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1

Cao, Ya-Nan, Ling-Li Zheng, Dan Wang, Xiao-Xia Liang, Feng Gao, and Xian-Li Zhou. "Recent advances in microtubule-stabilizing agents." European Journal of Medicinal Chemistry 143 (January 2018): 806–28. http://dx.doi.org/10.1016/j.ejmech.2017.11.062.

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2

Lee, James J., and Sandra M. Swain. "Peripheral Neuropathy Induced by Microtubule-Stabilizing Agents." Journal of Clinical Oncology 24, no. 10 (2006): 1633–42. http://dx.doi.org/10.1200/jco.2005.04.0543.

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Microtubule-stabilizing agents (MTSAs), including the taxanes and epothilones, are effective chemotherapeutic agents for the treatment of many cancers. Neuropathy is a major adverse effect of MTSA-based chemotherapy, with severe peripheral neuropathy (grade 3 or 4) occurring in as many as 30% of patients treated with a MTSA. MTSA-induced neuropathy usually resolves gradually after cessation of the treatment. The most reliable method to accurately assess MTSA-induced neuropathy is by clinical evaluation, although additional techniques are being developed and evaluated. Among MTSA-induced neurop
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3

Field, Jessica J., José Fernando Díaz, and John H. Miller. "The Binding Sites of Microtubule-Stabilizing Agents." Chemistry & Biology 20, no. 3 (2013): 301–15. http://dx.doi.org/10.1016/j.chembiol.2013.01.014.

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4

Mooberry, S. L., D. A. Randall-Hlubek, R. M. Leal, et al. "Microtubule-stabilizing agents based on designed laulimalide analogues." Proceedings of the National Academy of Sciences 101, no. 23 (2004): 8803–8. http://dx.doi.org/10.1073/pnas.0402759101.

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5

Khrapunovich-Baine, Marina, Vilas Menon, Chia-Ping Huang Yang, et al. "Hallmarks of Molecular Action of Microtubule Stabilizing Agents." Journal of Biological Chemistry 286, no. 13 (2011): 11765–78. http://dx.doi.org/10.1074/jbc.m110.162214.

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6

Prota, Andrea E., Katja Bargsten, Didier Zurwerra, et al. "Molecular Mechanism of Action of Microtubule-Stabilizing Anticancer Agents." Science 339, no. 6119 (2013): 587–90. http://dx.doi.org/10.1126/science.1230582.

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Microtubule-stabilizing agents (MSAs) are efficacious chemotherapeutic drugs widely used for the treatment of cancer. Despite the importance of MSAs for medical applications and basic research, their molecular mechanisms of action on tubulin and microtubules remain elusive. We determined high-resolution crystal structures of αβ-tubulin in complex with two unrelated MSAs, zampanolide and epothilone A. Both compounds were bound to the taxane pocket of β-tubulin and used their respective side chains to induce structuring of the M-loop into a short helix. Because the M-loop establishes lateral tub
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Bonini, Sara Anna, Andrea Mastinu, Giulia Ferrari-Toninelli, and Maurizio Memo. "Potential Role of Microtubule Stabilizing Agents in Neurodevelopmental Disorders." International Journal of Molecular Sciences 18, no. 8 (2017): 1627. http://dx.doi.org/10.3390/ijms18081627.

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8

Zhao, Ying, Xin Mu, and Guanhua Du. "Microtubule-stabilizing agents: New drug discovery and cancer therapy." Pharmacology & Therapeutics 162 (June 2016): 134–43. http://dx.doi.org/10.1016/j.pharmthera.2015.12.006.

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9

Brunden, Kurt R., John Q. Trojanowski, Amos B. Smith, Virginia M. Y. Lee, and Carlo Ballatore. "Microtubule-stabilizing agents as potential therapeutics for neurodegenerative disease." Bioorganic & Medicinal Chemistry 22, no. 18 (2014): 5040–49. http://dx.doi.org/10.1016/j.bmc.2013.12.046.

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10

Akbari, Vajihe, and Reza Mofid Mohammad. "binding mod of microtubule stabilizing agents to yeast tubulin." Clinical Biochemistry 44, no. 13 (2011): S101. http://dx.doi.org/10.1016/j.clinbiochem.2011.08.236.

