2NPU
 
 | | The solution structure of the rapamycin-binding domain of mTOR (FRB) | | 分子名称: | FKBP12-rapamycin complex-associated protein | | 著者 | Veverka, V, Crabbe, T, Bird, I, Lennie, G, Muskett, F.W, Taylor, R.J, Carr, M.D. | | 登録日 | 2006-10-30 | | 公開日 | 2007-09-18 | | 最終更新日 | 2024-05-15 | | 実験手法 | SOLUTION NMR | | 主引用文献 | Structural characterization of the interaction of mTOR with phosphatidic acid and a novel class of inhibitor: compelling evidence for a central role of the FRB domain in small molecule-mediated regulation of mTOR.
Oncogene, 27, 2008
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7PED
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6U62
 | | Raptor-Rag-Ragulator complex | | 分子名称: | GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, ... | | 著者 | Rogala, K.B, Sabatini, D.M. | | 登録日 | 2019-08-29 | | 公開日 | 2019-10-30 | | 最終更新日 | 2024-03-20 | | 実験手法 | ELECTRON MICROSCOPY (3.18 Å) | | 主引用文献 | Structural basis for the docking of mTORC1 on the lysosomal surface.
Science, 366, 2019
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5YK3
 | | human Ragulator complex | | 分子名称: | Ragulator complex protein LAMTOR1, Ragulator complex protein LAMTOR2, Ragulator complex protein LAMTOR3, ... | | 著者 | Wu, G, Mu, Z. | | 登録日 | 2017-10-12 | | 公開日 | 2019-01-23 | | 最終更新日 | 2024-03-27 | | 実験手法 | X-RAY DIFFRACTION (3.01 Å) | | 主引用文献 | Structural insight into the Ragulator complex which anchors mTORC1 to the lysosomal membrane
Cell Discov, 3, 2017
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5GPG
 | | Co-crystal structure of the FK506 binding domain of human FKBP25, Rapamycin and the FRB domain of human mTOR | | 分子名称: | Peptidyl-prolyl cis-trans isomerase FKBP3, RAPAMYCIN IMMUNOSUPPRESSANT DRUG, Serine/threonine-protein kinase mTOR | | 著者 | Lee, H.B, Lee, S.Y, Rhee, H.W, Lee, C.W. | | 登録日 | 2016-08-02 | | 公開日 | 2016-10-12 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (1.67 Å) | | 主引用文献 | Proximity-Directed Labeling Reveals a New Rapamycin-Induced Heterodimer of FKBP25 and FRB in Live Cells
Acs Cent.Sci., 2, 2016
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4DRI
 | | Co-crystal structure of the PPIase domain of FKBP51, Rapamycin and the FRB fragment of mTOR | | 分子名称: | Peptidyl-prolyl cis-trans isomerase FKBP5, RAPAMYCIN IMMUNOSUPPRESSANT DRUG, Serine/threonine-protein kinase mTOR | | 著者 | Maerz, A.M, Bracher, A, Hausch, F. | | 登録日 | 2012-02-17 | | 公開日 | 2013-02-06 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.45 Å) | | 主引用文献 | Large FK506-Binding Proteins Shape the Pharmacology of Rapamycin.
Mol.Cell.Biol., 33, 2013
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4DRJ
 | | o-crystal structure of the PPIase domain of FKBP52, Rapamycin and the FRB fragment of mTOR | | 分子名称: | Peptidyl-prolyl cis-trans isomerase FKBP4, RAPAMYCIN IMMUNOSUPPRESSANT DRUG, SULFATE ION, ... | | 著者 | Maerz, A.M, Bracher, A, Hausch, F. | | 登録日 | 2012-02-17 | | 公開日 | 2013-02-06 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Large FK506-Binding Proteins Shape the Pharmacology of Rapamycin.
Mol.Cell.Biol., 33, 2013
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5Y3A
 | | Crystal structure of Ragulator complex (p18 49-161) | | 分子名称: | Ragulator complex protein LAMTOR1, Ragulator complex protein LAMTOR2, Ragulator complex protein LAMTOR3, ... | | 著者 | Zhang, T, Ding, J. | | 登録日 | 2017-07-28 | | 公開日 | 2017-12-27 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Structural basis for Ragulator functioning as a scaffold in membrane-anchoring of Rag GTPases and mTORC1.
Nat Commun, 8, 2017
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5Y39
 | | Crystal structure of Ragulator complex (p18 76-145) | | 分子名称: | Ragulator complex protein LAMTOR1, Ragulator complex protein LAMTOR2, Ragulator complex protein LAMTOR3, ... | | 著者 | Zhang, T, Ding, J. | | 登録日 | 2017-07-28 | | 公開日 | 2017-12-06 | | 最終更新日 | 2024-03-27 | | 実験手法 | X-RAY DIFFRACTION (2.65 Å) | | 主引用文献 | Structural basis for Ragulator functioning as a scaffold in membrane-anchoring of Rag GTPases and mTORC1
Nat Commun, 8, 2017
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3TL5
 | | Discovery of GDC-0980: a Potent, Selective, and Orally Available Class I Phosphatidylinositol 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor for the Treatment of Cancer | | 分子名称: | (2S)-1-(4-{[2-(2-aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl}piperazin-1-yl)-2-hydroxypropan-1-one, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | | 著者 | Murray, J.M, Wiesmann, C. | | 登録日 | 2011-08-29 | | 公開日 | 2011-11-02 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (2.788 Å) | | 主引用文献 | Discovery of a Potent, Selective, and Orally Available Class I Phosphatidylinositol 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor (GDC-0980) for the Treatment of Cancer.
