7PE8
 
 | |
3SD5
 | | Crystal Structure of PI3K gamma with 5-(2,4-dimorpholinopyrimidin-6-yl)-4-(trifluoromethyl)pyridin-2-amine | | 分子名称: | 5-[2,6-di(morpholin-4-yl)pyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | | 著者 | Knapp, M.S, Elling, R.A. | | 登録日 | 2011-06-08 | | 公開日 | 2012-01-04 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Identification and Characterization of NVP-BKM120, an Orally Available Pan-Class I PI3-Kinase Inhibitor.
Mol.Cancer Ther., 11, 2012
|
|
5EUQ
 | |
6ZWM
 | | cryo-EM structure of human mTOR complex 2, overall refinement | | 分子名称: | ACETYL GROUP, INOSITOL HEXAKISPHOSPHATE, PHOSPHOTHIOPHOSPHORIC ACID-ADENYLATE ESTER, ... | | 著者 | Scaiola, A, Mangia, F, Imseng, S, Boehringer, D, Ban, N, Maier, T. | | 登録日 | 2020-07-28 | | 公開日 | 2020-11-18 | | 実験手法 | ELECTRON MICROSCOPY (3.2 Å) | | 主引用文献 | The 3.2- angstrom resolution structure of human mTORC2.
Sci Adv, 6, 2020
|
|
6Z2X
 | |
3CST
 | |
5C4G
 | |
4JSN
 | | structure of mTORdeltaN-mLST8 complex | | 分子名称: | Serine/threonine-protein kinase mTOR, Target of rapamycin complex subunit LST8 | | 著者 | Pavletich, N.P. | | 登録日 | 2013-03-22 | | 公開日 | 2013-05-08 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | mTOR kinase structure, mechanism and regulation.
Nature, 497, 2013
|
|
4HND
 | | Crystal structure of the catalytic domain of Selenomethionine substituted human PI4KIIalpha in complex with ADP | | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, Phosphatidylinositol 4-kinase type 2-alpha | | 著者 | Zhou, Q, Zhai, Y, Zhang, K, Chen, C, Sun, F. | | 登録日 | 2012-10-19 | | 公開日 | 2014-04-09 | | 最終更新日 | 2016-12-28 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Molecular insights into the membrane-associated phosphatidylinositol 4-kinase II alpha.
Nat Commun, 5, 2014
|
|
3P2B
 | | Crystal Structure of PI3K gamma with 3-(2-morpholino-6-(pyridin-3-ylamino)pyrimidin-4-yl)phenol | | 分子名称: | 3-[2-morpholin-4-yl-6-(pyridin-3-ylamino)pyrimidin-4-yl]phenol, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | | 著者 | Knapp, M.S, Elling, R.A, Ornelas, E. | | 登録日 | 2010-10-01 | | 公開日 | 2011-08-17 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Identification and structure-activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors.
Bioorg.Med.Chem.Lett., 20, 2010
|
|
7K11
 | |
6BCX
 | | mTORC1 structure refined to 3.0 angstroms | | 分子名称: | ADENOSINE-5'-TRIPHOSPHATE, Eukaryotic translation initiation factor 4E-binding protein 1, MAGNESIUM ION, ... | | 著者 | Pavletich, N.P, Yang, H. | | 登録日 | 2017-10-20 | | 公開日 | 2017-12-20 | | 最終更新日 | 2024-03-13 | | 実験手法 | ELECTRON MICROSCOPY (3.23 Å) | | 主引用文献 | Mechanisms of mTORC1 activation by RHEB and inhibition by PRAS40.
Nature, 552, 2017
|
|
6ZFP
 | | Cryo-EM structure of DNA-PKcs (State 2) | | 分子名称: | DNA-dependent protein kinase catalytic subunit,DNA-PKcs,DNA-PKcs | | 著者 | Chaplin, A.K, Hardwick, S.W, Chirgadze, D.Y, Blundell, T.L. | | 登録日 | 2020-06-17 | | 公開日 | 2020-10-21 | | 最終更新日 | 2024-05-01 | | 実験手法 | ELECTRON MICROSCOPY (3.24 Å) | | 主引用文献 | Dimers of DNA-PK create a stage for DNA double-strand break repair.
Nat.Struct.Mol.Biol., 28, 2021
|
|
7OTV
 | | DNA-PKcs in complex with wortmannin | | 分子名称: | (1S,6BR,9AS,11R,11BR)-9A,11B-DIMETHYL-1-[(METHYLOXY)METHYL]-3,6,9-TRIOXO-1,6,6B,7,8,9,9A,10,11,11B-DECAHYDRO-3H-FURO[4, 3,2-DE]INDENO[4,5-H][2]BENZOPYRAN-11-YL ACETATE, DNA-dependent protein kinase catalytic subunit,DNA-dependent protein kinase catalytic subunit,DNA-PKcs | | 著者 | Liang, S, Thomas, S.E, Blundell, T.L. | | 登録日 | 2021-06-10 | | 公開日 | 2022-01-12 | | 最終更新日 | 2024-07-17 | | 実験手法 | ELECTRON MICROSCOPY (3.24 Å) | | 主引用文献 | Structural insights into inhibitor regulation of the DNA repair protein DNA-PKcs.
Nature, 601, 2022
|
|
7BI2
 | | PI3KC2aDeltaN and DeltaC-C2 | | 分子名称: | 1,2-ETHANEDIOL, 9-(6-aminopyridin-3-yl)-1-[3-(trifluoromethyl)phenyl]benzo[h][1,6]naphthyridin-2(1H)-one, IODIDE ION, ... | | 著者 | Lo, W.T, Roske, Y, Daumke, O, Haucke, V. | | 登録日 | 2021-01-12 | | 公開日 | 2022-03-09 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (3.25 Å) | | 主引用文献 | Structural basis of phosphatidylinositol 3-kinase C2 alpha function.
