2NCK
 
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1RBB
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1NLK
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5OQ4
 | | PQR309 - a Potent, Brain-Penetrant, Orally Bioavailable, pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology | | 分子名称: | 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 | | 著者 | Williams, R.L, Zhang, X. | | 登録日 | 2017-08-10 | | 公開日 | 2017-09-06 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | 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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1LMK
 | | THE STRUCTURE OF A BIVALENT DIABODY | | 分子名称: | ANTI-PHOSPHATIDYLINOSITOL SPECIFIC PHOSPHOLIPASE C DIABODY | | 著者 | Williams, R.L. | | 登録日 | 1994-08-29 | | 公開日 | 1995-03-31 | | 最終更新日 | 2024-06-05 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Crystal structure of a diabody, a bivalent antibody fragment.
Structure, 2, 1994
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1NQB
 | | TRIVALENT ANTIBODY FRAGMENT | | 分子名称: | SINGLE-CHAIN ANTIBODY FRAGMENT | | 著者 | Williams, R.L, Pei, X.Y. | | 登録日 | 1997-04-04 | | 公開日 | 1997-08-20 | | 最終更新日 | 2023-08-09 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | 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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2G3P
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5FVM
 | | Cryo electron microscopy of a complex of Tor and Lst8 | | 分子名称: | SERINE/THREONINE-PROTEIN KINASE TOR2, TARGET OF RAPAMYCIN COMPLEX SUBUNIT LST8 | | 著者 | Baretic, D, Berndt, A, Ohashi, Y, Johnson, C.M, Williams, R.L. | | 登録日 | 2016-02-09 | | 公開日 | 2016-04-20 | | 最終更新日 | 2024-05-08 | | 実験手法 | ELECTRON MICROSCOPY (6.7 Å) | | 主引用文献 | Tor Forms a Dimer Through an N-Terminal Helical Solenoid with a Complex Topology
Nat.Commun., 7, 2016
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7OWG
 | | human DEPTOR in a complex with mutant human mTORC1 A1459P | | 分子名称: | DEP domain-containing mTOR-interacting protein, Regulatory-associated protein of mTOR, Serine/threonine-protein kinase mTOR, ... | | 著者 | 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. | | 登録日 | 2021-06-18 | | 公開日 | 2021-09-08 | | 最終更新日 | 2022-02-23 | | 実験手法 | ELECTRON MICROSCOPY (4.7 Å) | | 主引用文献 | Bipartite binding and partial inhibition links DEPTOR and mTOR in a mutually antagonistic embrace.
Elife, 10, 2021
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7PG5
 | | Crystal Structure of PI3Kalpha | | 分子名称: | GLYCEROL, PHOSPHATE ION, Phosphatidylinositol 3-kinase regulatory subunit alpha, ... | | 著者 | Gong, G, Pinotsis, N, Williams, R.L, Vanhaesebroeck, B. | | 登録日 | 2021-08-13 | | 公開日 | 2022-08-24 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (2.20029068 Å) | | 主引用文献 | A small-molecule PI3K alpha activator for cardioprotection and neuroregeneration.
Nature, 618, 2023
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7PG6
 | | Crystal Structure of PI3Kalpha in complex with the inhibitor NVP-BYL719 | | 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 | Gong, G, Pinotsis, N, Williams, R.L, Vanhaesebroeck, B. | | 登録日 | 2021-08-13 | | 公開日 | 2022-08-24 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (2.49943733 Å) | | 主引用文献 | A small-molecule PI3K alpha activator for cardioprotection and neuroregeneration.
Nature, 618, 2023
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5JHA
 | | Structure of Phosphoinositide 3-kinase gamma (PI3K) bound to the potent inhibitor PIKin2 | | 分子名称: | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION, [1-{4-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-6-(morpholin-4-yl)pyrimidin-2-yl}-3-(chloromethyl)azetidin-3-yl]methanol | | 著者 | Burke, J.E, Inglis, A.J, Williams, R.L. | | 登録日 | 2016-04-20 | | 公開日 | 2017-03-15 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.51 Å) | | 主引用文献 | Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention.
Nat Commun, 8, 2017
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8OW2
 | | Crystal structure of the p110alpha catalytic subunit from homo sapiens in complex with activator 1938 | | 分子名称: | 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 | | 著者 | Gong, G.Q, Bellini, D, Vanhaesebroeck, B, Williams, R.L. | | 登録日 | 2023-04-26 | | 公開日 | 2023-05-24 | | 最終更新日 | 2023-06-07 | | 実験手法 | X-RAY DIFFRACTION (2.57 Å) | | 主引用文献 | A small-molecule PI3K alpha activator for cardioprotection and neuroregeneration.