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11

Mulzer, Johann, Karl-Heinz Altmann, Gerhard Höfle, Rolf Müller, and Kathrin Prantz. "Epothilones – A fascinating family of microtubule stabilizing antitumor agents." Comptes Rendus Chimie 11, no. 11-12 (2008): 1336–68. http://dx.doi.org/10.1016/j.crci.2008.02.005.

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12

Chen, Xiaoyan, Angela Winstead, Hongtao Yu, and Jiangnan Peng. "Taccalonolides: A Novel Class of Microtubule-Stabilizing Anticancer Agents." Cancers 13, no. 4 (2021): 920. http://dx.doi.org/10.3390/cancers13040920.

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Microtubule stabilizing agents, such as paclitaxel, docetaxel, and cabazitaxel have been among the most used chemotherapeutic agents in the last decades for the treatment of a wide range of cancers in the clinic. One of the concerns that limit their use in clinical practice is their intrinsic and acquired drug resistance, which is common to most anti-cancer chemotherapeutics. Taccalonolides are a new class of microtubule stabilizers isolated from the roots of a few species in the genus of Tacca. In early studies, taccalonolides demonstrated different effects on interphase and mitotic microtubu
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13

Altaha, Ramin, Tito Fojo, Eddie Reed, and Jame Abraham. "Epothilones: A Novel Class of Non-taxane Microtubule-stabilizing Agents." Current Pharmaceutical Design 8, no. 19 (2002): 1707–12. http://dx.doi.org/10.2174/1381612023394043.

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14

Altmann, Karl-Heinz. "Microtubule-stabilizing agents: a growing class of important anticancer drugs." Current Opinion in Chemical Biology 5, no. 4 (2001): 424–31. http://dx.doi.org/10.1016/s1367-5931(00)00225-8.

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15

Albrethsen, J., R. H. Angeletti, S. B. Horwitz, and C. P. H. Yang. "Proteomics of Cancer Cell Lines Resistant to Microtubule-Stabilizing Agents." Molecular Cancer Therapeutics 13, no. 1 (2013): 260–69. http://dx.doi.org/10.1158/1535-7163.mct-13-0471.

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16

Lee, Sangbae, Yuno Lee, James M. Briggs, and Keun Woo Lee. "Pharmacophore Models of Paclitaxel- and Epothilone-Based Microtubule Stabilizing Agents." Bulletin of the Korean Chemical Society 34, no. 7 (2013): 1972–84. http://dx.doi.org/10.5012/bkcs.2013.34.7.1972.

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17

Smith, Charles D., Susan L. Mooberry, Xinqun Zhang, and Anna-Marija Helt. "A sensitive assay for taxol and other microtubule-stabilizing agents." Cancer Letters 79, no. 2 (1994): 213–19. http://dx.doi.org/10.1016/0304-3835(94)90262-3.

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18

Henry, Jeffrey L., Matthew R. Wilson, Michael P. Mulligan, Taylor R. Quinn, Dan L. Sackett, and Richard E. Taylor. "Synthesis, conformational preferences, and biological activity of conformational analogues of the microtubule-stabilizing agents, (−)-zampanolide and (−)-dactylolide." MedChemComm 10, no. 5 (2019): 800–805. http://dx.doi.org/10.1039/c9md00164f.

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19

Borys, Filip, Ewa Joachimiak, Hanna Krawczyk, and Hanna Fabczak. "Intrinsic and Extrinsic Factors Affecting Microtubule Dynamics in Normal and Cancer Cells." Molecules 25, no. 16 (2020): 3705. http://dx.doi.org/10.3390/molecules25163705.

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Microtubules (MTs), highly dynamic structures composed of α- and β-tubulin heterodimers, are involved in cell movement and intracellular traffic and are essential for cell division. Within the cell, MTs are not uniform as they can be composed of different tubulin isotypes that are post-translationally modified and interact with different microtubule-associated proteins (MAPs). These diverse intrinsic factors influence the dynamics of MTs. Extrinsic factors such as microtubule-targeting agents (MTAs) can also affect MT dynamics. MTAs can be divided into two main categories: microtubule-stabiliz
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20

Fojo, T., and M. Menefee. "Mechanisms of multidrug resistance: the potential role of microtubule-stabilizing agents." Annals of Oncology 18 (July 2007): v3—v8. http://dx.doi.org/10.1093/annonc/mdm172.

