ArticleChembiochem : a European journal of chemical biology2017
Structural Basis of Microtubule Stabilization by Discodermolide.
Article in Chembiochem : a European journal of chemical biology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed.
- Taxane-induced conformational changes in the microtubule lattice activate GEF-H1-dependent RhoA signalling.Nature cell biology · 2026Article
- Natural Products Beyond Inhibition: A Mechanistic Framework Spanning Pockets, Interfaces, and Kinetic Barriers.Molecules (Basel, Switzerland) · 2026Review
- Illuminating microtubule functions with small molecules: past, present and future of fluorescent tubulin-binding probes.RSC chemical biology · 2026Review
- Synthesis of Epoxyoxirenes: Phytotoxic Activity and Enzymatic Target Identification.Plants (Basel, Switzerland) · 2025Article
- Exploring tubulin-paclitaxel binding modes through extensive molecular dynamics simulations.Scientific reports · 2025Article
- First total synthesis, antitumor evaluation and target identification of mornaphthoate E: A new tubulin inhibitor template acting on PI3K/Akt signaling pathway.Acta pharmaceutica Sinica. B · 2024Article
- Structural basis of microtubule depolymerization by the kinesin-like activity of HIV-1 Rev.Structure (London, England : 1993) · 2023Article
- Article
- Computational Approaches to the Rational Design of Tubulin-Targeting Agents.Biomolecules · 2023Review
- The tubulin database: Linking mutations, modifications, ligands and local interactions.PloS one · 2023Article
- Utilization of Photoaffinity Labeling to Investigate Binding of Microtubule Stabilizing Agents to P-Glycoprotein and β-Tubulin.Journal of natural products · 2022Review
- Structural Refinement of the Tubulin Ligand (+)-Discodermolide to Attenuate Chemotherapy-Mediated Senescence.Molecular pharmacology · 2020Article
- Targeting and extending the eukaryotic druggable genome with natural products: cytoskeletal targets of natural products.Natural product reports · 2020Review
- Taxanes convert regions of perturbed microtubule growth into rescue sites.Nature materials · 2020Article
- Revisiting microtubule targeting agents: α-Tubulin and the pironetin binding site as unexplored targets for cancer therapeutics.Bioorganic & medicinal chemistry letters · 2019Review
- Unravelling the covalent binding of zampanolide and taccalonolide AJ to a minimalist representation of a human microtubule.Journal of computer-aided molecular design · 2019Article
- Crystal Structure of the Cyclostreptin-Tubulin Adduct: Implications for Tubulin Activation by Taxane-Site Ligands.International journal of molecular sciences · 2019Article
- Computationally Assisted Discovery and Assignment of a Highly Strained and PANC-1 Selective Alkaloid from Alaska's Deep Ocean.Journal of the American Chemical Society · 2019Article
- Computational Prediction of the Mode of Binding of Antitumor Lankacidin C to Tubulin.ACS omega · 2019Article
- Improved Dose-Response Relationship of (+)-Discodermolide-Taxol Hybrid Congeners.Journal of natural products · 2018Article
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Authors and funding
10 authors.
Funding
Abstract
Microtubule-stabilizing agents (MSAs) are widely used in chemotherapy. Using X-ray crystallography we elucidated the detailed binding modes of two potent MSAs, (+)-discodermolide (DDM) and the DDM-paclitaxel hybrid KS-1-199-32, in the taxane pocket of β-tubulin. The two compounds bind in a very similar hairpin conformation, as previously observed in solution. However, they stabilize the M-loop of β-tubulin differently: KS-1-199-32 induces an M-loop helical conformation that is not observed for DDM. In the context of the microtubule structure, both MSAs connect the β-tubulin helices H6 and H7 and loop S9-S10 with the M-loop. This is similar to the structural effects elicited by epothilone A, but distinct from paclitaxel. Together, our data reveal differential binding mechanisms of DDM and KS-1-199-32 on tubulin.
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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.