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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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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7UX2
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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 | | Descriptor: | (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 | | Authors: | Murray, J.M, Wiesmann, C. | | Deposit date: | 2011-08-29 | | Release date: | 2011-11-02 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (2.788 Å) | | Cite: | 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 | | 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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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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3OAW
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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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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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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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3ML8
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3O4Z
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3ML9
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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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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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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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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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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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7YRJ
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7YRI
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4FHK
 | | Crystal Structure of PI3K-gamma in Complex with Imidazopyridazine 19e | | Descriptor: | 3-[2-methyl-6-(pyrazin-2-ylamino)pyrimidin-4-yl]-N-(1H-pyrazol-3-yl)imidazo[1,2-b]pyridazin-2-amine, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION | | Authors: | Shaffer, P.L, Tang, J, Yakowec, P. | | Deposit date: | 2012-06-06 | | Release date: | 2013-04-10 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.
Bioorg.Med.Chem.Lett., 22, 2012
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4FHJ
 | | Crystal Structure of PI3K-gamma in Complex with Imidazopyridine 2 | | Descriptor: | 3-(4-amino-6-methyl-1,3,5-triazin-2-yl)-N-(1H-pyrazol-5-yl)imidazo[1,2-a]pyridin-2-amine, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION | | Authors: | Shaffer, P.L, Tang, J, Yakowec, P. | | Deposit date: | 2012-06-06 | | Release date: | 2012-07-18 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.
Bioorg.Med.Chem.Lett., 22, 2012
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