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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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6Y4N
 | | Structure of Tubulin Tyrosine Ligase in Complex with Tb116 | | Descriptor: | (2~{R})-1-methylpiperidine-2-carboxylic acid, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, ... | | Authors: | Gavrilyuk, J, Nocek, B, Rigol, S, Nicolaou, K.C, Stoll, V. | | Deposit date: | 2020-02-21 | | Release date: | 2021-03-31 | | Last modified: | 2022-11-23 | | Method: | X-RAY DIFFRACTION (2.852 Å) | | Cite: | Design, Synthesis, and Biological Evaluation of Tubulysin Analogues, Linker-Drugs, and Antibody-Drug Conjugates, Insights into Structure-Activity Relationships, and Tubulysin-Tubulin Binding Derived from X-ray Crystallographic Analysis.
J.Org.Chem., 86, 2021
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6Y4M
 | | Structure of Tubulin Tyrosine Ligase in Complex with Tb111 | | Descriptor: | (2~{R})-1-methylpiperidine-2-carboxylic acid, (2~{S},4~{R})-4-azanyl-2-methyl-5-phenyl-pentanoic acid, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, ... | | Authors: | Gavrilyuk, J, Nocek, B, Rigol, S, Nicolaou, K.C, Stoll, V. | | Deposit date: | 2020-02-21 | | Release date: | 2021-03-31 | | Last modified: | 2022-11-23 | | Method: | X-RAY DIFFRACTION (3.34 Å) | | Cite: | Design, Synthesis, and Biological Evaluation of Tubulysin Analogues, Linker-Drugs, and Antibody-Drug Conjugates, Insights into Structure-Activity Relationships, and Tubulysin-Tubulin Binding Derived from X-ray Crystallographic Analysis.
J.Org.Chem., 86, 2021
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4TV9
 | | Tubulin-PM060184 complex | | Descriptor: | (1Z,4S,6Z)-1-[(N-{(2Z,4Z,6E,8S)-8-[(2S)-5-methoxy-6-oxo-3,6-dihydro-2H-pyran-2-yl]-6-methylnona-2,4,6-trienoyl}-3-methy l-L-valyl)amino]octa-1,6-dien-4-yl carbamate, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, ... | | Authors: | Prota, A.E, Bargsten, K, Diaz, J.F, Marsh, M, Cuevas, C, Liniger, M, Neuhaus, C, Andreu, J.M, Altmann, K.H, Steinmetz, M.O. | | Deposit date: | 2014-06-26 | | Release date: | 2014-08-20 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | A new tubulin-binding site and pharmacophore for microtubule-destabilizing anticancer drugs.
Proc.Natl.Acad.Sci.USA, 111, 2014
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4TUY
 | | Tubulin-Rhizoxin complex | | Descriptor: | (1R,2R,3E,5R,7R,8S,10S,13E,16R)-8-hydroxy-10-[(2S,3R,4E,6E,8E)-3-methoxy-4,8-dimethyl-9-(2-methyl-1,3-oxazol-4-yl)nona-4,6,8-trien-2-yl]-2,7-dimethyl-6,11,19-trioxatricyclo[14.3.1.0~5,7~]icosa-3,13-diene-12,18-dione, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, ... | | Authors: | Prota, A.E, Bargsten, K, Diaz, J.F, Marsh, M, Cuevas, C, Liniger, M, Neuhaus, C, Andreu, J.M, Altmann, K.H, Steinmetz, M.O. | | Deposit date: | 2014-06-25 | | Release date: | 2014-08-27 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | A new tubulin-binding site and pharmacophore for microtubule-destabilizing anticancer drugs.
Proc.Natl.Acad.Sci.USA, 111, 2014
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4TV8
 | | Tubulin-Maytansine complex | | Descriptor: | (3beta,4beta,5beta,10beta,11E,13E)-maytansine, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, CALCIUM ION, ... | | Authors: | Prota, A.E, Bargsten, K, Diaz, J.F, Marsh, M, Cuevas, C, Liniger, M, Neuhaus, C, Andreu, J.M, Altmann, K.H, Steinmetz, M.O. | | Deposit date: | 2014-06-26 | | Release date: | 2014-08-27 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.103 Å) | | Cite: | A new tubulin-binding site and pharmacophore for microtubule-destabilizing anticancer drugs.
Proc.Natl.Acad.Sci.USA, 111, 2014
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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
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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
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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
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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
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3HKB
 | | Tubulin: RB3 Stathmin-like domain complex | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, ... | | Authors: | Dorleans, A, Gigant, B, Ravelli, R.B.G, Mailliet, P, Mikol, V, Knossow, M. | | Deposit date: | 2009-05-23 | | Release date: | 2009-09-01 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (3.65 Å) | | Cite: | Variations in the colchicine-binding domain provide insight into the structural switch of tubulin
Proc.Natl.Acad.Sci.USA, 106, 2009
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3HKC
 | | Tubulin-ABT751: RB3 stathmin-like domain complex | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, ... | | Authors: | Dorleans, A, Gigant, B, Ravelli, R.B.G, Mailliet, P, Mikol, V, Knossow, M. | | Deposit date: | 2009-05-23 | | Release date: | 2009-09-01 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (3.8 Å) | | Cite: | Variations in the colchicine-binding domain provide insight into the structural switch of tubulin
Proc.Natl.Acad.Sci.USA, 106, 2009
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3HKE
 | | Tubulin-T138067: RB3 stathmin-like domain complex | | Descriptor: | 2,3,4,5,6-pentafluoro-N-(3-fluoro-4-methoxyphenyl)benzenesulfonamide, GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, ... | | Authors: | Dorleans, A, Gigant, B, Ravelli, R.B.G, Mailliet, P, Mikol, V, Knossow, M. | | Deposit date: | 2009-05-23 | | Release date: | 2009-09-01 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (3.6 Å) | | Cite: | Variations in the colchicine-binding domain provide insight into the structural switch of tubulin
Proc.Natl.Acad.Sci.USA, 106, 2009
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3HKD
 | | Tubulin-TN16 : RB3 stathmin-like domain complex | | Descriptor: | (3Z,5S)-5-benzyl-3-[1-(phenylamino)ethylidene]pyrrolidine-2,4-dione, GUANOSINE-5'-DIPHOSPHATE, GUANOSINE-5'-TRIPHOSPHATE, ... | | Authors: | Dorleans, A, Gigant, B, Ravelli, R.B.G, Mailliet, P, Mikol, V, Knossow, M. | | Deposit date: | 2009-05-23 | | Release date: | 2009-09-01 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (3.7 Å) | | Cite: | Variations in the colchicine-binding domain provide insight into the structural switch of tubulin
Proc.Natl.Acad.Sci.USA, 106, 2009
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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
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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
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