8Y0U
 
 | | dormant ribosome with STM1 | | 分子名称: | 18S rRNA, 25S rRNA, 40S ribosomal protein S1-A, ... | | 著者 | Du, M, Zeng, F. | | 登録日 | 2024-01-23 | | 公開日 | 2024-02-07 | | 実験手法 | ELECTRON MICROSCOPY (3.59 Å) | | 主引用文献 | dormant ribosome with STM1
To Be Published
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8PPZ
 | | Co-crystal structure of FKBP12, compound 7 and the FRB fragment of mTOR | | 分子名称: | (1~{S},5~{S},6~{R})-10-[3,5-bis(chloranyl)phenyl]sulfonyl-5-[(~{E})-2-(2-chlorophenyl)ethenyl]-3-(pyridin-2-ylmethyl)-3,10-diazabicyclo[4.3.1]decan-2-one, ACETATE ION, CALCIUM ION, ... | | 著者 | Meyners, C, Deutscher, R.C.E, Hausch, F. | | 登録日 | 2023-07-10 | | 公開日 | 2023-08-09 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | Co-crystal structure of FKBP12, compound 7 and the FRB fragment of mTOR
Chemrxiv, 2023
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8FW5
 | | Chimeric HsGATOR1-SpGtr-SpLam complex | | 分子名称: | ALUMINUM FLUORIDE, GATOR complex protein DEPDC5, GATOR complex protein NPRL2, ... | | 著者 | Tettoni, S.D, Egri, S.B, Doxsey, D.D, Ouch, C, Chang, J, Song, K, Xu, C, Shen, K. | | 登録日 | 2023-01-20 | | 公開日 | 2023-07-26 | | 最終更新日 | 2023-09-20 | | 実験手法 | ELECTRON MICROSCOPY (3.08 Å) | | 主引用文献 | Structure of the Schizosaccharomyces pombe Gtr-Lam complex reveals evolutionary divergence of mTORC1-dependent amino acid sensing.
Structure, 31, 2023
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8SBJ
 | | Co-structure Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform complexed with brain penetrant inhibitors | | 分子名称: | (2M)-7-[(3R)-3-methylmorpholin-4-yl]-5-[(3S)-3-methylmorpholin-4-yl]-2-(1H-pyrazol-3-yl)-3H-imidazo[4,5-b]pyridine, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | 著者 | Knapp, M.S, Elling, R.A, Tang, J. | | 登録日 | 2023-04-03 | | 公開日 | 2023-07-19 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Identification of Brain-Penetrant ATP-Competitive mTOR Inhibitors for CNS Syndromes.
J.Med.Chem., 66, 2023
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8SBC
 | | Co-structure of Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform and brain penetrant inhibitors | | 分子名称: | (2M)-7-[(3R)-3-methylmorpholin-4-yl]-5-[(3S)-3-methylmorpholin-4-yl]-2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyridine, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, ... | | 著者 | Knapp, M.S, Elling, R.A, Tang, J. | | 登録日 | 2023-04-03 | | 公開日 | 2023-07-19 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Identification of Brain-Penetrant ATP-Competitive mTOR Inhibitors for CNS Syndromes.
J.Med.Chem., 66, 2023
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8JD0
 | | Cryo-EM structure of mGlu2-mGlu3 heterodimer in presence of NAM563 | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 4-(1-methylpyrazol-4-yl)-7-[[(2~{S})-2-(trifluoromethyl)morpholin-4-yl]methyl]quinoline-2-carboxamide, CHOLESTEROL, ... | | 著者 | Wang, X, Wang, M, Xu, T, Feng, Y, Han, S, Lin, S, Zhao, Q, Wu, B. | | 登録日 | 2023-05-12 | | 公開日 | 2023-06-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Structural insights into dimerization and activation of the mGlu2-mGlu3 and mGlu2-mGlu4 heterodimers.
Cell Res., 33, 2023
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8JCZ
 | | Cryo-EM structure of mGlu2-mGlu3 heterodimer in presence of LY341495, NAM563, and LY2389575 (dimerization mode III) | | 分子名称: | 2-[(1S,2S)-2-carboxycyclopropyl]-3-(9H-xanthen-9-yl)-D-alanine, 2-acetamido-2-deoxy-beta-D-glucopyranose, Metabotropic glutamate receptor 2,Peptidyl-prolyl cis-trans isomerase FKBP1A, ... | | 著者 | Wang, X, Wang, M, Xu, T, Feng, Y, Han, S, Lin, S, Zhao, Q, Wu, B. | | 登録日 | 2023-05-12 | | 公開日 | 2023-06-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | Structural insights into dimerization and activation of the mGlu2-mGlu3 and mGlu2-mGlu4 heterodimers.
Cell Res., 33, 2023
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8JD1
 | | Cryo-EM structure of mGlu2-mGlu3 heterodimer in Rco state | | 分子名称: | CHOLESTEROL, GLUTAMIC ACID, Metabotropic glutamate receptor 2,Peptidyl-prolyl cis-trans isomerase FKBP1A, ... | | 著者 | Wang, X, Wang, M, Xu, T, Feng, Y, Han, S, Lin, S, Zhao, Q, Wu, B. | | 登録日 | 2023-05-12 | | 公開日 | 2023-06-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | ELECTRON MICROSCOPY (3.7 Å) | | 主引用文献 | Structural insights into dimerization and activation of the mGlu2-mGlu3 and mGlu2-mGlu4 heterodimers.