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21

Karjala, Geoffrey, Queenie Chan, Emiliano Manzo, Raymond J. Andersen, and Michel Roberge. "Ceratamines, Structurally Simple Microtubule-Stabilizing Antimitotic Agents with Unusual Cellular Effects." Cancer Research 65, no. 8 (2005): 3040–43. http://dx.doi.org/10.1158/0008-5472.can-04-4369.

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22

Brunden, Kurt R., Carlo Ballatore, Virginia M. Y. Lee, Amos B. Smith, and John Q. Trojanowski. "Brain-penetrant microtubule-stabilizing compounds as potential therapeutic agents for tauopathies." Biochemical Society Transactions 40, no. 4 (2012): 661–66. http://dx.doi.org/10.1042/bst20120010.

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Neurons within the brains of those with AD (Alzheimer's disease) and related neurodegenerative disorders, collectively termed ‘tauopathies’, contain fibrillar inclusions composed of hyperphosphorylated tau protein. Tau is normally enriched in axons, where it binds and stabilizes MTs (microtubules). Tau hyperphosphorylation and aggregation probably result in reduced MT binding that could affect axonal transport and neuronal function. A possible therapeutic strategy to overcome a loss of tau function in tauopathies is administration of MT-stabilizing agents, such as those used in the treatment o
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23

Fanale, Daniele, Giuseppe Bronte, Francesco Passiglia, et al. "Stabilizing versus Destabilizing the Microtubules: A Double-Edge Sword for an Effective Cancer Treatment Option?" Analytical Cellular Pathology 2015 (2015): 1–19. http://dx.doi.org/10.1155/2015/690916.

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Microtubules are dynamic and structural cellular components involved in several cell functions, including cell shape, motility, and intracellular trafficking. In proliferating cells, they are essential components in the division process through the formation of the mitotic spindle. As a result of these functions, tubulin and microtubules are targets for anticancer agents. Microtubule-targeting agents can be divided into two groups: microtubule-stabilizing, and microtubule-destabilizing agents. The former bind to the tubulin polymer and stabilize microtubules, while the latter bind to the tubul
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24

Pruschy, M. "94 REGULATION OF PARACRINE SIGNALING BY MICROTUBULE STABILIZING AGENTS AND IONIZING RADIATION." Radiotherapy and Oncology 102 (March 2012): S36. http://dx.doi.org/10.1016/s0167-8140(12)70070-1.

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25

Garcia, Patrick, Diane Braguer, Gérard Carles, and Claudette Briand. "Simultaneous combination of microtubule depolymerizing and stabilizing agents acts at low doses." Anti-Cancer Drugs 6, no. 4 (1995): 533–44. http://dx.doi.org/10.1097/00001813-199508000-00006.

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26

O'Sullivan, David, John H. Miller, Peter T. Northcote, and Anne Camille La Flamme. "Microtubule‐stabilizing agents delay the onset of EAE through inhibition of migration." Immunology & Cell Biology 91, no. 9 (2013): 583–92. http://dx.doi.org/10.1038/icb.2013.47.

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27

Pfeiffer, B., C. N. Kuzniewski, C. Wullschleger, and K. H. Altmann. "ChemInform Abstract: Macrolide-Based Microtubule-Stabilizing Agents: Chemistry and Structure-Activity Relationships." ChemInform 41, no. 24 (2010): no. http://dx.doi.org/10.1002/chin.201024206.

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28

Michaelis, M. L., S. Ansar, Y. Chen та ін. "β-Amyloid-Induced Neurodegeneration and Protection by Structurally Diverse Microtubule-Stabilizing Agents". Journal of Pharmacology and Experimental Therapeutics 312, № 2 (2004): 659–68. http://dx.doi.org/10.1124/jpet.104.074450.

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29

Wen, Wei, Emily Marcinkowski, David Luyimbazi, et al. "Eribulin Synergistically Increases Anti-Tumor Activity of an mTOR Inhibitor by Inhibiting pAKT/pS6K/pS6 in Triple Negative Breast Cancer." Cells 8, no. 9 (2019): 1010. http://dx.doi.org/10.3390/cells8091010.

