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
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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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High expression of class III β-tubulin predicts good response to neoadjuvant taxane and doxorubicin/cyclophosphamide-based chemotherapy in estrogen receptor-negative breast cancer.
Yihong Wang,Joseph A. Sparano,Susan Fineberg,Lesley Stead,Jaya Sunkara,Susan Band Horwitz,Hayley M. McDaid +6 more
TL;DR: In this article, the authors determined βΙΙ-tubulin expression in 85 breast cancers, including 41 localized breast cancers treated with primary surgery and 44 treated with neoadjuvant chemotherapy before surgery.
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Taccalonolide C and D, two pentacyclic steroids of Tacca plantaginea
TL;DR: Two pentacyclic steroidal bitter principles, taccalonolide C and D have been isolated from Tacca plantaginea and the structures were established by spectroscopic methods as discussed by the authors.
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(Z)-Sarcodictyin A, a New Highly Cytotoxic Diterpenoid from the Soft Coral Bellonella albiflora
TL;DR: A new cytotoxic diterpene, (Z)-sarcodictyin A, was isolated from the Japanese soft coral Bellonella albiflora and showed strong cytotoxicity against HeLa human cervix cells.
Journal ArticleDOI
Structural evidence for cooperative microtubule stabilization by Taxol and the endogenous dynamics regulator MAP4.
Hui Xiao,Hui Wang,Xue-Chun Zhang,Zongcai Tu,Chloe Bulinski,Marina Khrapunovich-Baine,Ruth Hogue Angeletti,Susan Band Horwitz +7 more
TL;DR: In this paper, the authors investigated the structural changes in the αβ-tubulin heterodimer upon binding of endogenous microtubule associated proteins (MAPs) in the presence and absence of Taxol and showed that MAP4 significantly reduced deuterium incorporation into MTs, suggesting that it stabilizes the polymer via its effects on the multiple interfaces that comprise a stable MT polymer.
Journal ArticleDOI
Dissecting paclitaxel-microtubule association: quantitative assessment of the 2'-OH group
Shubhada Sharma,Chandraiah Lagisetti,Barbara Poliks,Robert M. Coates,David G. I. Kingston,Susan Bane +5 more
TL;DR: It is proposed that the hydrogen bonding interaction between the 2'-OH group and D26 is the most important stabilizing interaction that PTX forms with tubulin in the region of the C-13 side chain.
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