ArticleProceedings of the National Academy of Sciences of the United States of America2021
Gatorbulin-1, a distinct cyclodepsipeptide chemotype, targets a seventh tubulin pharmacological site.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 46 papers.
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Who cites it
46 citing papers in PubMed, 87 citations in OpenAlex.
- PM534, a Novel Colchicine Site Tubulin Inhibitor with Broad-Spectrum and Resistance-Overcoming Antitumor Activity.Molecular cancer therapeutics · 2026Article
- Illuminating microtubule functions with small molecules: past, present and future of fluorescent tubulin-binding probes.RSC chemical biology · 2026Review
- Harnessing engineered cyanobacteria for next-generation therapeutics.Archives of microbiology · 2026Review
- Green genes from blue greens: challenges and solutions to unlocking the potential of cyanobacteria in drug discovery.Natural product reports · 2026Review
- Discovery of Peptide-Based Tubulin Inhibitors Through Structure-Guided Design.Pharmaceutics · 2026Article
- The Impact of Combretastatin A-4 on Cancer Cells and Circulating Tumor Cells (CTCs): A Multi-Assay Approach.Oncology research · 2026Article
- Characterization of the Tychonamide Biosynthetic Pathway in the Recently Described Cyanobacterial SpeciesACS chemical biology · 2025Article
- Article
- Structure based drug design and machine learning approaches for identifying natural inhibitors against the human αβIII tubulin isotype.Scientific reports · 2025Article
- Recent Advances in Microtubule Targeting Agents for Cancer Therapy.Molecules (Basel, Switzerland) · 2025Review
- Microtubule-Targeting Agents: Advances in Tubulin Binding and Small Molecule Therapy for Gliomas and Neurodegenerative Diseases.International journal of molecular sciences · 2025Review
- In Silico Design and Analysis of Cyanobacterial Pseudo Natural Products.Journal of natural products · 2025Article
- Discovery and biological profile of pyridachlometyl.Pest management science · 2025Review
- Identification of therapeutic targets for chronic kidney disease through Mendelian randomization analysis of druggable genes.Scientific reports · 2025Article
- Identification of a ligand-binding site on tubulin mediating the tubulin-RB3 interaction.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Chemical diversity of cyanobacterial natural products.Natural product reports · 2025Review
- Computational discovery of potential therapeutic agents against brain-eating amoeba (Naegleria fowleri).PloS one · 2025Article
- Design, synthesis, and bioevaluation of 1Journal of enzyme inhibition and medicinal chemistry · 2024Article
- Synthesis,RSC medicinal chemistry · 2024Article
- Globospiramine fromCells · 2024Article
Corrections and comments
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Authors and funding
14 authors at 6 institutions in 4 countries.
Funding
Abstract
Tubulin-targeted chemotherapy has proven to be a successful and wide spectrum strategy against solid and liquid malignancies. Therefore, new ways to modulate this essential protein could lead to new antitumoral pharmacological approaches. Currently known tubulin agents bind to six distinct sites at α/β-tubulin either promoting microtubule stabilization or depolymerization. We have discovered a seventh binding site at the tubulin intradimer interface where a novel microtubule-destabilizing cyclodepsipeptide, termed gatorbulin-1 (GB1), binds. GB1 has a unique chemotype produced by a marine cyanobacterium. We have elucidated this dual, chemical and mechanistic, novelty through multidimensional characterization, starting with bioactivity-guided natural product isolation and multinuclei NMR-based structure determination, revealing the modified pentapeptide with a functionally critical hydroxamate group; and validation by total synthesis. We have investigated the pharmacology using isogenic cancer cell screening, cellular profiling, and complementary phenotypic assays, and unveiled the underlying molecular mechanism by in vitro biochemical studies and high-resolution structural determination of the α/β-tubulin-GB1 complex.
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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.