6U62
| Raptor-Rag-Ragulator complex | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, ... | Authors: | Rogala, K.B, Sabatini, D.M. | Deposit date: | 2019-08-29 | Release date: | 2019-10-30 | Last modified: | 2024-03-20 | Method: | ELECTRON MICROSCOPY (3.18 Å) | Cite: | Structural basis for the docking of mTORC1 on the lysosomal surface. Science, 366, 2019
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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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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 | Descriptor: | 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 | Authors: | Murray, J.M, Wiesmann, C. | Deposit date: | 2009-12-10 | Release date: | 2010-02-16 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | 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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5GPG
| Co-crystal structure of the FK506 binding domain of human FKBP25, Rapamycin and the FRB domain of human mTOR | Descriptor: | Peptidyl-prolyl cis-trans isomerase FKBP3, RAPAMYCIN IMMUNOSUPPRESSANT DRUG, Serine/threonine-protein kinase mTOR | Authors: | Lee, H.B, Lee, S.Y, Rhee, H.W, Lee, C.W. | Deposit date: | 2016-08-02 | Release date: | 2016-10-12 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (1.67 Å) | Cite: | 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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4FA6
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4FAD
| Design and Synthesis of a Novel Pyrrolidinyl Pyrido Pyrimidinone Derivative as a Potent Inhibitor of PI3Ka and mTOR | Descriptor: | 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 | Authors: | Greasley, S.E, Knighton, D.R, LaFleur Rogers, C.M. | Deposit date: | 2012-05-22 | Release date: | 2013-04-03 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | 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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4DRJ
| o-crystal structure of the PPIase domain of FKBP52, Rapamycin and the FRB fragment of mTOR | Descriptor: | Peptidyl-prolyl cis-trans isomerase FKBP4, RAPAMYCIN IMMUNOSUPPRESSANT DRUG, SULFATE ION, ... | Authors: | Maerz, A.M, Bracher, A, Hausch, F. | Deposit date: | 2012-02-17 | Release date: | 2013-02-06 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Large FK506-Binding Proteins Shape the Pharmacology of Rapamycin. Mol.Cell.Biol., 33, 2013
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4DRH
| Co-crystal structure of the PPIase domain of FKBP51, Rapamycin and the FRB fragment of mTOR at low pH | Descriptor: | Peptidyl-prolyl cis-trans isomerase FKBP5, RAPAMYCIN IMMUNOSUPPRESSANT DRUG, SULFATE ION, ... | Authors: | Maerz, A.M, Bracher, A, Hausch, F. | Deposit date: | 2012-02-17 | Release date: | 2013-02-06 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Large FK506-Binding Proteins Shape the Pharmacology of Rapamycin. Mol.Cell.Biol., 33, 2013
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4DRI
| Co-crystal structure of the PPIase domain of FKBP51, Rapamycin and the FRB fragment of mTOR | Descriptor: | Peptidyl-prolyl cis-trans isomerase FKBP5, RAPAMYCIN IMMUNOSUPPRESSANT DRUG, Serine/threonine-protein kinase mTOR | Authors: | Maerz, A.M, Bracher, A, Hausch, F. | Deposit date: | 2012-02-17 | Release date: | 2013-02-06 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (1.45 Å) | Cite: | Large FK506-Binding Proteins Shape the Pharmacology of Rapamycin. Mol.Cell.Biol., 33, 2013
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4HVB
| Catalytic unit of PI3Kg in complex with PI3K/mTOR dual inhibitor PF-04979064 | Descriptor: | 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 | Authors: | Knighton, D.R, Cheng, H. | Deposit date: | 2012-11-05 | Release date: | 2013-11-20 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.35 Å) | Cite: | 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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5YK3
| human Ragulator complex | Descriptor: | Ragulator complex protein LAMTOR1, Ragulator complex protein LAMTOR2, Ragulator complex protein LAMTOR3, ... | Authors: | Wu, G, Mu, Z. | Deposit date: | 2017-10-12 | Release date: | 2019-01-23 | Last modified: | 2024-03-27 | Method: | X-RAY DIFFRACTION (3.01 Å) | Cite: | Structural insight into the Ragulator complex which anchors mTORC1 to the lysosomal membrane Cell Discov, 3, 2017
