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.
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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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Cellular studies reveal mechanistic differences between taccalonolide A and paclitaxel
TL;DR: The propensity of taccalonolide A to alter interphase microtubules at antiproliferative concentrations as well as its high degree of cellular persistence may explain why tacconolide B is more potent in vivo than would be expected from cellular studies.
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Mariculture and Natural Production of the Antitumoural (+)-Discodermolide by the Caribbean Marine Sponge Discodermia dissoluta
TL;DR: In situ, 6-month fragment culture trials were performed to assess the performance of the Caribbean marine sponge Discodermia dissoluta in terms of growth and additional discodermolide production and studied possible factors that influence the variability of discoderolide concentrations in the wild.
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Biological and phytochemical evaluation of plants XI: Isolation of aspidospermine, quebrachidine, rhazinilam, (—)‐pyrifolidine, and akuammidine from Aspidosperma quebracho‐blanco (apocynaceae)
TL;DR: A phytochemical investigation of the leaves of Aspidosperma quebracho-blanco (Apocynaceae) resulted in the isolation of rhazinilam, a new nonindole lactam alkaloid, in addition to the known bases, aspidos permine, quebrachidine, (—)-pyrifolidine, and akuammidine.
Journal ArticleDOI
Mutations in the β-tubulin binding site for peloruside A confer resistance by targeting a cleft significant in side chain binding.
Adrian Begaye,Shana Trostel,Zhiming Zhao,Richard E. Taylor,David C. Schriemer,Dan L. Sackett +5 more
TL;DR: Four resistant lines of the human ovarian carcinoma cell line A2780(1A9) are described with single-base mutations in class I β-tubulin that result in the following substitutions: R306H, Y340S, N337D, and A296S in various combinations.
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Probing the Pore Drug Binding Site of Microtubules with Fluorescent Taxanes: Evidence of Two Binding Poses
Isabel Barasoain,Ana M. García-Carril,Ruth Matesanz,Giorgio Maccari,Chiara Trigili,Mattia Mori,Jing-Zhe Shi,Wei-Shuo Fang,José Manuel Andreu,Maurizio Botta,J. Fernando Díaz +10 more
TL;DR: Analysis of the phases indicates that two different binding sites are detected, reflecting two different modes of binding, which could arise from different arrangements of the taxane or fluorescein moieties in the pore.
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