Recent progress with microtubule stabilizers: new compounds, binding modes and cellular activities
TLDR
Recent progress in the chemistry and biology of these diverse microtubule stabilizers focusing on the wide range of organisms that produce these compounds, their mechanisms of inhibiting microtubules-dependent processes, mechanisms of drug resistance, and their interactions with tubulin including their distinct binding sites and modes are covered.About:
This article is published in Natural Product Reports.The article was published on 2014-02-11 and is currently open access. It has received 113 citations till now.read more
Citations
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Paclitaxel targets FOXM1 to regulate KIF20A in mitotic catastrophe and breast cancer paclitaxel resistance
Pasarat Khongkow,Ana R. Gomes,Chun Gong,Chun Gong,E P S Man,J W-H Tsang,Fung Zhao,Fung Zhao,Lara J. Monteiro,R. C. Coombes,René H. Medema,Ui-Soon Khoo,E W-F Lam +12 more
TL;DR: It is suggested that paclitaxel targets the FOXM1-KIF20A axis to drive abnormal mitotic spindle formation and mitotic catastrophe and that deregulated FoxM1 and Kif20A expression may confer paclitAXel resistance.
Journal ArticleDOI
Recent advances in microtubule-stabilizing agents
TL;DR: This review focuses on the natural sources, structural features, mechanisms of action, structure-activity relationship (SAR) and chemical synthesis of MSAs, which mainly include paclitaxel, taccalonolides, epothilones, and FR182877 (cyclostreptin).
Journal ArticleDOI
Microtubule-targeting agents and their impact on cancer treatment.
Vladimír Čermák,Vojtěch Dostál,Michael Jelinek,Lenka Libusova,Jan Kovář,Daniel Rösel,Jan Brábek +6 more
TL;DR: In anti-metastatic therapy, MTAs should be combined with other drugs to target all modes of cancer cell invasion, and some of the novel MTAs overcome the resistance mediated by both multidrug resistance transporters as well as overexpression of specific β-tubulin types.
Journal ArticleDOI
Taxanes in cancer treatment: Activity, chemoresistance and its overcoming
TL;DR: Taxanes have been widely used as microtubule-targeting antitumor agents and have shown impact on key molecular mechanisms including disruption of mitotic spindle, mitosis slippage and inhibition of angiogenesis.
Journal ArticleDOI
Synthesis, molecular editing, and biological assessment of the potent cytotoxin leiodermatolide.
Damien Mailhol,Jens Willwacher,Nina Kausch-Busies,Elizabeith E. Rubitski,Zhanna Sobol,Maik Schuler,My-Hanh Lam,Sylvia Musto,Frank Loganzo,Andreas Maderna,Alois Fürstner +10 more
TL;DR: The acquired biodata show that 1 is a potent cytotoxin in human tumor cell proliferation assays, distinguished by GI50 values in the ≤3 nM range even for cell lines expressing the Pgp efflux transporter.
References
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Journal ArticleDOI
Personal recollections on the early development of taxol.
TL;DR: All of us who have worked with taxol in the laboratory and the clinic, and the many patients all over the world who have benefited from the drug, owe a great debt of gratitude to Monroe Wall, Mansukh Wani, and their colleagues for the initial isolation and characterization of this compound.
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Large-Scale Synthesis of the Anti-Cancer Marine Natural Product (+)-Discodermolide. Part 2: Synthesis of Fragments C1-6 and C9-14
Stuart J. Mickel,Gottfried Sedelmeier,Daniel Niederer,Friedrich Schuerch,Dominique Grimler,Guido Koch,Robert Daeffler,Adnan Osmani,Alfred Hirni,and Karl Schaer,Remo Gamboni,Andrew Bach,Apurva Chaudhary,Stephen Chen,Weichun Chen,Bin Hu,Jagoe Christopher Turchik,Hong-Yong Kim,Frederick Ray Kinder,Yugang Liu,Yansong Lu,Joseph Mckenna,Mahavir Prashad,Timothy Michael Ramsey,Oljan Repic,Larry Rogers,Wen-Chung Shieh,and Run-Ming Wang,Liladhar Murlidhar Waykole +28 more
TL;DR: In this article, the authors described a kilogram-scale synthesisation of fragments C1-6 (6) and C9-14 (4) of (+)-discodermolide from common precursor 3.
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NMR determination of the bioactive conformation of peloruside A bound to microtubules.
Jesús Jiménez-Barbero,Ángeles Canales,Peter T. Northcote,Rubén M. Buey,José Manuel Andreu,J. Fernando Díaz +5 more
TL;DR: The determination of the conformation of Peloruside A bound to biochemically stabilized microtubules is determined by using TR-NOESY NMR experiments, by docking the bioactive conformed of peloruside, which involves the alpha-tubulin monomer in contrast with taxol, which binds to the beta-monomer.
Journal ArticleDOI
Microtubules Regulate Hypoxia-inducible Factor-1α Protein Trafficking and Activity IMPLICATIONS FOR TAXANE THERAPY
TL;DR: This work shows that microtubule-targeting drug (MTD) treatment impaired HIF-1α protein nuclear translocation, which significantly down-regulated HIF transcriptional activity, and provides strong evidence that Hif-1 α protein associates with polymerized microtubules and traffics to the nucleus, with the aid of the dynein motor protein.
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Identification and characterization of an intermediate taxol binding site within microtubule nanopores and a mechanism for tubulin isotype binding selectivity.
TL;DR: In this article, the H6/H7 loop was used as a hinge hinge for paclitaxel to move directly from this intermediate binding site to its final position in the luminal binding site.
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