ArticleJournal of chemical information and modeling2011
Interactions of halichondrin B and eribulin with tubulin.
Article in Journal of chemical information and modeling, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 58 citations in OpenAlex.
- Epithelial-mesenchymal dynamics in cancer: Role of signalling pathways, stromal interactions and natural therapies.ADMET & DMPK · 2025Review
- The interaction of spongistatin 1 with tubulin.Archives of biochemistry and biophysics · 2022Article
- Interaction of diazonamide A with tubulin.Archives of biochemistry and biophysics · 2020Article
- Oncolytic Vaccinia Virus ExpressingMarine drugs · 2019Article
- Selectively high efficacy of eribulin against high-grade invasive recurrent and/or metastatic squamous cell carcinoma of the head and neck.Oncology letters · 2019Article
- Managing sarcoma: where have we come from and where are we going?Therapeutic advances in medical oncology · 2017Review
- Eribulin alone or in combination with the PLK1 inhibitor BI 6727 triggers intrinsic apoptosis in Ewing sarcoma cell lines.Oncotarget · 2017Article
- HMBA is a putative HSP70 activator stimulating HEXIM1 expression that is down-regulated by estrogen.The Journal of steroid biochemistry and molecular biology · 2017Article
- Complementary isonitrile-based multicomponent reactions for the synthesis of diversified cytotoxic hemiasterlin analogues.Organic & biomolecular chemistry · 2015Article
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- Eribulin mesylate: mechanism of action of a unique microtubule-targeting agent.Clinical cancer research : an official journal of the American Association for Cancer Research · 2015Review
- The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.Bioorganic & medicinal chemistry · 2015Article
- A novel natural phenyl alkene with cytotoxic activity.Tetrahedron letters · 2013Article
- Effects of eribulin, vincristine, paclitaxel and ixabepilone on fast axonal transport and kinesin-1 driven microtubule gliding: implications for chemotherapy-induced peripheral neuropathy.Neurotoxicology · 2013Article
- Article
- Cytotoxicity and glycan-binding properties of an 18 kDa lectin isolated from the marine sponge Halichondria okadai.Toxins · 2012Article
- Evading Pgp activity in drug-resistant cancer cells: a structural and functional study of antitubulin furan metotica compounds.Molecular cancer therapeutics · 2012Article
- Natural products as sources of new drugs over the 30 years from 1981 to 2010.Journal of natural products · 2012Review
- Antineoplastic agents. 592. Highly effective cancer cell growth inhibitory structural modifications of dolastatin 10.Journal of natural products · 2011Article
Corrections and comments
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Authors and funding
9 authors at 5 institutions in 2 countries.
Funding
Abstract
Compounds that modulate microtubule dynamics include highly effective anticancer drugs, leading to continuing efforts to identify new agents and improve the activity of established ones. Here, we demonstrate that [(3)H]-labeled halichondrin B (HB), a complex, sponge-derived natural product, is bound to and dissociated from tubulin rapidly at one binding site per αβ-heterodimer, with an apparent K(d) of 0.31 μM. We found no HB-induced aggregation of tubulin by high-performance liquid chromatography, even following column equilibration with HB. Binding of [(3)H]HB was competitively inhibited by a newly approved clinical agent, the truncated HB analogue eribulin (apparent K(i), 0.80 μM) and noncompetitively by dolastatin 10 and vincristine (apparent K(i)'s, 0.35 and 5.4 μM, respectively). Our earlier studies demonstrated that HB inhibits nucleotide exchange on β-tubulin, and this, together with the results presented here, indicated the HB site is located on β-tubulin. Using molecular dynamics simulations, we determined complementary conformations of HB and β-tubulin that delineated in atomic detail binding interactions of HB with only β-tubulin, with no involvement of the α-subunit in the binding interaction. Moreover, the HB model served as a template for an eribulin binding model that furthered our understanding of the properties of eribulin as a drug. Overall, these results established a mechanistic basis for the antimitotic activity of the halichondrin class of compounds.
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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.