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Unlike other breast cancer subtypes, patients with triple negative breast cancer (TNBC) have poor outcomes and no effective targeted therapies, leaving an unmet need for therapeutic targets. Efforts to profile these tumors have revealed the PI3K/AKT/mTOR pathway as a potential target. Activation of this pathway also contributes to resistance to anti-cancer agents, including microtubule-targeting agents. Eribulin is one such microtubule-targeting agent that is beneficial in treating taxane and anthracycline refractory breast cancer. In this study, we compared the effect of eribulin on the PI3K/
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30

Bogenberger, James M., Nanna Hansen, Devora Delman, et al. "Synergistic Activity of Lysine Deacetylase Inhibitors and Microtubule-Targeting Agents in AML." Blood 128, no. 22 (2016): 3948. http://dx.doi.org/10.1182/blood.v128.22.3948.3948.

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Abstract Background: Treatment options for elderly acute myeloid leukemia (AML) patients, despite various novel therapies, are still limited. Relapse is common after chemotherapy, and progression on lower intensity treatment with hypomethylating agents is inevitable in all patients even after initial response. Lysine deacetylase inhibitors (KDIs or HDAC inhibitors) have shown limited single-agent clinical activity in AML. Therefore, to develop potential novel treatment options for AML, we aimed to identify synergistic KDI-based drug combinations to build upon the single-agent activity and clin
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31

Pietra, Francesco. "Fighting cancer with microtubule-stabilizing agents: a computational investigation of the complex between β-tubulin and the microtubule-stabilizing, antitumor marine diterpenoid sarcodictyin A". Structural Chemistry 31, № 3 (2019): 927–35. http://dx.doi.org/10.1007/s11224-019-01440-8.

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32

Paterson, Ian, Nicola M. Gardner, and Guy J. Naylor. "Total synthesis of novel dictyostatin analogs and hybrids as microtubule-stabilizing anticancer agents." Pure and Applied Chemistry 81, no. 2 (2009): 169–80. http://dx.doi.org/10.1351/pac-con-08-09-17.

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Structural modification of the dictyostatin macrolide template through adaptation of our total synthesis has led to the identification of a number of potent analogs of this novel microtubule-stabilizing agent. A common synthetic strategy was exploited, employing a (Z)-selective Still-Gennari olefination between various advanced C11-C26 aldehyde and C4-C10 (or C1-C10) β-ketophosphonate intermediates. In vitro evaluation of the growth inhibitory activity of these analogs against both Taxol-sensitive and -resistant human cancer cell lines has provided a foundation for structure-activity relations
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33

Ballatore, Carlo, Kurt R. Brunden, Donna M. Huryn, John Q. Trojanowski, Virginia M. Y. Lee, and Amos B. Smith. "Microtubule Stabilizing Agents as Potential Treatment for Alzheimer’s Disease and Related Neurodegenerative Tauopathies." Journal of Medicinal Chemistry 55, no. 21 (2012): 8979–96. http://dx.doi.org/10.1021/jm301079z.

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34

Abro, Asma, Saima Kulsoom, and Naveeda Riaz. "Pharmacophore model generation for microtubule-stabilizing anti-mitotic agents (MSAAs) against ovarian cancer." Medicinal Chemistry Research 22, no. 9 (2013): 4322–30. http://dx.doi.org/10.1007/s00044-012-0445-8.

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35

Wilmes, Anja, Kelly Bargh, Colleen Kelly, Peter T. Northcote, and John H. Miller. "Peloruside A Synergizes with Other Microtubule Stabilizing Agents in Cultured Cancer Cell Lines." Molecular Pharmaceutics 4, no. 2 (2007): 269–80. http://dx.doi.org/10.1021/mp060101p.

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36

Sáez-Calvo, Gonzalo, Ashwani Sharma, Francisco de Asís Balaguer, et al. "Triazolopyrimidines Are Microtubule-Stabilizing Agents that Bind the Vinca Inhibitor Site of Tubulin." Cell Chemical Biology 24, no. 6 (2017): 737–50. http://dx.doi.org/10.1016/j.chembiol.2017.05.016.

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37

Gasic, Ivana, Brian J. Groendyke, Radosław P. Nowak, et al. "Tubulin Resists Degradation by Cereblon-Recruiting PROTACs." Cells 9, no. 5 (2020): 1083. http://dx.doi.org/10.3390/cells9051083.

