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  • Microtubule-Targeting Agent... Microtubule-Targeting Agents: Strategies To Hijack the Cytoskeleton
    Steinmetz, Michel O.; Prota, Andrea E. Trends in cell biology, October 2018, 2018-10-00, 20181001, Volume: 28, Issue: 10
    Journal Article
    Peer reviewed

    Microtubule-targeting agents (MTAs) such as paclitaxel and the vinca alkaloids are among the most important medical weapons available to combat cancer. MTAs interfere with intracellular transport, ...
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  • Structural Basis of Microtu... Structural Basis of Microtubule Destabilization by Potent Auristatin Anti-Mitotics
    Waight, Andrew B; Bargsten, Katja; Doronina, Svetlana ... PloS one, 08/2016, Volume: 11, Issue: 8
    Journal Article
    Peer reviewed
    Open access

    The auristatin class of microtubule destabilizers are highly potent cytotoxic agents against several cancer cell types when delivered as antibody drug conjugates. Here we describe the high resolution ...
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  • Molecular Mechanism of Acti... Molecular Mechanism of Action of Microtubule-Stabilizing Anticancer Agents
    Prota, Andrea E.; Bargsten, Katja; Zurwerra, Didier ... Science (American Association for the Advancement of Science), 02/2013, Volume: 339, Issue: 6119
    Journal Article
    Peer reviewed
    Open access

    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 ...
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  • Comprehensive Analysis of B... Comprehensive Analysis of Binding Sites in Tubulin
    Mühlethaler, Tobias; Gioia, Dario; Prota, Andrea E. ... Angewandte Chemie, June 7, 2021, Volume: 60, Issue: 24
    Journal Article
    Peer reviewed
    Open access

    Tubulin plays essential roles in vital cellular activities and is the target of a wide range of proteins and ligands. Here, using a combined computational and crystallographic fragment screening ...
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  • new tubulin-binding site an... new tubulin-binding site and pharmacophore for microtubule-destabilizing anticancer drugs
    Prota, Andrea E.; Bargsten, Katja; Diaz, J. Fernando ... Proceedings of the National Academy of Sciences - PNAS, 09/2014, Volume: 111, Issue: 38
    Journal Article
    Peer reviewed
    Open access

    Significance Microtubules are dynamic protein filaments assembled from tubulin subunits, which play a key role for cell division. Ligands that target microtubules and affect their dynamics belong to ...
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  • Serial millisecond crystall... Serial millisecond crystallography for routine room-temperature structure determination at synchrotrons
    Weinert, Tobias; Olieric, Natacha; Cheng, Robert ... Nature communications, 09/2017, Volume: 8, Issue: 1
    Journal Article
    Peer reviewed
    Open access

    Historically, room-temperature structure determination was succeeded by cryo-crystallography to mitigate radiation damage. Here, we demonstrate that serial millisecond crystallography at a ...
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  • Structure-based discovery a... Structure-based discovery and rational design of microtubule-targeting agents
    Steinmetz, Michel O.; Prota, Andrea E. Current opinion in structural biology, 08/2024, Volume: 87
    Journal Article
    Peer reviewed
    Open access

    Microtubule-targeting agents (MTAs) have demonstrated remarkable efficacy as antitumor, antifungal, antiparasitic, and herbicidal agents, finding applications in the clinical, veterinary, and ...
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  • Gatorbulin-1, a distinct cy... Gatorbulin-1, a distinct cyclodepsipeptide chemotype, targets a seventh tubulin pharmacological site
    Matthew, Susan; Chen, Qi-Yin; Ratnayake, Ranjala ... Proceedings of the National Academy of Sciences - PNAS, 03/2021, Volume: 118, Issue: 9
    Journal Article
    Peer reviewed
    Open access

    Tubulin-targeted chemotherapy has proven to be a successful and wide spectrum strategy against solid and liquid malignancies. Therefore, new ways to modulate this essential protein could lead to new ...
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  • Computational Approaches to... Computational Approaches to the Rational Design of Tubulin-Targeting Agents
    Pérez-Peña, Helena; Abel, Anne-Catherine; Shevelev, Maxim ... Biomolecules, 02/2023, Volume: 13, Issue: 2
    Journal Article
    Peer reviewed
    Open access

    Microtubules are highly dynamic polymers of α,β-tubulin dimers which play an essential role in numerous cellular processes such as cell proliferation and intracellular transport, making them an ...
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  • Structural Basis of Microtu... Structural Basis of Microtubule Stabilization by Laulimalide and Peloruside A
    Prota, Andrea E.; Bargsten, Katja; Northcote, Peter T. ... Angewandte Chemie (International ed.), February 3, 2014, Volume: 53, Issue: 6
    Journal Article
    Peer reviewed

    Laulimalide and peloruside A are microtubule‐stabilizing agents (MSAs), the mechanism of action on microtubules of which is poorly defined. Here, using X‐ray crystallography it is shown that ...
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