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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Distinct Pose of Discodermolide in Taxol Binding Pocket Drives a Complementary Mode of Microtubule Stabilization
Marina Khrapunovich-Baine,Vilas Menon,Pascal Verdier-Pinard,Amos B. Smith,Ruth Hogue Angeletti,Andras Fiser,Susan Band Horwitz,Hui Xiao +7 more
TL;DR: Hydrogen-deuterium exchange is applied to determine the binding mode and the conformational effects on chicken erythrocyte tubulin of another MSA, discodermolide, whose synthetic analogues may have potential use in the clinic and indicate complementary stabilizing effects of Taxol and discodernolide on the microtubules, which may explain the synergy observed between the two drugs in vivo.
Journal ArticleDOI
Laulimalide and synthetic laulimalide analogues are synergistic with paclitaxel and 2-methoxyestradiol.
TL;DR: The results show that the laulimalides together with other tubulin-binding antimitotic agents provide synergistic antiproliferative actions, and suggest that specific combinations of microtubule-targeting agents should be considered for clinical utilities as they have excellent potential to improve clinical response.
Journal ArticleDOI
Total synthesis of (-)-zampanolide and structure-activity relationship studies on (-)-dactylolide derivatives.
Didier Zurwerra,Florian Glaus,Leo Betschart,Julia K. Schuster,Jürg Gertsch,Walter Ganci,Karl-Heinz Altmann +6 more
TL;DR: Synthetic 1 inhibited human cancer cell growth in vitro with nM IC(50) values, while ent-2, which lacks the diene-containing hemiaminal-linked side chain of 1, is 25- to 260-fold less active.
Journal ArticleDOI
Conformations of Laulimalide in DMSO-d6
Pahk Thepchatri,Daniel O. Cicero,Edith Monteagudo,Arun K. Ghosh,Ben Cornett,Eric R. Weeks,James P. Snyder +6 more
TL;DR: 15 laulimalide conformations that can be classified into 5 different families: Supine, Convex, Cobra, Stretch, and Concave motifs are identified.
Journal ArticleDOI
Identification and Biological Activities of New Taccalonolide Microtubule Stabilizers
Jiangnan Peng,April L. Risinger,Gary A. Fest,Evelyn M. Jackson,Gregory L. Helms,Lisa Polin,Susan L. Mooberry +6 more
TL;DR: In vivo antitumor evaluations of taccalonolides A, E, and N show that each of these molecules has in vivo antitUMor activity.
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