ArticleJournal of natural products2019
Identification of C-6 as a New Site for Linker Conjugation to the Taccalonolide Microtubule Stabilizers.
Article in Journal of natural products, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 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
7 citing papers in PubMed, 13 citations in OpenAlex.
- Illuminating microtubule functions with small molecules: past, present and future of fluorescent tubulin-binding probes.RSC chemical biology · 2026Review
- Taccalonolides: Structure, semi-synthesis, and biological activity.Frontiers in pharmacology · 2022Review
- Review
- Elucidating target specificity of the taccalonolide covalent microtubule stabilizers employing a combinatorial chemical approach.Nature communications · 2020Article
- Taccalonolide Microtubule Stabilizers.Progress in the chemistry of organic natural products · 2020Review
- MAP7 promotes migration and invasion and progression of human cervical cancer through modulating the autophagy.Cancer cell international · 2020Article
- Unravelling the covalent binding of zampanolide and taccalonolide AJ to a minimalist representation of a human microtubule.Journal of computer-aided molecular design · 2019Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
The taccalonolides are a class of microtubule stabilizers that circumvent clinically relevant forms of drug resistance due to their unique mechanism of microtubule stabilization imparted by the covalent binding of the C-22-C-23 epoxide moiety to tubulin. A taccalonolide (8) with a fluorescein group attached with a linker at C-6 was generated, and biochemical and cell-based assays showed that it bound directly to tubulin and stabilized microtubules. This pharmacological probe has allowed, for the first time, a direct visualization of a taccalonolide binding to microtubules, verifying their cellular binding site. This C-6-modified taccalonolide showed potency comparable to the untagged compound in biochemical experiments; however, its potency was lower in cellular assays, presumably due to decreased cellular permeability. These studies provide a valuable tool to facilitate the further understanding of taccalonolide pharmacology and demonstrate that C-6 is a promising site for a linker to be added to this novel class of microtubule stabilizers for targeted drug delivery.
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Registered trials
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.