6TH4
| Tubulin-inhibitor complex | Descriptor: | 1,2,3,9-tetramethoxy-6-methylidene-5~{H}-cyclohepta[a]naphthalen-8-one, GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, ... | Authors: | Varela, P.F, Gigant, B. | Deposit date: | 2019-11-18 | Release date: | 2021-12-01 | Last modified: | 2024-01-24 | Method: | X-RAY DIFFRACTION (2.121 Å) | Cite: | B-nor-methylene Colchicinoid PT-100 Selectively Induces Apoptosis in Multidrug-Resistant Human Cancer Cells via an Intrinsic Pathway in a Caspase-Independent Manner Acs Omega, 7, 2022
|
|
7OGN
| Crystal structure of T2R-TTL -mebendazole complex | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, CHLORIDE ION, ... | Authors: | Oliva, M.A, Bonato, F, Diaz, J.F. | Deposit date: | 2021-05-07 | Release date: | 2022-04-06 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Effect of Clinically Used Microtubule Targeting Drugs on Viral Infection and Transport Function. Int J Mol Sci, 23, 2022
|
|
3UT5
| Tubulin-Colchicine-Ustiloxin: Stathmin-like domain complex | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, ... | Authors: | Ranaivoson, F.M, Gigant, B, Knossow, M. | Deposit date: | 2011-11-25 | Release date: | 2012-08-01 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.73 Å) | Cite: | Structural plasticity of tubulin assembly probed by vinca-domain ligands. Acta Crystallogr.,Sect.D, 68, 2012
|
|
8HUH
| Crystal structure of T2R-TTL-3a complex | Descriptor: | 2-(1-methylindol-4-yl)-4-(3,4,5-trimethoxyphenyl)-1~{H}-imidazo[4,5-c]pyridine, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, ... | Authors: | Wang, Y.X, Chen, J.J. | Deposit date: | 2022-12-23 | Release date: | 2023-12-27 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Crystal structure of T2R-TTL-3a complex To Be Published
|
|
8C0F
| Tubulin-PTC596 complex | Descriptor: | 1,2-ETHANEDIOL, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 5-fluoranyl-2-(6-fluoranyl-2-methyl-benzimidazol-1-yl)-~{N}4-[4-(trifluoromethyl)phenyl]pyrimidine-4,6-diamine, ... | Authors: | Prota, A.E, Muehlethaler, T, Weetall, M, Steinmetz, M.O. | Deposit date: | 2022-12-16 | Release date: | 2022-12-28 | Last modified: | 2024-02-07 | Method: | X-RAY DIFFRACTION (2.1005 Å) | Cite: | Preclinical and Early Clinical Development of PTC596, a Novel Small-Molecule Tubulin-Binding Agent Mol Cancer Ther, 20, 2021
|
|
7AU5
| Tubulin-noscapine-analogue-14e complex | Descriptor: | (5~{R})-5-[(1~{S})-4,5-dimethoxy-1,3-dihydro-2-benzofuran-1-yl]-~{N}-ethyl-4-methoxy-7,8-dihydro-5~{H}-[1,3]dioxolo[4,5-g]isoquinoline-6-carboxamide, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, ... | Authors: | Yong, C, Devine, S.M, Abel, A.-C, Muthiah, D, Gao, X, Callaghan, R, Capuano, B, Steinmetz, M.O, Prota, A.E, Scammels, P.J. | Deposit date: | 2020-11-02 | Release date: | 2021-07-07 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | 1,3-Benzodioxole-Modified Noscapine Analogues: Synthesis, Antiproliferative Activity, and Tubulin-Bound Structure. Chemmedchem, 16, 2021
|
|
4EB6
| Tubulin-Vinblastine: Stathmin-like complex | Descriptor: | (2ALPHA,2'BETA,3BETA,4ALPHA,5BETA)-VINCALEUKOBLASTINE, GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, ... | Authors: | Ranaivoson, F.M, Gigant, B, Knossow, M. | Deposit date: | 2012-03-23 | Release date: | 2012-08-01 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (3.47 Å) | Cite: | Structural plasticity of tubulin assembly probed by vinca-domain ligands. Acta Crystallogr.,Sect.D, 68, 2012
|
|
1Z2B
| Tubulin-colchicine-vinblastine: stathmin-like domain complex | Descriptor: | (2ALPHA,2'BETA,3BETA,4ALPHA,5BETA)-VINCALEUKOBLASTINE, 2-MERCAPTO-N-[1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL]ACETAMIDE, GUANOSINE-5'-DIPHOSPHATE, ... | Authors: | Gigant, B, Wang, C, Ravelli, R.B.G, Roussi, F, Steinmetz, M.O, Curmi, P.A, Sobel, A, Knossow, M. | Deposit date: | 2005-03-08 | Release date: | 2005-05-31 | Last modified: | 2023-08-23 | Method: | X-RAY DIFFRACTION (4.1 Å) | Cite: | Structural basis for the regulation of tubulin by vinblastine. Nature, 435, 2005
|
|
6KPP
