3RYI
 
 | | GDP-Tubulin: rb3 stathmin-like domain complex | | 分子名称: | GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, ... | | 著者 | Nawrotek, A, Knossow, M, Gigant, B. | | 登録日 | 2011-05-11 | | 公開日 | 2011-10-05 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | The Determinants That Govern Microtubule Assembly from the Atomic Structure of GTP-Tubulin.
J.Mol.Biol., 412, 2011
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5S51
 | | Tubulin-Z1251207602-complex | | 分子名称: | 1-(5-methyl-1,3,4-thiadiazol-2-yl)piperidine, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, ... | | 著者 | Muehlethaler, T, Gioia, D, Prota, A.E, Sharpe, M.E, Cavalli, A, Steinmetz, M.O. | | 登録日 | 2020-11-08 | | 公開日 | 2021-06-30 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Comprehensive Analysis of Binding Sites in Tubulin.
Angew.Chem.Int.Ed.Engl., 60, 2021
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5CA1
 | | Crystal structure of T2R-TTL-Nocodazole complex | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, GLYCEROL, ... | | 著者 | Wang, Y, Yu, Y, Chen, Q, Yang, J. | | 登録日 | 2015-06-29 | | 公開日 | 2015-11-04 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.401 Å) | | 主引用文献 | Structures of a diverse set of colchicine binding site inhibitors in complex with tubulin provide a rationale for drug discovery.
Febs J., 283, 2016
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6HX8
 | | Tubulin-STX3451 complex | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, GUANOSINE-5'-DIPHOSPHATE, ... | | 著者 | Dohle, W, Prota, A.E, Menchon, G, Hamel, E, Steinmetz, M.O, Potter, B.V.L. | | 登録日 | 2018-10-16 | | 公開日 | 2019-02-27 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.402 Å) | | 主引用文献 | Tetrahydroisoquinoline Sulfamates as Potent Microtubule Disruptors: Synthesis, Antiproliferative and Antitubulin Activity of Dichlorobenzyl-Based Derivatives, and a Tubulin Cocrystal Structure.
ACS Omega, 4, 2019
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6FJF
 | | Tubulin-FcMaytansine complex | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, DI(HYDROXYETHYL)ETHER, ... | | 著者 | Menchon, G, Prota, A.E, Lucena Angell, D, Bucher, P, Mueller, R, Paterson, I, Diaz, J.F, Altmann, K.-H, Steinmetz, M.O. | | 登録日 | 2018-01-22 | | 公開日 | 2018-05-30 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.402 Å) | | 主引用文献 | A fluorescence anisotropy assay to discover and characterize ligands targeting the maytansine site of tubulin.
Nat Commun, 9, 2018
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5OV7
 | | tubulin - rigosertib complex | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, GLYCEROL, ... | | 著者 | Menchon, G, Prota, A.E, Steinmetz, M, Jost, M. | | 登録日 | 2017-08-28 | | 公開日 | 2017-10-11 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.402 Å) | | 主引用文献 | Combined CRISPRi/a-Based Chemical Genetic Screens Reveal that Rigosertib Is a Microtubule-Destabilizing Agent.
Mol. Cell, 68, 2017
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6FII
 | | Tubulin-Spongistatin complex | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, DIMETHYL SULFOXIDE, ... | | 著者 | Menchon, G, Prota, A.E, Lucena Angell, D, Bucher, P, Mueller, R, Paterson, I, Diaz, J.F, Altmann, K.-H, Steinmetz, M.O. | | 登録日 | 2018-01-18 | | 公開日 | 2018-05-30 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.405 Å) | | 主引用文献 | A fluorescence anisotropy assay to discover and characterize ligands targeting the maytansine site of tubulin.