Cell Res., 33, 2023
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8JCV
 | | Cryo-EM structure of mGlu2-mGlu3 heterodimer in presence of LY341495 (dimerization mode II) | | 分子名称: | 2-[(1S,2S)-2-carboxycyclopropyl]-3-(9H-xanthen-9-yl)-D-alanine, 2-acetamido-2-deoxy-beta-D-glucopyranose, Metabotropic glutamate receptor 2,Peptidyl-prolyl cis-trans isomerase FKBP1A, ... | | 著者 | Wang, X, Wang, M, Xu, T, Feng, Y, Han, S, Zhao, Q, Wu, B. | | 登録日 | 2023-05-12 | | 公開日 | 2023-06-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | ELECTRON MICROSCOPY (3.4 Å) | | 主引用文献 | Structural insights into dimerization and activation of the mGlu2-mGlu3 and mGlu2-mGlu4 heterodimers.
Cell Res., 33, 2023
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8JCU
 | | Cryo-EM structure of mGlu2-mGlu3 heterodimer in presence of LY341495 (dimerization mode I) | | 分子名称: | 2-[(1S,2S)-2-carboxycyclopropyl]-3-(9H-xanthen-9-yl)-D-alanine, 2-acetamido-2-deoxy-beta-D-glucopyranose, Metabotropic glutamate receptor 2,Peptidyl-prolyl cis-trans isomerase FKBP1A, ... | | 著者 | Wang, X, Wang, M, Xu, T, Feng, Y, Zhao, Q, Wu, B. | | 登録日 | 2023-05-12 | | 公開日 | 2023-06-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | ELECTRON MICROSCOPY (2.8 Å) | | 主引用文献 | Structural insights into dimerization and activation of the mGlu2-mGlu3 and mGlu2-mGlu4 heterodimers.
Cell Res., 33, 2023
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8JCX
 | | Cryo-EM structure of mGlu2-mGlu3 heterodimer in presence of LY341495 and NAM563 (dimerization mode II) | | 分子名称: | 2-[(1S,2S)-2-carboxycyclopropyl]-3-(9H-xanthen-9-yl)-D-alanine, 2-acetamido-2-deoxy-beta-D-glucopyranose, Metabotropic glutamate receptor 2,Peptidyl-prolyl cis-trans isomerase FKBP1A, ... | | 著者 | Wang, X, Wang, M, Xu, T, Feng, Y, Han, S, Lin, S, Zhao, Q, Wu, B. | | 登録日 | 2023-05-12 | | 公開日 | 2023-06-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | Structural insights into dimerization and activation of the mGlu2-mGlu3 and mGlu2-mGlu4 heterodimers.
Cell Res., 33, 2023
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8JCY
 | | Cryo-EM structure of mGlu2-mGlu3 heterodimer in presence of LY341495, NAM563, and LY2389575 (dimerization mode I) | | 分子名称: | 2-[(1S,2S)-2-carboxycyclopropyl]-3-(9H-xanthen-9-yl)-D-alanine, 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL, ... | | 著者 | Wang, X, Wang, M, Xu, T, Feng, Y, Han, S, Lin, S, Zhao, Q, Wu, B. | | 登録日 | 2023-05-12 | | 公開日 | 2023-06-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | ELECTRON MICROSCOPY (2.9 Å) | | 主引用文献 | Structural insights into dimerization and activation of the mGlu2-mGlu3 and mGlu2-mGlu4 heterodimers.
Cell Res., 33, 2023
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8JD4
 | | Cryo-EM structure of G protein-free mGlu2-mGlu4 heterodimer in Acc state | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, GLUTAMIC ACID, Metabotropic glutamate receptor 2,Peptidyl-prolyl cis-trans isomerase FKBP1A, ... | | 著者 | Wang, X, Wang, M, Xu, T, Feng, Y, Han, S, Lin, S, Zhao, Q, Wu, B. | | 登録日 | 2023-05-12 | | 公開日 | 2023-06-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | ELECTRON MICROSCOPY (2.9 Å) | | 主引用文献 | Structural insights into dimerization and activation of the mGlu2-mGlu3 and mGlu2-mGlu4 heterodimers.
Cell Res., 33, 2023
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8JCW
 | | Cryo-EM structure of mGlu2-mGlu3 heterodimer in presence of LY341495 and NAM563 (dimerization mode I) | | 分子名称: | 2-[(1S,2S)-2-carboxycyclopropyl]-3-(9H-xanthen-9-yl)-D-alanine, 2-acetamido-2-deoxy-beta-D-glucopyranose, CHOLESTEROL, ... | | 著者 | Wang, X, Wang, M, Xu, T, Feng, Y, Han, S, Lin, S, Zhao, Q, Wu, B. | | 登録日 | 2023-05-12 | | 公開日 | 2023-06-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | Structural insights into dimerization and activation of the mGlu2-mGlu3 and mGlu2-mGlu4 heterodimers.
