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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A ciprofloxacin derivative with four mechanisms of action overcomes paclitaxel resistance in p53-mutant and MDR1 gene-expressing type II human endometrial cancer.
Suhaila Omar Alhaj-Suliman,Youssef W. Naguib,Emad I. Wafa,Sanjib Saha,Kareem Ebeid,Xiangbing Meng,Hamada H.H. Mohammed,Gamal El-Din A. Abuo-Rahma,Shujie Yang,Aliasger K. Salem +9 more
TL;DR: In this paper , a new ciprofloxacin derivative (CIP2b) was tested either alone or in combination with taxanes against four human endometrial cancer cell lines.
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Crosstalk between Microtubule Stabilizing Agents and Prostate Cancer
TL;DR: In this article , a review of microtubule stabilizing cytotoxic agents (MSA) for prostate cancer is presented. And the authors provide an overview of the anti-prostate cancer profiles (including preclinical and clinical studies, and clinical use) of diverse MSAs as well as the mechanism of action.
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Computational Prediction and Experimental Validation of the Unique Molecular Mode of Action of Scoulerine
TL;DR: In this article , the authors performed computational prediction and experimental validation of the mode of action of scoulerine and found the highest affinity binding sites located in both the free tubulin and in a microtubule.
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RNAseq Analysis of Novel 1,3,4-Oxadiazole Chalcogen Analogues Reveals Anti-Tubulin Properties on Cancer Cell Lines
Stefano Zoroddu,L. Sanna,Valentina Bordoni,Weidong Lyu,Gabriele Murineddu,Gérard Aimé Pinna,Sonia Vanina Forcales,Arturo Sala,David J. Kelvin,Luigi Bagella +9 more
TL;DR: In this article , the authors investigated the characterization of two new compounds named 6 and 14 on HeLa and PC-3 cancer cell lines and found that they strongly inhibited the proliferation of cancer cells by arresting them in the G2/M phase of the cell cycle.
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Challenges and opportunities for improving the druggability of natural product: Why need drug delivery system?
TL;DR: In this article , the advantages of drug delivery systems on the druggability improvement of BNPs from the perspective of their bioactive nature, discusses why BNs need drugs delivery systems, and predicts the next direction.
References
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Microtubules as a target for anticancer drugs.
Mary Ann Jordan,Leslie Wilson +1 more
TL;DR: Highly dynamic mitotic-spindle microtubules are among the most successful targets for anticancer therapy, and it is now known that at lower concentrations, microtubule-targeted drugs can suppress micro Tubule dynamics without changingmicrotubule mass; this action leads to mitotic block and apoptosis.
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Plant antitumor agents. VI. The isolation and structure of taxol, a novel antileukemic and antitumor agent from Taxus brevifolia.
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Promotion of microtubule assembly in vitro by taxol
TL;DR: It is reported here that taxol acts as a promoter of calf brain microtubule assembly in vitro, in contrast to plant products such as colchicine and podophyllotoxin, which inhibit assembly.
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Microtubule-binding agents: a dynamic field of cancer therapeutics
Charles Dumontet,Mary Ann Jordan +1 more
TL;DR: The screening of a range of botanical species and marine organisms has yielded promising new antitubulin agents with novel properties, and the three main objectives are enhanced tumour specificity, reduced neurotoxicity and insensitivity to chemoresistance mechanisms.
Journal Article
Epothilones, a New Class of Microtubule-stabilizing Agents with a Taxol-like Mechanism of Action
Daniel M. Bollag,Patricia A. McQueney,Jian Zhu,Otto D. Hensens,Lawrence R. Koupal,Jerrold M. Liesch,Michael A. Goetz,Elias Lazarides,Catherine M. Woods +8 more
TL;DR: Epothilones represent a novel structural class of compounds, the first to be described since the original discovery ofTaxol, which not only mimic the biological effects of taxol but also appear to bind to the same microtubule-binding site as taxol.
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