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8DHB
| Active FLCN GAP complex | Descriptor: | BERYLLIUM TRIFLUORIDE ION, Folliculin, Folliculin-interacting protein 2, ... | Authors: | Jansen, R.M, Hurley, J.H. | Deposit date: | 2022-06-25 | Release date: | 2022-09-28 | Method: | ELECTRON MICROSCOPY (3.53 Å) | Cite: | Structural basis for FLCN RagC GAP activation in MiT-TFE substrate-selective mTORC1 regulation. Sci Adv, 8, 2022
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3OAW
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6B9X
| Crystal structure of Ragulator | Descriptor: | Hepatitis B virus x interacting protein, Ragulator complex protein LAMTOR1, Ragulator complex protein LAMTOR2, ... | Authors: | SU, M.-Y, Hurley, J.H. | Deposit date: | 2017-10-11 | Release date: | 2017-11-08 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (1.42 Å) | Cite: | Hybrid Structure of the RagA/C-Ragulator mTORC1 Activation Complex. Mol. Cell, 68, 2017
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5VOK
| Crystal structure of the C7orf59-HBXIP dimer | Descriptor: | Ragulator complex protein LAMTOR4, Ragulator complex protein LAMTOR5 | Authors: | Rasheed, N, Nascimento, A.F.Z, Bar-Peled, L, Shen, K, Sabatini, D.M, Aparicio, R, Smetana, J.H.C. | Deposit date: | 2017-05-03 | Release date: | 2018-05-23 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.89 Å) | Cite: | C7orf59/Lamtor4 phosphorylation and structural flexibility modulate Ragulator assembly. Febs Open Bio, 2019
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5Y3A
| Crystal structure of Ragulator complex (p18 49-161) | Descriptor: | Ragulator complex protein LAMTOR1, Ragulator complex protein LAMTOR2, Ragulator complex protein LAMTOR3, ... | Authors: | Zhang, T, Ding, J. | Deposit date: | 2017-07-28 | Release date: | 2017-12-27 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | 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) | Descriptor: | Ragulator complex protein LAMTOR1, Ragulator complex protein LAMTOR2, Ragulator complex protein LAMTOR3, ... | Authors: | Zhang, T, Ding, J. | Deposit date: | 2017-07-28 | Release date: | 2017-12-06 | Last modified: | 2024-03-27 | Method: | X-RAY DIFFRACTION (2.65 Å) | Cite: | Structural basis for Ragulator functioning as a scaffold in membrane-anchoring of Rag GTPases and mTORC1 Nat Commun, 8, 2017
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3O4Z
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3ML9
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3ML8
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3PS6
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3PRE
| Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors. | Descriptor: | 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 | Authors: | Knighton, D.R, Greasley, S.E, Rodgers, C.M.-L. | Deposit date: | 2010-11-29 | Release date: | 2011-02-09 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (2.91 Å) | Cite: | Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors. Bioorg.Med.Chem.Lett., 21, 2011
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3PRZ
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3LQ9
| Crystal structure of human REDD1, a hypoxia-induced regulator of mTOR | Descriptor: | DNA-damage-inducible transcript 4 protein | Authors: | Vega-Rubin-de-Celis, S, Abdallah, Z, Brugarolas, J, Zhang, X. | Deposit date: | 2010-02-08 | Release date: | 2010-03-09 | Last modified: | 2017-11-01 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Structural analysis and functional implications of the negative mTORC1 regulator REDD1. Biochemistry, 49, 2010
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5Y38
| Crystal structure of C7orf59-HBXIP complex | Descriptor: | Ragulator complex protein LAMTOR4, Ragulator complex protein LAMTOR5, SULFATE ION | Authors: | Zhang, T, Ding, J. | Deposit date: | 2017-07-28 | Release date: | 2017-12-06 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Structural basis for Ragulator functioning as a scaffold in membrane-anchoring of Rag GTPases and mTORC1 Nat Commun, 8, 2017
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