| BNC105 in complex with tubulin | Descriptor: | (6-methoxy-2-methyl-7-oxidanyl-1-benzofuran-3-yl)-(3,4,5-trimethoxyphenyl)methanone, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, ... | Authors: | Wang, T, Wu, C, Pu, D. | Deposit date: | 2019-08-15 | Release date: | 2020-08-19 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2.74524117 Å) | Cite: | Unraveling the molecular mechanism of BNC105, a phase II clinical trial vascular disrupting agent, provides insights into drug design. Biochem.Biophys.Res.Commun., 2020
|
|
5OSK
| Tubulin-7j complex | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 3-(2,5-Dimethoxybenzyl)-7-sulfamoyloxy-6-methoxy-3,4-dihydroquinazolin-2(1H)-one, CALCIUM ION, ... | Authors: | Menchon, G, Prota, A.E, Steinmetz, M.O, Potter, B.V.L. | Deposit date: | 2017-08-17 | Release date: | 2017-12-20 | Last modified: | 2024-01-17 | Method: | X-RAY DIFFRACTION (2.11 Å) | Cite: | Quinazolinone-Based Anticancer Agents: Synthesis, Antiproliferative SAR, Antitubulin Activity, and Tubulin Co-crystal Structure. J. Med. Chem., 61, 2018
|
|
5J2U
| Tubulin-MMAF complex | Descriptor: | CALCIUM ION, GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, ... | Authors: | Waight, A.B, Bargsten, K, Doronina, S, Steinmetz, M.O, Sussman, D, Prota, A.E. | Deposit date: | 2016-03-30 | Release date: | 2016-08-17 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Structural Basis of Microtubule Destabilization by Potent Auristatin Anti-Mitotics. Plos One, 11, 2016
|
|
5OV7
| tubulin - rigosertib complex | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, GLYCEROL, ... | Authors: | Menchon, G, Prota, A.E, Steinmetz, M, Jost, M. | Deposit date: | 2017-08-28 | Release date: | 2017-10-11 | Last modified: | 2024-01-17 | Method: | X-RAY DIFFRACTION (2.402 Å) | Cite: | Combined CRISPRi/a-Based Chemical Genetic Screens Reveal that Rigosertib Is a Microtubule-Destabilizing Agent. Mol. Cell, 68, 2017
|
|
5JCB
| Microtubule depolymerizing agent podophyllotoxin derivative YJTSF1 | Descriptor: | (5R,5aR,8aS,9R)-9-[(4H-1,2,4-triazol-3-yl)sulfanyl]-5-(3,4,5-trimethoxyphenyl)-5,8,8a,9-tetrahydro-2H-furo[3',4':6,7]naphtho[2,3-d][1,3]dioxol-6(5aH)-one, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, ... | Authors: | Guan, Z, Zhao, W, Yin, P. | Deposit date: | 2016-04-14 | Release date: | 2017-09-27 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Structural Insights into the Inhibition of Tubulin by the Antitumor Agent 4 beta-(1,2,4-triazol-3-ylthio)-4-deoxypodophyllotoxin. ACS Chem. Biol., 12, 2017
|
|
3E22
| Tubulin-colchicine-soblidotin: Stathmin-like domain complex | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, ... | Authors: | Cormier, A, Marchand, M, Ravelli, R.B, Knossow, M, Gigant, B. | Deposit date: | 2008-08-05 | Release date: | 2008-10-21 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (3.8 Å) | Cite: | Structural insight into the inhibition of tubulin by vinca domain peptide ligands Embo Rep., 9, 2008
|
|
6LS4
| A novel anti-tumor agent S-40 in complex with tubulin | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 3-[(4-cyclopropylphenyl)sulfonylamino]-4-methyl-N-(pyridin-3-ylmethyl)benzamide, GLYCEROL, ... | Authors: | Du, T, Lin, S, Ji, M, Xue, N, Liu, Y, Zhang, K, Lu, D, Chen, X, Xu, H. | Deposit date: | 2020-01-17 | Release date: | 2021-01-20 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | A novel orally active microtubule destabilizing agent S-40 targets the colchicine-binding site and shows potent antitumor activity. Cancer Lett., 495, 2020
|
|
8JJB
| Crystal structure of T2R-TTL-Y61 complex | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, CHLORIDE ION, ... | Authors: | Yang, J. | Deposit date: | 2023-05-30 | Release date: | 2024-03-27 | Method: | X-RAY DIFFRACTION (2.68 Å) | Cite: | Structure-based design and synthesis of BML284 derivatives: A novel class of colchicine-site noncovalent tubulin degradation agents. Eur.J.Med.Chem., 268, 2024
|
|
8JJC
| Tubulin-Y62 | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 4-(6,7-dimethoxy-3,4-dihydro-1~{H}-isoquinolin-2-yl)-6-(3-methoxyphenyl)pyrimidin-2-amine, CALCIUM ION, ... | Authors: | Yang, J. | Deposit date: | 2023-05-30 | Release date: | 2024-03-27 | Method: | X-RAY DIFFRACTION (2.76 Å) | Cite: | Structure-based design and synthesis of BML284 derivatives: A novel class of colchicine-site noncovalent tubulin degradation agents. Eur.J.Med.Chem., 268, 2024