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Dysregulation of microtubules and tubulin homeostasis has been linked to developmental disorders, neurodegenerative diseases, and cancer. In general, both microtubule-stabilizing and destabilizing agents have been powerful tools for studies of microtubule cytoskeleton and as clinical agents in oncology. However, many cancers develop resistance to these agents, limiting their utility. We sought to address this by developing a different kind of agent: tubulin-targeted small molecule degraders. Degraders (also known as proteolysis-targeting chimeras (PROTACs)) are compounds that recruit endogenou
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38

Berges, Nina, Katharina Arens, Verena Kreusch, Rainer Fischer, and Stefano Di Fiore. "Toward Discovery of Novel Microtubule Targeting Agents: A SNAP-tag–Based High-Content Screening Assay for the Analysis of Microtubule Dynamics and Cell Cycle Progression." SLAS DISCOVERY: Advancing the Science of Drug Discovery 22, no. 4 (2017): 387–98. http://dx.doi.org/10.1177/2472555216685518.

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Microtubule targeting agents (MTAs) are used for the treatment of cancer. Novel MTAs could provide additional and beneficial therapeutic options. To improve the sensitivity and throughput of standard immunofluorescence assays for the characterization of MTAs, we used SNAP-tag technology to produce recombinant tubulin monomers. To visualize microtubule filaments, A549 cells transfected with SNAP-tubulin were stained with a membrane-permeable, SNAP-reactive dye. The treatment of SNAP-tubulin cells with stabilizing MTAs such as paclitaxel resulted in the formation of coarsely structured microtubu
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39

Miller, John H., and Viswanath Das. "Potential for Treatment of Neurodegenerative Diseases with Natural Products or Synthetic Compounds that Stabilize Microtubules." Current Pharmaceutical Design 26, no. 35 (2020): 4362–72. http://dx.doi.org/10.2174/1381612826666200621171302.

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No effective therapeutics to treat neurodegenerative diseases exist, despite significant attempts to find drugs that can reduce or rescue the debilitating symptoms of tauopathies such as Alzheimer’s disease, Parkinson’s disease, frontotemporal dementia, amyotrophic lateral sclerosis, or Pick’s disease. A number of in vitro and in vivo models exist for studying neurodegenerative diseases, including cell models employing induced-pluripotent stem cells, cerebral organoids, and animal models of disease. Recent research has focused on microtubulestabilizing agents, either natural products or synthe
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40

Chen, Huan, Yongmei Li, Chunquan Sheng, et al. "Design and Synthesis of Cyclopropylamide Analogues of Combretastatin-A4 as Novel Microtubule-Stabilizing Agents." Journal of Medicinal Chemistry 56, no. 3 (2013): 685–99. http://dx.doi.org/10.1021/jm301864s.

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41

Mohanraj, Sumithra, and Mukesh Doble. "3-D QSAR Studies of Microtubule Stabilizing Antimitotic Agents Towards Six Cancer Cell Lines." QSAR & Combinatorial Science 25, no. 10 (2006): 952–60. http://dx.doi.org/10.1002/qsar.200630029.

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42

Teng, Miao, Yong-Ming Dang, Jia-ping Zhang та ін. "Microtubular stability affects cardiomyocyte glycolysis by HIF-1α expression and endonuclear aggregation during early stages of hypoxia". American Journal of Physiology-Heart and Circulatory Physiology 298, № 6 (2010): H1919—H1931. http://dx.doi.org/10.1152/ajpheart.01039.2009.

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Hypoxia-inducible factor (HIF)-1α is a key regulator of anaerobic energy metabolism. We asked the following question: Does the breakdown of microtubular structures influence glycolysis in hypoxic cardiomyocytes by regulating HIF-1α? Neonatal rat cardiomyocytes were cultured under hypoxic conditions, while microtubule-stabilizing (paclitaxel) and -depolymerizing (colchicine) agents were used to change microtubular structure. Models of high microtubule-associated protein 4 (MAP4) expression and RNA interference of microtubulin expression were established. Microtubular structural changes and intr
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43

Vassal, Emilie, Caroline Barette, Xavier Fonrose, Raphaël Dupont, Emmanuelle Sans-Soleilhac, and Laurence Lafanechère. "Miniaturization and Validation of a Sensitive Multiparametric Cell-Based Assay for the Concomitant Detection of Microtubule-Destabilizing and Microtubule-Stabilizing Agents." Journal of Biomolecular Screening 11, no. 4 (2006): 377–89. http://dx.doi.org/10.1177/1087057106286210.

