ArticleNature communications2018
A fluorescence anisotropy assay to discover and characterize ligands targeting the maytansine site of tubulin.
Article in Nature communications, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 52 citations in OpenAlex.
- Eukaryotic-like microtubules and dynamic instability of Asgard archaeal tubulins.Science advances · 2026Article
- Illuminating microtubule functions with small molecules: past, present and future of fluorescent tubulin-binding probes.RSC chemical biology · 2026Review
- Development of a Stereoselective Synthesis of Isomers of (+)-Disorazole Z1's Lateral Chain.The Journal of organic chemistry · 2025Article
- Synthesis of a Non-Symmetrical Disorazole CMolecules (Basel, Switzerland) · 2024Article
- Discovery of potent tubulin inhibitors targeting the colchicine binding site via structure-based lead optimization and antitumor evaluation.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- The Disorazole Z Family of Highly Potent Anticancer Natural Products from Sorangium cellulosum: Structure, Bioactivity, Biosynthesis, and Heterologous Expression.Microbiology spectrum · 2023Article
- Computational Approaches to the Rational Design of Tubulin-Targeting Agents.Biomolecules · 2023Review
- Synthesis and Biological Evaluation of C(13)/C(13')-Bis(desmethyl)disorazole Z.Angewandte Chemie (International ed. in English) · 2023Article
- Quantification of Engagement of Microtubules by Small Molecules in Living Cells by Flow Cytometry.ACS bio & med chem Au · 2022Article
- Maytansinol Derivatives: Side Reactions as a Chance for New Tubulin Binders.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- Engineering ofFrontiers in microbiology · 2022Article
- Development and Evaluation of Competitive Inhibitors of Trastuzumab-HER2 Binding to Bypass the Binding-Site Barrier.Frontiers in pharmacology · 2022Article
- Gatorbulin-1, a distinct cyclodepsipeptide chemotype, targets a seventh tubulin pharmacological site.Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- New Class of Betulinic Acid-Based Nanoassemblies of Cabazitaxel, Podophyllotoxin, and Thiocolchicine.ACS medicinal chemistry letters · 2020Article
- Targeting and extending the eukaryotic druggable genome with natural products: cytoskeletal targets of natural products.Natural product reports · 2020Review
- Linear Extrapolation of the Analyte-Specific Light Scattering and Fluorescence Depolarization in Turbid Samples.ACS omega · 2019Article
- Synthesis, Microtubule-Binding Affinity, and Antiproliferative Activity of New Epothilone Analogs and of an EGFR-Targeted Epothilone-Peptide Conjugate.International journal of molecular sciences · 2019Article
Corrections and comments
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Authors and funding
11 authors at 6 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Microtubule-targeting agents (MTAs) like taxol and vinblastine are among the most successful chemotherapeutic drugs against cancer. Here, we describe a fluorescence anisotropy-based assay that specifically probes for ligands targeting the recently discovered maytansine site of tubulin. Using this assay, we have determined the dissociation constants of known maytansine site ligands, including the pharmacologically active degradation product of the clinical antibody-drug conjugate trastuzumab emtansine. In addition, we discovered that the two natural products spongistatin-1 and disorazole Z with established cellular potency bind to the maytansine site on β-tubulin. The high-resolution crystal structures of spongistatin-1 and disorazole Z in complex with tubulin allowed the definition of an additional sub-site adjacent to the pocket shared by all maytansine-site ligands, which could be exploitable as a distinct, separate target site for small molecules. Our study provides a basis for the discovery and development of next-generation MTAs for the treatment of cancer.
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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.