, Y, Bertram, J, Perisic, O. | | Deposit date: | 2021-01-17 | | Release date: | 2021-03-03 | | Last modified: | 2021-03-24 | | Method: | ELECTRON MICROSCOPY (9.8 Å) | | Cite: | Structural basis for VPS34 kinase activation by Rab1 and Rab5 on membranes.
Nat Commun, 12, 2021
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8AJ8
 | | Structure of p110 gamma bound to the p84 regulatory subunit | | Descriptor: | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, Phosphoinositide 3-kinase regulatory subunit 6 | | Authors: | Burke, J.E, Williams, R.L, Zhang, X. | | Deposit date: | 2022-07-27 | | Release date: | 2023-03-22 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (8.5 Å) | | Cite: | Molecular basis for differential activation of p101 and p84 complexes of PI3K gamma by Ras and GPCRs.
Cell Rep, 42, 2023
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2CHX
 | | A pharmacological map of the PI3-K family defines a role for p110alpha in signaling: The structure of complex of phosphoinositide 3-kinase gamma with inhibitor PIK-90 | | Descriptor: | N-(2,3-DIHYDRO-7,8-DIMETHOXYIMIDAZO[1,2-C] QUINAZOLIN-5-YL)NICOTINAMIDE, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT GAMMA ISOFORM | | Authors: | Knight, Z.A, Gonzalez, B, Feldman, M.E, Zunder, E.R, Goldenberg, D.D, Williams, O, Loewith, R, Stokoe, D, Balla, A, Toth, B, Balla, T, Weiss, W.A, Williams, R.L, Shokat, K.M. | | Deposit date: | 2006-03-16 | | Release date: | 2006-05-22 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | A Pharmacological Map of the Pi3-K Family Defines a Role for P110Alpha in Signaling
Cell(Cambridge,Mass.), 125, 2006
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2CHW
 | | A pharmacological map of the PI3-K family defines a role for p110 alpha in signaling: The structure of complex of phosphoinositide 3- kinase gamma with inhibitor PIK-39 | | Descriptor: | 2-((9H-PURIN-6-YLTHIO)METHYL)-5-CHLORO-3-(2-METHOXYPHENYL)QUINAZOLIN-4(3H)-ONE, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT GAMMA ISOFORM | | Authors: | Knight, Z.A, Gonzalez, B, Feldman, M.E, Zunder, E.R, Goldenberg, D.D, Williams, O, Loewith, R, Stokoe, D, Balla, A, Toth, B, Balla, T, Weiss, W.A, Williams, R.L, Shokat, K.M. | | Deposit date: | 2006-03-16 | | Release date: | 2006-05-22 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | A Pharmacological Map of the Pi3-K Family Defines a Role for P110Alpha in Signaling
Cell(Cambridge,Mass.), 125, 2006
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2CHZ
 | | A pharmacological map of the PI3-K family defines a role for p110alpha in signaling: The structure of complex of phosphoinositide 3-kinase gamma with inhibitor PIK-93 | | Descriptor: | N-(5-(4-CHLORO-3-(2-HYDROXY-ETHYLSULFAMOYL)- PHENYLTHIAZOLE-2-YL)-ACETAMIDE, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT GAMMA ISOFORM | | Authors: | Knight, Z.A, Gonzalez, B, Feldman, M.E, Zunder, E.R, Goldenberg, D.D, Williams, O, Loewith, R, Stokoe, D, Balla, A, Toth, B, Balla, T, Weiss, W.A, Williams, R.L, Shokat, K.M. | | Deposit date: | 2006-03-16 | | Release date: | 2006-05-22 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | A Pharmacological Map of the Pi3-K Family Defines a Role for P110Alpha in Signaling
Cell(Cambridge,Mass.), 125, 2006
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6S6D
 | | Crystal structure of RagA-Q66L-GTP/RagC-S75N-GDP GTPase heterodimer complex | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, ... | | Authors: | Anandapadamanaban, M, Masson, G.R, Perisic, O, Kaufman, J, Williams, R.L. | | Deposit date: | 2019-07-02 | | Release date: | 2019-10-16 | | Last modified: | 2019-10-23 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Architecture of human Rag GTPase heterodimers and their complex with mTORC1.
Science, 366, 2019
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6S6A
 | | Crystal structure of RagA-Q66L/RagC-T90N GTPase heterodimer complex | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, ... | | Authors: | Anandapadamanaban, M, Masson, G.R, Perisic, O, Kaufman, J, Williams, R.L. | | Deposit date: | 2019-07-02 | | Release date: | 2019-10-16 | | Last modified: | 2019-10-23 | | Method: | X-RAY DIFFRACTION (2.63 Å) | | Cite: | Architecture of human Rag GTPase heterodimers and their complex with mTORC1.
Science, 366, 2019
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6SB2
 | | cryo-EM structure of mTORC1 bound to active RagA/C GTPases | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, Ras-related GTP-binding protein A, ... | | Authors: | Anandapadamanaban, M, Berndt, A, Masson, G.R, Perisic, O, Williams, R.L. | | Deposit date: | 2019-07-18 | | Release date: | 2019-10-16 | | Last modified: | 2019-10-23 | | Method: | ELECTRON MICROSCOPY (6.2 Å) | | Cite: | Architecture of human Rag GTPase heterodimers and their complex with mTORC1.
