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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Microtubule Alterations Occur Early in Experimental Parkinsonism and The Microtubule Stabilizer Epothilone D Is Neuroprotective
Daniele Cartelli,Francesca Casagrande,Carla L. Busceti,Domenico Bucci,Gemma Molinaro,Anna Traficante,Daniele Passarella,Erminio Giavini,Gianni Pezzoli,Giuseppe Battaglia,Graziella Cappelletti +10 more
TL;DR: In this paper, the role of microtubule dysfunction in Parkinson's disease was examined in C57Bl mice and the effect of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) was found to precede axonal transport impairment and neurite degeneration.
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Randomized, Open-Label, Phase III Study Comparing Patupilone (EPO906) With Pegylated Liposomal Doxorubicin in Platinum-Refractory or -Resistant Patients With Recurrent Epithelial Ovarian, Primary Fallopian Tube, or Primary Peritoneal Cancer
Nicoletta Colombo,Elzbieta Kutarska,Meletios A. Dimopoulos,Duk-Soo Bae,Izabella Rzepka-Górska,Mariusz Bidziński,Giovanni Scambia,Svend Aage Engelholm,Florence Joly,Dirk Weber,Mona El-Hashimy,Jingjin Li,Farida Souami,Patricia Wing,S.A. Engelholm,Aristotelis Bamias,Peter E. Schwartz +16 more
TL;DR: Patupilone did not demonstrate significant improvement in OS compared with the active control, PLD, and no new or unexpected serious AEs were identified.
Journal ArticleDOI
A Unique Mode of Microtubule Stabilization Induced by Peloruside A
J. Torin Huzil,John K. Chik,Gordon W. Slysz,Holly Freedman,Jack A. Tuszynski,Richard E. Taylor,Dan L. Sackett,David C. Schriemer +7 more
TL;DR: It is suggested that taxoid-site ligands epothilone A and docetaxel stabilize microtubules primarily through improved longitudinal interactions centered on the interdimer interface, with no observable contributions from lateral interactions between protofilaments.
Journal ArticleDOI
Total Synthesis and Configurational Assignment of (−)‐Dictyostatin, a Microtubule‐Stabilizing Macrolide of Marine Sponge Origin
Journal ArticleDOI
The Binding Sites of Microtubule-Stabilizing Agents
TL;DR: The binding site of an MSA on tubulin is important for characterizing the compound as an anticancer agent and provides insight not only into possible synergistic interactions with other compounds but also on the MSA "pharmacophore," which can aid in the design of novel MSAs with improved properties.
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