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The authors describe a cell-based assay for anti-microtubule compounds suitable for automation. This assay allows the identification, in a single screening campaign, of both microtubule-destabilizing and microtubule-stabilizing agents. Its rationale is based on the substrate properties of the tubulin-modifying enzymes involved in the tubulin tyrosination cycle. This cycle involves the removal of the C-terminal tyrosine of the tubulin α-subunit by an ill-defined tubulin carboxypeptidase and its readdition by tubulin tyrosine ligase. Because of the substrate properties of these enzymes, dynamic
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44

Maccari, Laura, Fabrizio Manetti, Federico Corelli та Maurizio Botta. "3D QSAR studies for the β-tubulin binding site of microtubule-stabilizing anticancer agents (MSAAs)". Il Farmaco 58, № 9 (2003): 659–68. http://dx.doi.org/10.1016/s0014-827x(03)00099-5.

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45

Ballatore, Carlo, Kurt R. Brunden, John Q. Trojanowski, Virginia M. Y. Lee, and Amos B. Smith. "Non-Naturally Occurring Small Molecule Microtubule-Stabilizing Agents: A Potential Tactic for CNS-Directed Therapies." ACS Chemical Neuroscience 8, no. 1 (2016): 5–7. http://dx.doi.org/10.1021/acschemneuro.6b00384.

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46

NAKAMURA, Machiko, Junko NAKAZAWA, Takeo USUI, Hiroyuki OSADA, Yoshiki KONO, and Akira TAKATSUKI. "Nordihydroguaiaretic Acid, of a New Family of Microtubule-stabilizing Agents, Shows Effects Differentiated from Paclitaxel." Bioscience, Biotechnology, and Biochemistry 67, no. 1 (2003): 151–57. http://dx.doi.org/10.1271/bbb.67.151.

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47

Altmann, Karl-Heinz, and Jürg Gertsch. "Anticancer drugs from nature—natural products as a unique source of new microtubule-stabilizing agents." Nat. Prod. Rep. 24, no. 2 (2007): 327–57. http://dx.doi.org/10.1039/b515619j.

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48

Bergstralh, Daniel T., and Jenny P. Y. Ting. "Microtubule stabilizing agents: Their molecular signaling consequences and the potential for enhancement by drug combination." Cancer Treatment Reviews 32, no. 3 (2006): 166–79. http://dx.doi.org/10.1016/j.ctrv.2006.01.004.

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49

Peronne, Lauralie, Eric Denarier, Ankit Rai, et al. "Two Antagonistic Microtubule Targeting Drugs Act Synergistically to Kill Cancer Cells." Cancers 12, no. 8 (2020): 2196. http://dx.doi.org/10.3390/cancers12082196.

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Paclitaxel is a microtubule stabilizing agent and a successful drug for cancer chemotherapy inducing, however, adverse effects. To reduce the effective dose of paclitaxel, we searched for pharmaceutics which could potentiate its therapeutic effect. We screened a chemical library and selected Carba1, a carbazole, which exerts synergistic cytotoxic effects on tumor cells grown in vitro, when co-administrated with a low dose of paclitaxel. Carba1 targets the colchicine binding-site of tubulin and is a microtubule-destabilizing agent. Catastrophe induction by Carba1 promotes paclitaxel binding to
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50

Norsov, A. K., and S. A. Reva. "The role of taxanes in prostate cancer: literature review." Cancer Urology 14, no. 2 (2018): 130–41. http://dx.doi.org/10.17650/1726-9776-2018-14-2-130-141.

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Prostate cancer is one of the most common causes of death from oncological diseases in men. Taxanes (including docetaxel and cabazitaxel) are microtubule-stabilizing agents which block mitotic cell division leading to apoptosis. Past data have shown promise and good tolerability for different regimens. Recent studies demonstrated that taxanes prolonged the survival both metastatic (hormone sensitive and castrationresistant) locally advanced prostate cancer. In this article, we describe current treatments for рrostate cancer in different stages with taxanes.
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