Nat Commun, 9, 2018
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5S5K
 | | Tubulin-Z2472938267-complex | | 分子名称: | 1-[2-(2-oxidanylidenepyrrolidin-1-yl)ethyl]-3-phenyl-urea, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, ... | | 著者 | Muehlethaler, T, Gioia, D, Prota, A.E, Sharpe, M.E, Cavalli, A, Steinmetz, M.O. | | 登録日 | 2020-11-08 | | 公開日 | 2021-06-30 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.41 Å) | | 主引用文献 | Comprehensive Analysis of Binding Sites in Tubulin.
Angew.Chem.Int.Ed.Engl., 60, 2021
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8AHM
 | | Crystal structure of tubulin in complex with C(13)/C(13')-Bis-Desmethyl-Disorazole Z | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, DIMETHYL SULFOXIDE, ... | | 著者 | Oliva, M.A, Diaz, J.F, Altmann, K.H. | | 登録日 | 2022-07-22 | | 公開日 | 2022-11-16 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (2.42 Å) | | 主引用文献 | Synthesis and Biological Evaluation of C(13)/C(13')-Bis(desmethyl)disorazole Z.
Angew.Chem.Int.Ed.Engl., 62, 2023
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7DP8
 | | Crystal structure of T2R-TTL-Cevipabulin-eribulin complex | | 分子名称: | (1S,3S,6S,9S,12S,14R,16R,18S,20R,21R,22S,26R,29S,31R,32S,33R,35R,36S)-20-[(2S)-3-amino-2-hydroxypropyl]-21-methoxy-14-methyl-8,15-dimethylidene-2,19,30,34,37,39,40,41-octaoxanonacyclo[24.9.2.1~3,32~.1~3,33~.1~6,9~.1~12,16~.0~18,22~.0~29,36~.0~31,35~]hentetracontan-24-one (non-preferred name), 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 6-[2,6-bis(fluoranyl)-4-[3-(methylamino)propoxy]phenyl]-5-chloranyl-N-[(2S)-1,1,1-tris(fluoranyl)propan-2-yl]-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine, ... | | 著者 | Chen, L.J, Chen, Q, Yu, Y, Yang, J.H. | | 登録日 | 2020-12-18 | | 公開日 | 2021-07-07 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2.446 Å) | | 主引用文献 | Cevipabulin-tubulin complex reveals a novel agent binding site on alpha-tubulin with tubulin degradation effect.
Sci Adv, 7, 2021
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5S57
 | | Tubulin-Z2856434883-complex | | 分子名称: | 1-{4-[(2-phenylethyl)amino]piperidin-1-yl}ethan-1-one, CALCIUM ION, GUANOSINE-5'-DIPHOSPHATE, ... | | 著者 | Muehlethaler, T, Gioia, D, Prota, A.E, Sharpe, M.E, Cavalli, A, Steinmetz, M.O. | | 登録日 | 2020-11-08 | | 公開日 | 2021-06-30 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.45 Å) | | 主引用文献 | Comprehensive Analysis of Binding Sites in Tubulin.
Angew.Chem.Int.Ed.Engl., 60, 2021
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7ZYW
 | | Crystal structure of T2R-TTL-PM534 complex | | 分子名称: | (4R)-N-[(1R)-1-[4-(cyclopropylmethoxy)-6-oxidanylidene-pyran-2-yl]butyl]-4-methyl-2-[(E)-C-methyl-N-oxidanyl-carbonimidoyl]-5H-1,3-thiazole-4-carboxamide, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, ... | | 著者 | Oliva, M.A, Diaz, J.F, Cuevas, C. | | 登録日 | 2022-05-25 | | 公開日 | 2023-11-29 | | 最終更新日 | 2024-06-12 | | 実験手法 | X-RAY DIFFRACTION (2.45 Å) | | 主引用文献 | PM534, an Optimized Target-Protein Interaction Strategy through the Colchicine Site of Tubulin.
