Recent progress with microtubule stabilizers: new compounds, binding modes and cellular activities
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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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Journal ArticleDOI
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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Total Syntheses of (+)-Zampanolide and (+)-Dactylolide Exploiting a Unified Strategy
TL;DR: The first total syntheses of (+)-zampanolide and (+)-dactylolide, members of a new class of tumor cell growth inhibitory macrolides, have been achieved.
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Class III beta-tubulin expression predicts prostate tumor aggressiveness and patient response to docetaxel-based chemotherapy.
Guillaume Ploussard,Stéphane Terry,Pascale Maillé,Yves Allory,Nanor Sirab,Laurence Kheuang,Pascale Soyeux,Nathalie Nicolaiew,Estelle Coppolani,Bernard Paule,Laurent Salomon,Stéphane Culine,Ralph Buttyan,Francis Vacherot,Alexandre de la Taille +14 more
TL;DR: A role for βIII-tubulin as candidate theranostic biomarker to predict the response to docetaxel-based chemotherapy as well as to target for treatment of docetAXel-resistant CRPC is suggested.
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Tubulin polymerizing activity of dictyostatin-1, a polyketide of marine sponge origin.
TL;DR: Results indicate that dictyostatin-1 is a potent inducer of tubulin polymerization and retains activity in cells expressing the P-glycoprotein efflux pump.
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Molecular recognition of taxol by microtubules. Kinetics and thermodynamics of binding of fluorescent taxol derivatives to an exposed site
TL;DR: The kinetic scheme and reaction rates of binding to microtubules of two fluorescent taxoids and the results indicate that the Taxol binding site is directly accessible, in contrast with its location at lumen in the current model of micro Tubules.
Journal ArticleDOI
Cyclostreptin binds covalently to microtubule pores and lumenal taxoid binding sites
Rubén M. Buey,Enrique Calvo,Isabel Barasoain,Oriol Pineda,Michael C. Edler,Ruth Matesanz,Gemma Cerezo,Christopher D. Vanderwal,Billy W. Day,Erik J. Sorensen,Juan Antonio López,José Manuel Andreu,Ernest Hamel,J. Fernando Díaz +13 more
TL;DR: The pore region of beta-tubulin is an undescribed binding site that elucidates the mechanism by which taxoid-site compounds reach the kinetically unfavorable lumenal site and explains how taxoids-site drugs induce microtubule formation from dimeric and oligomeric tubulin.
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