ArticleNature communications2017
Mechanism of microtubule stabilization by taccalonolide AJ.
Article in Nature communications, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
35 citing papers in PubMed, 71 citations in OpenAlex.
- Taccalonolide AJ uncouples tubulin GTP hydrolysis from microtubule depolymerization.bioRxiv : the preprint server for biology · 2026Article
- Elucidating the Covalent Binding of Ottelione A and Withaferin A at the Colchicine Site of β‑Tubulin.ACS omega · 2026Article
- Tetrahedral framework nucleic acids: Nanokeys unlocking a new era of precision biomedicine.Journal of advanced research · 2026Review
- Illuminating microtubule functions with small molecules: past, present and future of fluorescent tubulin-binding probes.RSC chemical biology · 2026Review
- Design and synthesis of novel 4-aryl-2-benzoyl-imidazoles as colchicine binding site inhibitors.European journal of medicinal chemistry · 2025Article
- Pharmacokinetic and Biodistribution Studies of [ACS medicinal chemistry letters · 2025Article
- Review
- Design, Synthesis, and Biological Evaluation of Pyrimidine Dihydroquinoxalinone Derivatives as Tubulin Colchicine Site-Binding Agents That Displayed Potent Anticancer Activity Both In Vitro and In Vivo.ACS pharmacology & translational science · 2023Article
- Measuring the linear viscoelastic regime of MCF-7 cells with a monolayer rheometer in the presence of microtubule-active anti-cancer drugs at high concentrations.Interface focus · 2022Article
- In Vivo Evaluation of (-)-Zampanolide Demonstrates Potent and Persistent Antitumor Efficacy When Targeted to the Tumor Site.Molecules (Basel, Switzerland) · 2022Article
- Multistage pH-responsive codelivery liposomal platform for synergistic cancer therapy.Journal of nanobiotechnology · 2022Article
- Taccalonolides: Structure, semi-synthesis, and biological activity.Frontiers in pharmacology · 2022Review
- X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor.Journal of medicinal chemistry · 2021Article
- Design, Synthesis, and Biological Evaluation of Stable Colchicine-Binding Site Tubulin Inhibitors 6-Aryl-2-benzoyl-pyridines as Potential Anticancer Agents.Journal of medicinal chemistry · 2021Article
- Efficacy of a Covalent Microtubule Stabilizer in Taxane-Resistant Ovarian Cancer Models.Molecules (Basel, Switzerland) · 2021Article
- Taccalonolide C-6 Analogues, Including Paclitaxel Hybrids, Demonstrate Improved Microtubule Polymerizing Activities.Journal of natural products · 2021Article
- Review
- Synthesis and Biological Evaluations of Electrophilic Steroids Inspired by the Taccalonolides.ACS medicinal chemistry letters · 2020Article
- Development of Taccalonolide AJ-Hydroxypropyl-β-Cyclodextrin Inclusion Complexes for Treatment of Clear Cell Renal-Cell Carcinoma.Molecules (Basel, Switzerland) · 2020Article
- Viriditoxin Stabilizes Microtubule Polymers in SK-OV-3 Cells and Exhibits Antimitotic and Antimetastatic Potential.Marine drugs · 2020Article
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
As a major component of the cytoskeleton, microtubules consist of αβ-tubulin heterodimers and have been recognized as attractive targets for cancer chemotherapy. Microtubule-stabilizing agents (MSAs) promote polymerization of tubulin and stabilize the polymer, preventing depolymerization. The molecular mechanisms by which MSAs stabilize microtubules remain elusive. Here we report a 2.05 Å crystal structure of tubulin complexed with taccalonolide AJ, a newly identified taxane-site MSA. Taccalonolide AJ covalently binds to β-tubulin D226. On AJ binding, the M-loop undergoes a conformational shift to facilitate tubulin polymerization. In this tubulin-AJ complex, the E-site of tubulin is occupied by GTP rather than GDP. Biochemical analyses confirm that AJ inhibits the hydrolysis of the E-site GTP. Thus, we propose that the β-tubulin E-site is locked into a GTP-preferred status by AJ binding. Our results provide experimental evidence for the connection between MSA binding and tubulin nucleotide state, and will help design new MSAs to overcome taxane resistance.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.