J.Med.Chem., 67, 2024
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6EG5
 | | The structure of SB-1-202-tubulin complex | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 4-(2-chloropyrido[2,3-d]pyrimidin-4-yl)-7-methoxy-3,4-dihydroquinoxalin-2(1H)-one, CALCIUM ION, ... | | 著者 | Banerjee, A.K, Wang, Y, Chen, H, Miller, D, Li, W. | | 登録日 | 2018-08-18 | | 公開日 | 2019-08-21 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.45 Å) | | 主引用文献 | The structure of SB-1-202/SB-2-204-tubulin complex
To Be Published
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6KNZ
 | | Crystal structure of T2R-TTL-KXO1 complex | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 2-[5-[4-(2-morpholin-4-ylethoxy)phenyl]pyridin-2-yl]-~{N}-(phenylmethyl)ethanamide, CALCIUM ION, ... | | 著者 | Chen, Q, Yu, Y. | | 登録日 | 2019-08-07 | | 公開日 | 2019-10-23 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2.475 Å) | | 主引用文献 | Reversible binding of the anticancer drug KXO1 (tirbanibulin) to the colchicine-binding site of beta-tubulin explains KXO1's low clinical toxicity.
J.Biol.Chem., 294, 2019
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5GON
 | | Structures of a beta-lactam bridged analogue in complex with tubulin | | 分子名称: | (3R,4R)-4-(4-methoxy-3-oxidanyl-phenyl)-3-methyl-1-(3,4,5-trimethoxyphenyl)azetidin-2-one, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, ... | | 著者 | Zhou, L, Liu, Y, Cheng, L, Wang, Y. | | 登録日 | 2016-07-28 | | 公開日 | 2017-03-22 | | 最終更新日 | 2024-03-20 | | 実験手法 | X-RAY DIFFRACTION (2.48 Å) | | 主引用文献 | Potent Antitumor Activities and Structure Basis of the Chiral beta-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin.
J. Med. Chem., 59, 2016
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5S5I
 | | Tubulin-Z295848548-complex | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 4-[(3-cyclopropyl-1,2,4-oxadiazol-5-yl)methyl]morpholine, CALCIUM ION, ... | | 著者 | Muehlethaler, T, Gioia, D, Prota, A.E, Sharpe, M.E, Cavalli, A, Steinmetz, M.O. | | 登録日 | 2020-11-08 | | 公開日 | 2021-06-30 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.49 Å) | | 主引用文献 | Comprehensive Analysis of Binding Sites in Tubulin.
Angew.Chem.Int.Ed.Engl., 60, 2021
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6GZE
 | | Tubulin-GDP.BeF complex | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, BERYLLIUM TRIFLUORIDE ION, CALCIUM ION, ... | | 著者 | Oliva, M.A, Diaz, J.F. | | 登録日 | 2018-07-04 | | 公開日 | 2020-01-22 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.49 Å) | | 主引用文献 | Structural model for differential cap maturation at growing microtubule ends.
Elife, 9, 2020
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5O7A
 | | Quinolin-6-yloxyacetamides are microtubule destabilizing agents that bind to the colchicine site of tubulin | | 分子名称: | (2~{R})-2-(3-ethynylquinolin-6-yl)oxy-2-methoxy-~{N}-[(1~{E})-1-methoxyimino-2-methyl-propan-2-yl]ethanamide, GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, ... | | 著者 | Sharma, A, Olieric, N, Steinmetz, M.O. | | 登録日 | 2017-06-08 | | 公開日 | 2017-07-05 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (2.495 Å) | | 主引用文献 | Quinolin-6-Yloxyacetamides Are Microtubule Destabilizing Agents That Bind to the Colchicine Site of Tubulin.
Int J Mol Sci, 18, 2017
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5S5H
 | | Tubulin-Z2074076908-complex | | 分子名称: | 1-(5-azaspiro[2.5]octan-5-yl)-2-(difluoromethoxy)ethan-1-one, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, ... | | 著者 | Muehlethaler, T, Gioia, D, Prota, A.E, Sharpe, M.E, Cavalli, A, Steinmetz, M.O. | | 登録日 | 2020-11-08 | | 公開日 | 2021-06-30 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Comprehensive Analysis of Binding Sites in Tubulin.