Nature, 618, 2023
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8OXP
 | | ATM(Q2971A) in complex with Mg AMP-PNP | | 分子名称: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, Serine-protein kinase ATM, ... | | 著者 | Howes, A.C, Perisic, O, Williams, R.L. | | 登録日 | 2023-05-02 | | 公開日 | 2023-09-27 | | 最終更新日 | 2023-10-11 | | 実験手法 | ELECTRON MICROSCOPY (2.6 Å) | | 主引用文献 | 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 | | 分子名称: | Cellular tumor antigen p53, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | 著者 | Howes, A.C, Perisic, O, Williams, R.L. | | 登録日 | 2023-05-02 | | 公開日 | 2023-09-27 | | 最終更新日 | 2023-10-11 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | 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 | | 分子名称: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, Serine-protein kinase ATM, ... | | 著者 | Howes, A.C, Perisic, O, Williams, R.L. | | 登録日 | 2023-05-02 | | 公開日 | 2023-09-27 | | 最終更新日 | 2023-10-11 | | 実験手法 | ELECTRON MICROSCOPY (2.5 Å) | | 主引用文献 | Structural insights into the activation of ataxia-telangiectasia mutated by oxidative stress.
Sci Adv, 9, 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 | | 分子名称: | Cellular tumor antigen p53, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | | 著者 | Howes, A.C, Perisic, O, Williams, R.L. | | 登録日 | 2023-05-02 | | 公開日 | 2023-09-27 | | 最終更新日 | 2023-10-11 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | Structural insights into the activation of ataxia-telangiectasia mutated by oxidative stress.
Sci Adv, 9, 2023
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5KC2
 | | Negative stain structure of Vps15/Vps34 complex | | 分子名称: | Phosphatidylinositol 3-kinase VPS34, Serine/threonine-protein kinase VPS15 | | 著者 | Kirsten, M.L, Zhang, L, Ohashi, Y, Perisic, O, Williams, R.L, Sachse, C. | | 登録日 | 2016-06-04 | | 公開日 | 2016-10-05 | | 最終更新日 | 2024-05-15 | | 実験手法 | ELECTRON MICROSCOPY (28 Å) | | 主引用文献 | Characterization of Atg38 and NRBF2, a fifth subunit of the autophagic Vps34/PIK3C3 complex.
Autophagy, 12, 2016
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8AJ8
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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 | | 分子名称: | N-(5-(4-CHLORO-3-(2-HYDROXY-ETHYLSULFAMOYL)- PHENYLTHIAZOLE-2-YL)-ACETAMIDE, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT GAMMA ISOFORM | | 著者 | 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. | | 登録日 | 2006-03-16 | | 公開日 | 2006-05-22 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | A Pharmacological Map of the Pi3-K Family Defines a Role for P110Alpha in Signaling
Cell(Cambridge,Mass.), 125, 2006
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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 | | 分子名称: | N-(2,3-DIHYDRO-7,8-DIMETHOXYIMIDAZO[1,2-C] QUINAZOLIN-5-YL)NICOTINAMIDE, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT GAMMA ISOFORM | | 著者 | 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. | | 登録日 | 2006-03-16 | | 公開日 | 2006-05-22 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | 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 | | 分子名称: | 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 | | 著者 | 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. | | 登録日 | 2006-03-16 | | 公開日 | 2006-05-22 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | A Pharmacological Map of the Pi3-K Family Defines a Role for P110Alpha in Signaling
Cell(Cambridge,Mass.), 125, 2006
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8BFU
 | | Crystal structure of the apo p110alpha catalytic subunit from homo sapiens | | 分子名称: | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | 著者 | Gong, G.Q, Bellini, D, Vanhaesebroeck, B, Williams, R.L. | | 登録日 | 2022-10-26 | | 公開日 | 2023-02-15 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (2.41 Å) | | 主引用文献 | A small-molecule PI3K alpha activator for cardioprotection and neuroregeneration.
Nature, 618, 2023
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5JHB
 | | Structure of Phosphoinositide 3-kinase gamma (PI3K) bound to the potent inhibitor PIKin3 | | 分子名称: | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION, [1-{4-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl}-3-(chloromethyl)azetidin-3-yl]methanol | | 著者 | Burke, J.E, Inglis, A.J, Williams, R.L. | | 登録日 | 2016-04-20 | | 公開日 | 2017-03-15 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.48 Å) | | 主引用文献 | Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention.
Nat Commun, 8, 2017
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