Science, 366, 2019
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6SB0
 | | cryo-EM structure of mTORC1 bound to PRAS40-fused active RagA/C GTPases | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, Proline-rich AKT1 substrate 1, ... | | Authors: | Anandapadamanaban, M, Berndt, A, Masson, G.R, Perisic, O, Williams, R.L. | | Deposit date: | 2019-07-18 | | Release date: | 2019-10-16 | | Last modified: | 2019-10-23 | | Method: | ELECTRON MICROSCOPY (5.5 Å) | | Cite: | Architecture of human Rag GTPase heterodimers and their complex with mTORC1.
Science, 366, 2019
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8OW2
 | | Crystal structure of the p110alpha catalytic subunit from homo sapiens in complex with activator 1938 | | Descriptor: | 1-[7-[[2-[[4-(4-ethylpiperazin-1-yl)phenyl]amino]pyridin-4-yl]amino]-2,3-dihydroindol-1-yl]ethanone, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | Authors: | Gong, G.Q, Bellini, D, Vanhaesebroeck, B, Williams, R.L. | | Deposit date: | 2023-04-26 | | Release date: | 2023-05-24 | | Last modified: | 2023-06-07 | | Method: | X-RAY DIFFRACTION (2.57 Å) | | Cite: | A small-molecule PI3K alpha activator for cardioprotection and neuroregeneration.
Nature, 618, 2023
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8OXO
 | | ATM(Q2971A) dimeric C-terminal region activated by oxidative stress in complex with Mg AMP-PNP and p53 peptide | | Descriptor: | Cellular tumor antigen p53, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | Authors: | Howes, A.C, Perisic, O, Williams, R.L. | | Deposit date: | 2023-05-02 | | Release date: | 2023-09-27 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Structural insights into the activation of ataxia-telangiectasia mutated by oxidative stress.
Sci Adv, 9, 2023
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8OXP
 | | ATM(Q2971A) in complex with Mg AMP-PNP | | Descriptor: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, Serine-protein kinase ATM, ... | | Authors: | Howes, A.C, Perisic, O, Williams, R.L. | | Deposit date: | 2023-05-02 | | Release date: | 2023-09-27 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (2.6 Å) | | Cite: | Structural insights into the activation of ataxia-telangiectasia mutated by oxidative stress.
Sci Adv, 9, 2023
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8OXQ
 | | ATM(Q2971A) dimeric C-terminal region in complex with Mg AMP-PNP | | Descriptor: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, Serine-protein kinase ATM, ... | | Authors: | Howes, A.C, Perisic, O, Williams, R.L. | | Deposit date: | 2023-05-02 | | Release date: | 2023-09-27 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (2.5 Å) | | Cite: | Structural insights into the activation of ataxia-telangiectasia mutated by oxidative stress.
Sci Adv, 9, 2023
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8OXM
 | | ATM(Q2971A) activated by oxidative stress in complex with Mg AMP-PNP and p53 peptide | | Descriptor: | Cellular tumor antigen p53, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | Authors: | Howes, A.C, Perisic, O, Williams, R.L. | | Deposit date: | 2023-05-02 | | Release date: | 2023-09-27 | | Last modified: | 2023-10-11 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | Structural insights into the activation of ataxia-telangiectasia mutated by oxidative stress.
Sci Adv, 9, 2023
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7PG6
 | | Crystal Structure of PI3Kalpha in complex with the inhibitor NVP-BYL719 | | 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: | Gong, G, Pinotsis, N, Williams, R.L, Vanhaesebroeck, B. | | Deposit date: | 2021-08-13 | | Release date: | 2022-08-24 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.49943733 Å) | | Cite: | A small-molecule PI3K alpha activator for cardioprotection and neuroregeneration.
Nature, 618, 2023
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7PG5
 | | Crystal Structure of PI3Kalpha | | Descriptor: | GLYCEROL, PHOSPHATE ION, Phosphatidylinositol 3-kinase regulatory subunit alpha, ... | | Authors: | Gong, G, Pinotsis, N, Williams, R.L, Vanhaesebroeck, B. | | Deposit date: | 2021-08-13 | | Release date: | 2022-08-24 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.20029068 Å) | | Cite: | A small-molecule PI3K alpha activator for cardioprotection and neuroregeneration.
Nature, 618, 2023
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7OWG
 | | human DEPTOR in a complex with mutant human mTORC1 A1459P | | Descriptor: | DEP domain-containing mTOR-interacting protein, Regulatory-associated protein of mTOR, Serine/threonine-protein kinase mTOR, ... | | Authors: | Heimhalt, M, Berndt, A, Wagstaff, J, Anandapadamanaban, M, Perisic, O, Maslen, S, McLaughlin, S, Yu, W.-H, Masson, G.R, Boland, A, Ni, X, Yamashita, K, Murshudov, G.N, Skehel, M, Freund, S.M, Williams, R.L. | | Deposit date: | 2021-06-18 | | Release date: | 2021-09-08 | | Last modified: | 2022-02-23 | | Method: | ELECTRON MICROSCOPY (4.7 Å) | | Cite: | Bipartite binding and partial inhibition links DEPTOR and mTOR in a mutually antagonistic embrace.
Elife, 10, 2021
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5NP0
 | | Closed dimer of human ATM (Ataxia telangiectasia mutated) | | Descriptor: | Serine-protein kinase ATM | | Authors: | Baretic, D, Pollard, H.K, Fisher, D.I, Johnson, C.M, Santhanam, B, Truman, C.M, Kouba, T, Fersht, A.R, Phillips, C, Williams, R.L. | | Deposit date: | 2017-04-13 | | Release date: | 2017-05-17 | | Last modified: | 2019-12-11 | | Method: | ELECTRON MICROSCOPY (5.7 Å) | | Cite: | Structures of closed and open conformations of dimeric human ATM.
Sci Adv, 3, 2017
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