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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Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology.
TL;DR: Bifunctional compounds in which one component is a lead compound or a drug, and chemical features of chimeric molecules and their use for targeted delivery and for target engagement studies are discussed.
Journal ArticleDOI
Synthesis and Bioevaluation of 3,6-Diaryl-[1,2,4]triazolo[4,3-b] Pyridazines as Antitubulin Agents
Qile Xu,Wang Yueting,Jingwen Xu,Maolin Sun,Haiqiu Tian,Daiying Zuo,Qi Guan,Kai Bao,Yingliang Wu,Weige Zhang +9 more
TL;DR: The compound 4q with a 3-amino-4-methoxyphenyl moiety as the B-ring displayed the highly active antiproliferative activity against SGC-7901, A549, and HT-1080 cell lines with IC50 values of 0.014, 0.008, and 0.012 μM, respectively.
Journal ArticleDOI
Regulation of E-cadherin localization by microtubule targeting agents: rapid promotion of cortical E-cadherin through p130Cas/Src inhibition by eribulin.
TL;DR: The results suggest that microtubules can be actively co-opted by cancer cells to inhibit cortical E-cadherin localization, a hallmark of EMT, and provide a direct link between the initial disruption of the microtubule network and reversal of E MT phenotypes demonstrated by eribulin in long-term studies.
Journal ArticleDOI
Design and synthesis of (2-(phenylamino)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone analogues as potent anti-tubulin polymerization agents.
TL;DR: The results demonstrated that 14 is a potent anti-tubulin agent with strong concentration dependent effect of inhibition of colony formation, induction of G2/M arrest and induction of apoptosis through mitochondrial pathway.
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Overview of the optimal perioperative intraperitoneal chemotherapy regimens used in current clinical practice.
TL;DR: The combination of CRS and intraperitoneal (IP) chemotherapy should now be considered standard of care for PSM from appendiceal epithelial cancers, colorectal cancer and peritoneal mesothelioma.
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.
Journal ArticleDOI
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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