ArticleCells2020
Tubulin Resists Degradation by Cereblon-Recruiting PROTACs.
Article in Cells, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 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.
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Who cites it
9 citing papers in PubMed, 34 citations in OpenAlex.
- Tubulin autoregulation tunes microtubule dynamics to support multicellular architecture and viability.Nature communications · 2026Article
- Tipping the balance: synthesis and evaluation of centrinone-based degraders of polo-like kinase 4.RSC chemical biology · 2026Article
- An overview of PROTACs: a promising drug discovery paradigm.Molecular biomedicine · 2022Review
- Recent Approaches to the Identification of Novel Microtubule-Targeting Agents.Frontiers in molecular biosciences · 2022Review
- The PROTACtable genome.Nature reviews. Drug discovery · 2021Review
- PROTACs to address the challenges facing small molecule inhibitors.European journal of medicinal chemistry · 2021Review
- Tackling Drug Resistance in EGFR Exon 20 Insertion Mutant Lung Cancer.Pharmacogenomics and personalized medicine · 2021Review
- Article
- Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library.ACS chemical biology · 2020Article
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
Dysregulation of microtubules and tubulin homeostasis has been linked to developmental disorders, neurodegenerative diseases, and cancer. In general, both microtubule-stabilizing and destabilizing agents have been powerful tools for studies of microtubule cytoskeleton and as clinical agents in oncology. However, many cancers develop resistance to these agents, limiting their utility. We sought to address this by developing a different kind of agent: tubulin-targeted small molecule degraders. Degraders (also known as proteolysis-targeting chimeras (PROTACs)) are compounds that recruit endogenous E3 ligases to a target of interest, resulting in the target's degradation. We developed and examined several series of α- and β-tubulin degraders, based on microtubule-destabilizing agents. Our results indicate, that although previously reported covalent tubulin binders led to tubulin degradation, in our hands, cereblon-recruiting PROTACs were not efficient. In summary, while we consider tubulin degraders to be valuable tools for studying the biology of tubulin homeostasis, it remains to be seen whether the PROTAC strategy can be applied to this target of high clinical relevance.
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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.