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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Discodermolide: a new bioactive polyhydroxylated lactone from the marine sponge Discodermia dissoluta
TL;DR: A new polyhydroxylated lactone, discodermolide (1), was isolated from a Caribbean marine sponge, Discodermia dissoluta, and its structure was elucidated through a combination of spectroscopic techniques, in particular NMR spectroscopy, and verified by X-ray crystallographic analysis.
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The Microtubule-Stabilizing Agent, Epothilone D, Reduces Axonal Dysfunction, Neurotoxicity, Cognitive Deficits, and Alzheimer-Like Pathology in an Interventional Study with Aged Tau Transgenic Mice
Bin Zhang,Jenna C. Carroll,John Q. Trojanowski,Yuemang Yao,Michiyo Iba,Justin S. Potuzak,Anne-Marie L. Hogan,Sharon X. Xie,Carlo Ballatore,Amos B. Smith,Virginia M.-Y. Lee,Kurt R. Brunden +11 more
TL;DR: Data reveal that brain-penetrant MT-stabilizing drugs hold promise for the treatment of AD and related tauopathies, and that EpoD could be a candidate for clinical testing.
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Tubulin-targeting chemotherapy impairs androgen receptor activity in prostate cancer.
TL;DR: It is shown that in addition to blocking cell division, docetaxel impairs AR signaling, evidence that enables new insights into the therapeutic efficacy of microtubule-targeting drugs in prostate cancer.
Journal ArticleDOI
Camptothecin and taxol: discovery to clinic
TL;DR: Camptothecin (CPT) is a pentacyclic alkaloid isolated from wood and bark of Camptotheca acuminata that was found to be highly active in a number of mouse in vivo cancer assays and found to uniquely inhibit an enzyme, topoisomerase I, which is involved in DNA replication.
Journal Article
Laulimalide and Isolaulimalide, New Paclitaxel-Like Microtubule-Stabilizing Agents
TL;DR: Laulimalides and isolaulimalide represent a new class of microtubule-stabilizing agents with activities that may provide therapeutic utility and, although less potent than paclitaxel, it was more effective.
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