Cell Res., 33, 2023
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8JD2
 | | Cryo-EM structure of G protein-free mGlu2-mGlu3 heterodimer in Acc state | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, GLUTAMIC ACID, Metabotropic glutamate receptor 2,Peptidyl-prolyl cis-trans isomerase FKBP1A, ... | | 著者 | Wang, X, Wang, M, Xu, T, Feng, Y, Han, S, Lin, S, Zhao, Q, Wu, B. | | 登録日 | 2023-05-12 | | 公開日 | 2023-06-21 | | 最終更新日 | 2023-10-18 | | 実験手法 | ELECTRON MICROSCOPY (2.8 Å) | | 主引用文献 | Structural insights into dimerization and activation of the mGlu2-mGlu3 and mGlu2-mGlu4 heterodimers.
Cell Res., 33, 2023
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8FNY
 | | Nucleotide-bound structure of a functional construct of eukaryotic elongation factor 2 kinase. | | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, ADENOSINE-5'-TRIPHOSPHATE, CALCIUM ION, ... | | 著者 | Piserchio, A, Isiorho, E.A, Dalby, K.N, Ghose, R. | | 登録日 | 2022-12-28 | | 公開日 | 2023-05-03 | | 実験手法 | X-RAY DIFFRACTION (2.22 Å) | | 主引用文献 | ADP enhances the allosteric activation of eukaryotic elongation factor 2 kinase by calmodulin.
Proc.Natl.Acad.Sci.USA, 120, 2023
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8FO6
 | | Nucleotide-free structure of a functional construct of eukaryotic elongation factor 2 kinase. | | 分子名称: | CALCIUM ION, Calmodulin-1, Eukaryotic elongation factor 2 kinase, ... | | 著者 | Piserchio, A, Isiorho, E.A, Dalby, K.N, Ghose, R. | | 登録日 | 2022-12-29 | | 公開日 | 2023-05-03 | | 実験手法 | X-RAY DIFFRACTION (2.553 Å) | | 主引用文献 | ADP enhances the allosteric activation of eukaryotic elongation factor 2 kinase by calmodulin.
Proc.Natl.Acad.Sci.USA, 120, 2023
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7Y62
 | | Crystal structure of human TFEB HLHLZ domain | | 分子名称: | Transcription factor EB | | 著者 | Yang, G, Li, P, Lin, Y, Liu, Z, Sun, H, Zhao, Z, Fang, P, Wang, J. | | 登録日 | 2022-06-18 | | 公開日 | 2023-03-22 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | A small-molecule drug inhibits autophagy gene expression through the central regulator TFEB.
Proc.Natl.Acad.Sci.USA, 120, 2023
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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 | | 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
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8ERA
 | | RMC-5552 in complex with mTORC1 and FKBP12 | | 分子名称: | (3S,5R,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,30R,34aS)-5,9,27-trihydroxy-3-{(2R)-1-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl}-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-5,6,9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-octadecahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontine-1,11,28,29(4H,31H)-tetrone, 1-[6-{[(3M)-4-amino-3-(2-amino-1,3-benzoxazol-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl}-3,4-dihydroisoquinolin-2(1H)-yl]-3-hydroxypropan-1-one, Peptidyl-prolyl cis-trans isomerase FKBP1A, ... | | 著者 | Tomlinson, A.C.A, Yano, J.K. | | 登録日 | 2022-10-11 | | 公開日 | 2022-12-28 | | 最終更新日 | 2023-01-25 | | 実験手法 | ELECTRON MICROSCOPY (2.86 Å) | | 主引用文献 | Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors.
J.Med.Chem., 66, 2023
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8ER6
 | | FKBP12-FRB in Complex with Compound 11 | | 分子名称: | (3S,5R,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,30R,34aS)-5,9,27-trihydroxy-3-{(2R)-1-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl}-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-5,6,9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-octadecahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontine-1,11,28,29(4H,31H)-tetrone, 1,2-ETHANEDIOL, Peptidyl-prolyl cis-trans isomerase FKBP1A, ... | | 著者 | Tomlinson, A.C.A, Yano, J.K. | | 登録日 | 2022-10-11 | | 公開日 | 2022-12-28 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (2.81 Å) | | 主引用文献 | Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors.
J.Med.Chem., 66, 2023
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8ER7
 | | FKBP12-FRB in Complex with Compound 12 | | 分子名称: | (3S,5R,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,30R,34aS)-9,27-dihydroxy-3-{(2R)-1-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl}-5,10,21-trimethoxy-6,8,12,14,20,26-hexamethyl-5,6,9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-octadecahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontine-1,11,28,29(4H,31H)-tetrone, CHLORIDE ION, Peptidyl-prolyl cis-trans isomerase FKBP1A, ... | | 著者 | Tomlinson, A.C.A, Yano, J.K. | | 登録日 | 2022-10-11 | | 公開日 | 2022-12-28 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (3.07 Å) | | 主引用文献 | Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors.
J.Med.Chem., 66, 2023
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7UXC
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7UXH
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7UX2
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