Angew.Chem.Int.Ed.Engl., 60, 2021
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5SB9
 | | Tubulin-maytansinoid-4a-complex | | 分子名称: | (1S,2R,3S,5S,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.1~10,14~.0~3,5~]hexacosa-10(26),11,13,16,18-pentaen-6-yl phenylacetate, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, ... | | 著者 | Marzullo, P, Boiarska, Z, Perez-Pena, H, Abel, A.-C, Alvarez-Bernad, B, Lucena-Agell, D, Vasile, F, Sironi, M, Steinmetz, M.O, Prota, A.E, Diaz, J.F, Pieraccini, S, Passarella, D. | | 登録日 | 2021-07-20 | | 公開日 | 2021-12-08 | | 最終更新日 | 2024-05-22 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Maytansinol Derivatives: Side Reactions as a Chance for New Tubulin Binders.
Chemistry, 28, 2022
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5SB4
 | | Tubulin-todalam-8-complex | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, GUANOSINE-5'-DIPHOSPHATE, ... | | 著者 | Muehlethaler, T, Milanos, L, Ortega, J.A, Blum, T.B, Gioia, D, Prota, A.E, Cavalli, A, Steinmetz, M.O. | | 登録日 | 2021-07-08 | | 公開日 | 2022-04-27 | | 最終更新日 | 2024-05-22 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Rational Design of a Novel Tubulin Inhibitor with a Unique Mechanism of Action.
Angew.Chem.Int.Ed.Engl., 61, 2022
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5BMV
 | | CRYSTAL STRUCTURE OF TUBULIN-STATHMIN-TTL-Vinblastine COMPLEX | | 分子名称: | (2ALPHA,2'BETA,3BETA,4ALPHA,5BETA)-VINCALEUKOBLASTINE, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, ... | | 著者 | Wang, Y, Chen, Q, Zhang, R. | | 登録日 | 2015-05-23 | | 公開日 | 2016-07-13 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Structural Insights into the Pharmacophore of Vinca Domain Inhibitors of Microtubules.
Mol.Pharmacol., 89, 2016
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4O2A
 | | Tubulin-BAL27862 complex | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 3-[(4-{1-[2-(4-aminophenyl)-2-oxoethyl]-1H-benzimidazol-2-yl}-1,2,5-oxadiazol-3-yl)amino]propanenitrile, ADENOSINE-5'-DIPHOSPHATE, ... | | 著者 | Prota, A.E, Franck, D, Bachmann, F, Bargsten, K, Buey, R.M, Pohlmann, J, Reinelt, S, Lane, H, Steinmetz, M.O. | | 登録日 | 2013-12-17 | | 公開日 | 2014-03-05 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | The Novel Microtubule-Destabilizing Drug BAL27862 Binds to the Colchicine Site of Tubulin with Distinct Effects on Microtubule Organization.
J.Mol.Biol., 426, 2014
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6XER
 | | Tubulin-RB3_SLD in complex with colchicine | | 分子名称: | GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, ... | | 著者 | White, S.W, Yun, M. | | 登録日 | 2020-06-13 | | 公開日 | 2021-08-25 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Design, Synthesis, and Biological Evaluation of Stable Colchicine-Binding Site Tubulin Inhibitors 6-Aryl-2-benzoyl-pyridines as Potential Anticancer Agents.
J.Med.Chem., 64, 2021
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5J2U
 | | Tubulin-MMAF complex | | 分子名称: | CALCIUM ION, GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, ... | | 著者 | Waight, A.B, Bargsten, K, Doronina, S, Steinmetz, M.O, Sussman, D, Prota, A.E. | | 登録日 | 2016-03-30 | | 公開日 | 2016-08-17 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Structural Basis of Microtubule Destabilization by Potent Auristatin Anti-Mitotics.
Plos One, 11, 2016
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