J.Med.Chem., 54, 2011
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8DHB
 | | Active FLCN GAP complex | | 分子名称: | BERYLLIUM TRIFLUORIDE ION, Folliculin, Folliculin-interacting protein 2, ... | | 著者 | Jansen, R.M, Hurley, J.H. | | 登録日 | 2022-06-25 | | 公開日 | 2022-09-28 | | 最終更新日 | 2024-10-09 | | 実験手法 | ELECTRON MICROSCOPY (3.53 Å) | | 主引用文献 | Structural basis for FLCN RagC GAP activation in MiT-TFE substrate-selective mTORC1 regulation.
Sci Adv, 8, 2022
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7UX2
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3L16
 | | Discovery of (thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer | | 分子名称: | 5-(6-{[4-(methylsulfonyl)piperazin-1-yl]methyl}-4-morpholin-4-ylthieno[3,2-d]pyrimidin-2-yl)pyridin-2-amine, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | | 著者 | Murray, J.M, Wiesmann, C. | | 登録日 | 2009-12-10 | | 公開日 | 2010-02-16 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Discovery of (Thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer.
J.Med.Chem., 53, 2010
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3L13
 | | Crystal Structures of Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors | | 分子名称: | Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, [3-(6-{[4-(methylsulfonyl)piperazin-1-yl]methyl}-4-morpholin-4-ylthieno[3,2-d]pyrimidin-2-yl)phenyl]methanol | | 著者 | Murray, J.M, Wiesmann, C. | | 登録日 | 2009-12-10 | | 公開日 | 2010-02-16 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Discovery of (Thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer.
J.Med.Chem., 53, 2010
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3L17
 | | Discovery of (thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer | | 分子名称: | 4-methyl-5-(6-{[4-(methylsulfonyl)piperazin-1-yl]methyl}-4-morpholin-4-ylthieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | | 著者 | Murray, J.M, Wiesmann, C. | | 登録日 | 2009-12-10 | | 公開日 | 2010-02-16 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Discovery of (Thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer.
J.Med.Chem., 53, 2010
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6B9X
 | | Crystal structure of Ragulator | | 分子名称: | Hepatitis B virus x interacting protein, Ragulator complex protein LAMTOR1, Ragulator complex protein LAMTOR2, ... | | 著者 | SU, M.-Y, Hurley, J.H. | | 登録日 | 2017-10-11 | | 公開日 | 2017-11-08 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.42 Å) | | 主引用文献 | Hybrid Structure of the RagA/C-Ragulator mTORC1 Activation Complex.
Mol. Cell, 68, 2017
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3ML8
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3ML9
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4HVB
 | | Catalytic unit of PI3Kg in complex with PI3K/mTOR dual inhibitor PF-04979064 | | 分子名称: | 1-{1-[(2S)-2-hydroxypropanoyl]piperidin-4-yl}-3-methyl-8-(6-methylpyridin-3-yl)-1,3-dihydro-2H-imidazo[4,5-c][1,5]naphthyridin-2-one, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | | 著者 | Knighton, D.R, Cheng, H. | | 登録日 | 2012-11-05 | | 公開日 | 2013-11-20 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.35 Å) | | 主引用文献 | Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design.
ACS Med Chem Lett, 4, 2013
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4FA6
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4FAD
 | | Design and Synthesis of a Novel Pyrrolidinyl Pyrido Pyrimidinone Derivative as a Potent Inhibitor of PI3Ka and mTOR | | 分子名称: | 2-amino-6-(5-fluoro-6-methoxypyridin-3-yl)-4-methyl-8-(pyrrolidin-1-yl)pyrido[2,3-d]pyrimidin-7(8H)-one, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | | 著者 | Greasley, S.E, Knighton, D.R, LaFleur Rogers, C.M. | | 登録日 | 2012-05-22 | | 公開日 | 2013-04-03 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kalpha and mTOR
Bioorg.Med.Chem.Lett., 22, 2012
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3O4Z
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5VOK
 | | Crystal structure of the C7orf59-HBXIP dimer | | 分子名称: | Ragulator complex protein LAMTOR4, Ragulator complex protein LAMTOR5 | | 著者 | Rasheed, N, Nascimento, A.F.Z, Bar-Peled, L, Shen, K, Sabatini, D.M, Aparicio, R, Smetana, J.H.C. | | 登録日 | 2017-05-03 | | 公開日 | 2018-05-23 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.89 Å) | | 主引用文献 | C7orf59/Lamtor4 phosphorylation and structural flexibility modulate Ragulator assembly.
Febs Open Bio, 2019
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3PS6
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3PRE
 | | Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors. | | 分子名称: | 2-amino-8-(trans-4-methoxycyclohexyl)-4-methyl-6-(1H-pyrazol-3-yl)pyrido[2,3-d]pyrimidin-7(8H)-one, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | | 著者 | Knighton, D.R, Greasley, S.E, Rodgers, C.M.-L. | | 登録日 | 2010-11-29 | | 公開日 | 2011-02-09 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.91 Å) | | 主引用文献 | Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors.
Bioorg.Med.Chem.Lett., 21, 2011
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