ArticleThe Journal of biological chemistry2019
Covalent modification of Cys-239 in β-tubulin by small molecules as a strategy to promote tubulin heterodimer degradation.
Article in The Journal of biological chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
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Who cites it
20 citing papers in PubMed, 47 citations in OpenAlex.
- Elucidating the Covalent Binding of Ottelione A and Withaferin A at the Colchicine Site of β‑Tubulin.ACS omega · 2026Article
- Tubulin autoregulation tunes microtubule dynamics to support multicellular architecture and viability.Nature communications · 2026Article
- Global Proteomics Investigation of SAMT-247 Targets: An Antiviral Thioester that Acetylates Zinc Finger Proteins.bioRxiv : the preprint server for biology · 2026Article
- 2'-Nitroflavone targets PARP1 and alters cytoskeleton to inhibit triple-negative breast cancer progression.Scientific reports · 2026Article
- Leveraging Tubulin Isotype Structural Differences to Design Less Hematotoxic β5 Selective Covalent Inhibitors for NSCLC.Current topics in medicinal chemistry · 2026Article
- Isothiocyanates as Tubulin Polymerization Inhibitors-Synthesis and Structure-Activity Relationship Studies.International journal of molecular sciences · 2023Article
- 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
- LWJ-M30, a conjugate of DM1 and B6, for the targeted therapy of colorectal cancer with improved therapeutic effects.RSC advances · 2023Article
- Colchicine-Binding Site Agent CH-2-77 as a Potent Tubulin Inhibitor Suppressing Triple-Negative Breast Cancer.Molecular cancer therapeutics · 2022Article
- Eribulin prolongs survival in an orthotopic xenograft mouse model of malignant meningioma.Cancer science · 2022Article
- Possible Roles of Specific Amino Acids in β-Tubulin Isotypes in the Growth and Maintenance of Neurons: Novel Insights From Cephalopod Mollusks.Frontiers in molecular neuroscience · 2022Article
- Recent Approaches to the Identification of Novel Microtubule-Targeting Agents.Frontiers in molecular biosciences · 2022Review
- The PROTACtable genome.Nature reviews. Drug discovery · 2021Review
- Cevipabulin-tubulin complex reveals a novel agent binding site on α-tubulin with tubulin degradation effect.Science advances · 2021Article
- Covalent Modification of Proteins by Plant-Derived Natural Products: Proteomic Approaches and Biological Impacts.Proteomics · 2021Review
- PROTACs to address the challenges facing small molecule inhibitors.European journal of medicinal chemistry · 2021Review
- A Multipronged Approach Establishes Covalent Modification of β-Tubulin as the Mode of Action of Benzamide Anti-cancer Toxins.Journal of medicinal chemistry · 2020Article
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- Synthesis of the Novel Covalent Cysteine Proteases Inhibitor with Iodoacetic Functional Group.Molecules (Basel, Switzerland) · 2020Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Clinical microtubule-targeting drugs are functionally divided into microtubule-destabilizing and microtubule-stabilizing agents. Drugs from both classes achieve microtubule inhibition by binding different sites on tubulin and inhibiting or promoting polymerization with no concomitant effects on the protein levels of tubulin heterodimers. Here, we have identified a series of small molecules with diverse structures potentially representing a third class of novel tubulin inhibitors that promote degradation by covalent binding to Cys-239 of β-tubulin. The small molecules highlighted in this study include T0070907 (a peroxisome proliferator-activated receptor γ inhibitor), T007-1 (a T0070907 derivative), T138067,
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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.