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
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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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Effects of Paclitaxel on EGFR Endocytic Trafficking Revealed Using Quantum Dot Tracking in Single Cells
TL;DR: The present study may shed light on the mechanism of the effect of PTX on the treatment of lung cancer by labeling quantum dots to the epidermal growth factor and tracking the endocytosis and post-endocytic trafficking of EGF receptors in A549 cells for a long time interval.
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Peloruside B, A Potent Antitumor Macrolide from the New Zealand Marine Sponge Mycale hentscheli: Isolation, Structure, Total Synthesis, and Bioactivity
A. Jonathan Singh,Chun-Xiao Xu,Xiao Ming Xu,Lyndon M. West,Anja Wilmes,Ariane Chan,Ernest Hamel,John H. Miller,Peter T. Northcote,Arun K. Ghosh +9 more
TL;DR: NMR-directed isolation, structure elucidation, structure confirmation by total synthesis, and bioactivity of peloruside B are described in this article.
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A Formal Total Synthesis of Eleutherobin Using the Ring‐Closing Metathesis (RCM) Reaction of a Densely Functionalized Diene as the Key Step: Investigation of the Unusual Kinetically Controlled RCM Stereochemistry
Damiano Castoldi,Lorenzo Caggiano,Lorenzo Caggiano,Laura Panigada,Ofer Sharon,Anna M. Costa,Cesare Gennari +6 more
TL;DR: A detailed investigation of this unusual cyclization stereochemistry by computational methods has shown that the E isomer of the ten-membered carbocycle is indeed less thermodynamically stable than the corresponding Z isomer, and the selectivity is believed to be due to the dense functionality around the ruthenacyclobutane intermediate.
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Total Synthesis of Laulimalide: Synthesis of the Northern and Southern Fragments
TL;DR: The retrosynthetic analysis envisioned a novel macrocyclization route to the natural product by using a Ru-catalyzed alkene-alkyne coupling to form the dihydropyran ring from a diyne precursor, which proved to be selective for the formation of a six-membered ring.
Journal ArticleDOI
Tubulin-β-III overexpression by uterine serous carcinomas is a marker for poor overall survival after platinum/taxane chemotherapy and sensitivity to epothilones
Dana M. Roque,Stefania Bellone,Diana P. English,Natalia Buza,Emiliano Cocco,Sara Gasparrini,Ileana Bortolomai,Elena Ratner,Dan-Arin Silasi,Masoud Azodi,Thomas J. Rutherford,Peter E. Schwartz,Alessandro D. Santin +12 more
TL;DR: Relationships are clarified, in USCs relative to ovarian serous carcinomas (OSCs), between tubulin‐β‐III and p‐glycoprotein expression, clinical outcome, and in vitro chemoresponsiveness to epothilone B, ixabepilone, and paclitaxel.
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