Nat.Struct.Mol.Biol., 29, 2022
|
|
4KZC
 | | Structure of PI3K gamma with Imidazopyridine inhibitors | | 分子名称: | N-{6-[6-amino-5-(trifluoromethyl)pyridin-3-yl]imidazo[1,2-a]pyridin-2-yl}acetamide, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION | | 著者 | Knapp, M.S, Elling, E.A. | | 登録日 | 2013-05-29 | | 公開日 | 2013-07-17 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (3.25 Å) | | 主引用文献 | Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K.
Bioorg.Med.Chem.Lett., 23, 2013
|
|
7PW4
 | | Human SMG1-8-9 kinase complex bound to a SMG1 inhibitor | | 分子名称: | 1-[4-[4-[2-[[4-chloranyl-3-(diethylsulfamoyl)phenyl]amino]pyrimidin-4-yl]pyridin-2-yl]phenyl]-3-methyl-urea, ADENOSINE-5'-TRIPHOSPHATE, INOSITOL HEXAKISPHOSPHATE, ... | | 著者 | Langer, L.M, Conti, E. | | 登録日 | 2021-10-06 | | 公開日 | 2021-12-01 | | 実験手法 | ELECTRON MICROSCOPY (3.27 Å) | | 主引用文献 | Cryo-EM reconstructions of inhibitor-bound SMG1 kinase reveal an autoinhibitory state dependent on SMG8.
Elife, 10, 2021
|
|
7TZO
 | | The apo structure of human mTORC2 complex | | 分子名称: | Rapamycin-insensitive companion of mTOR, Serine/threonine-protein kinase mTOR, Target of rapamycin complex 2 subunit MAPKAP1, ... | | 著者 | Yu, Z, Chen, J, Pearce, D. | | 登録日 | 2022-02-16 | | 公開日 | 2023-01-11 | | 最終更新日 | 2024-06-12 | | 実験手法 | ELECTRON MICROSCOPY (3.28 Å) | | 主引用文献 | 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
|
|
5FBR
 | | PI4KB in complex with Rab11 and the MI359 Inhibitor | | 分子名称: | 5'-GUANOSINE-DIPHOSPHATE-MONOTHIOPHOSPHATE, Phosphatidylinositol 4-kinase beta,Phosphatidylinositol 4-kinase beta, Ras-related protein Rab-11A, ... | | 著者 | Chalupska, D, Mejdrova, I, Nencka, R, Boura, E. | | 登録日 | 2015-12-14 | | 公開日 | 2016-12-28 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (3.28 Å) | | 主引用文献 | PI4KB in complex with Rab11 and the MI359 Inhibitor
To Be Published
|
|
5FBV
 | | PI4KB in complex with Rab11 and the MI364 Inhibitor | | 分子名称: | 5'-GUANOSINE-DIPHOSPHATE-MONOTHIOPHOSPHATE, Phosphatidylinositol 4-kinase beta,Phosphatidylinositol 4-kinase beta, Ras-related protein Rab-11A, ... | | 著者 | Chalupska, D, Mejdrova, I, Nencka, R, Boura, E. | | 登録日 | 2015-12-14 | | 公開日 | 2016-12-28 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (3.285 Å) | | 主引用文献 | PI4KB in complex with Rab11 and the MI364 Inhibitor
To Be Published
|
|
7SU3
 | | CryoEM structure of DNA-PK complex VII | | 分子名称: | ADENOSINE-5'-TRIPHOSPHATE, DNA (5'-D(*AP*AP*GP*CP*AP*GP*TP*AP*GP*AP*G)-3'), DNA (5'-D(*GP*CP*AP*TP*GP*CP*TP*CP*TP*AP*CP*TP*GP*CP*TP*TP*CP*GP*AP*TP*AP*TP*CP*G)-3'), ... | | 著者 | Chen, X, Liu, L, Gellert, M, Yang, W. | | 登録日 | 2021-11-16 | | 公開日 | 2022-01-12 | | 最終更新日 | 2024-06-05 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Autophosphorylation transforms DNA-PK from protecting to processing DNA ends.
Mol.Cell, 82, 2022
|
|
4JSP
 | |
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
|
|
5SW8
 | | Crystal structure of PI3Kalpha in complex with fragments 7 and 11 | | 分子名称: | 2-CHLOROBENZENESULFONAMIDE, 2H-indazol-5-amine, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, ... | | 著者 | Gabelli, S.B, Vogelstein, B, Miller, M.S, Amzel, L.M. | | 登録日 | 2016-08-08 | | 公開日 | 2017-02-15 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | | 主引用文献 | Identification of allosteric binding sites for PI3K alpha oncogenic mutant specific inhibitor design.
Bioorg. Med. Chem., 25, 2017
|
|
5SXB
 | | Crystal Structure of PI3Kalpha in complex with fragment 23 | | 分子名称: | ISATOIC ANHYDRIDE, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | 著者 | Gabelli, S.B, Vogelstein, B, Miller, M.S, Amzel, L.M. | | 登録日 | 2016-08-09 | | 公開日 | 2017-02-15 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | | 主引用文献 | Identification of allosteric binding sites for PI3K alpha oncogenic mutant specific inhibitor design.
Bioorg. Med. Chem., 25, 2017
|
|
