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
More filters
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
More filters
Journal ArticleDOI
Characterization of the Taxol Binding Site on the Microtubule IDENTIFICATION OF Arg282 IN β-TUBULIN AS THE SITE OF PHOTOINCORPORATION OF A 7-BENZOPHENONE ANALOGUE OF TAXOL
TL;DR: Advances made by electron crystallography in understanding the structure of the tubulin dimer have allowed us to visualize the three sites of photoincorporation by molecular modeling, and there is good agreement between the binding site of Taxol in β-tubulin as determined by photoaffinity labeling and electron crystallographers.
Journal ArticleDOI
Fijianolides, polyketide heterocycles from a marine sponge
Journal ArticleDOI
The paradox of paclitaxel neurotoxicity: Mechanisms and unanswered questions.
TL;DR: Approaches taken to investigate mechanisms of paclitaxel-induced neuropathy and evidence for potential mechanisms of the axonal degeneration downstream of or distinct from microtubule stabilization by pac litaxel are reviewed.
Journal ArticleDOI
Analysis of Mitosis and Antimitotic Drug Responses in Tumors by In Vivo Microscopy and Single-Cell Pharmacodynamics
James D. Orth,Rainer H. Kohler,Floris Foijer,Peter K. Sorger,Ralph Weissleder,Timothy J. Mitchison +5 more
TL;DR: In vivo microscopy offers a useful tool to visualize mitosis during tumor progression, drug responses, and cell fate at the single-cell level and is shown to be a semiquantitative, single- cell measure of PD.
Journal ArticleDOI
The coral-derived natural products eleutherobin and sarcodictyins A and B: effects on the assembly of purified tubulin with and without microtubule-associated proteins and binding at the polymer taxoid site.
TL;DR: Tubulin assembly reactions induced by all compounds were similar to the paclitaxel-driven reactions in being enhanced by the addition of microtubule-associated proteins and/or GTP to the reaction mixture and by progressively higher reaction temperatures.
Related Papers (5)
Microtubule-binding agents: a dynamic field of cancer therapeutics
Charles Dumontet,Mary Ann Jordan +1 more