|
|
3DU7
| Tubulin-colchicine-phomopsin A: Stathmin-like domain complex | Descriptor: | 2-MERCAPTO-N-[1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL]ACETAMIDE, GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, ... | Authors: | Cormier, A, Marchand, M, Ravelli, R.B, Knossow, M, Gigant, B. | Deposit date: | 2008-07-17 | Release date: | 2008-10-21 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (4.1 Å) | Cite: | Structural insight into the inhibition of tubulin by vinca domain peptide ligands Embo Rep., 9, 2008
|
|
7JFR
| Auristatin bound to tubulin | Descriptor: | Auristatin, CALCIUM ION, GUANOSINE-5'-DIPHOSPHATE, ... | Authors: | Moquist, P.N, Waight, A. | Deposit date: | 2020-07-17 | Release date: | 2020-09-16 | Last modified: | 2023-11-15 | Method: | X-RAY DIFFRACTION (2.35 Å) | Cite: | Novel Auristatins with High Bystander and Cytotoxic Activities in Drug Efflux-positive Tumor Models. Mol.Cancer Ther., 20, 2021
|
|
7LZ8
| Tubulin-RB3_SLD-TTL in complex with compound 5t | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 4-[2-(ethylamino)pyrido[3,2-d]pyrimidin-4-yl]-7-methoxy-3,4-dihydroquinoxalin-2(1H)-one, CALCIUM ION, ... | Authors: | White, S.W, Yun, M. | Deposit date: | 2021-03-09 | Release date: | 2021-09-22 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.92 Å) | Cite: | X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor. J.Med.Chem., 64, 2021
|
|
7LZ7
| Tubulin-RB3_SLD-TTL in complex with compound 5k | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 4-(3,6-dimethyl[1,2]oxazolo[5,4-d]pyrimidin-4-yl)-7-methoxy-3,4-dihydroquinoxalin-2(1H)-one, CALCIUM ION, ... | Authors: | White, S.W, Yun, M. | Deposit date: | 2021-03-09 | Release date: | 2021-09-22 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor. J.Med.Chem., 64, 2021
|
|
3N2G
| TUBULIN-NSC 613863: RB3 Stathmin-like domain complex | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, ... | Authors: | Barbier, P, Dorleans, A, Devred, F, Sanz, L, Allegro, D, Alfonso, C, Knossow, M, Peyrot, V, Andreu, J.M. | Deposit date: | 2010-05-18 | Release date: | 2010-07-28 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (4 Å) | Cite: | Stathmin and interfacial microtubule inhibitors recognize a naturally curved conformation of tubulin dimers. J.Biol.Chem., 285, 2010
|
|
1SA1
| Tubulin-podophyllotoxin: stathmin-like domain complex | Descriptor: | 9-HYDROXY-5-(3,4,5-TRIMETHOXYPHENYL)-5,8,8A,9-TETRAHYDROFURO[3',4':6,7]NAPHTHO[2,3-D][1,3]DIOXOL-6(5AH)-ONE, GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, ... | Authors: | Ravelli, R.B, Gigant, B, Curmi, P.A, Jourdain, I, Lachkar, S, Sobel, A, Knossow, M. | Deposit date: | 2004-02-06 | Release date: | 2004-03-23 | Last modified: | 2023-08-23 | Method: | X-RAY DIFFRACTION (4.2 Å) | Cite: | Insight into tubulin regulation from a complex with colchicine and a stathmin-like domain. Nature, 428, 2004
|
|
7L05
| Complex of novel maytansinoid M24 bound to T2R-TTL (two tubulin alpha/beta heterodimers, RB3 stathmin-like domain, and tubulin tyrosine ligase) | Descriptor: | (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 (2S)-2-{methyl[3-(methylamino)propanoyl]amino}propanoate (non-preferred name), 1,2-ETHANEDIOL, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, ... | Authors: | Franklin, M.C. | Deposit date: | 2020-12-11 | Release date: | 2021-12-22 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.21 Å) | Cite: | A Biparatopic Antibody-Drug Conjugate to Treat MET-Expressing Cancers, Including Those that Are Unresponsive to MET Pathway Blockade. Mol.Cancer Ther., 20, 2021
|
|
1SA0
| TUBULIN-COLCHICINE: STATHMIN-LIKE DOMAIN COMPLEX | Descriptor: | 2-MERCAPTO-N-[1,2,3,10-TETRAMETHOXY-9-OXO-5,6,7,9-TETRAHYDRO-BENZO[A]HEPTALEN-7-YL]ACETAMIDE, GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, ... | Authors: | Ravelli, R.B, Gigant, B, Curmi, P.A, Jourdain, I, Lachkar, S, Sobel, A, Knossow, M. | Deposit date: | 2004-02-06 | Release date: | 2004-03-23 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (3.58 Å) | Cite: | Insight into tubulin regulation from a complex with colchicine and a stathmin-like domain. Nature, 428, 2004
|
|