ArticleScience translational medicine2016
The synthetic diazonamide DZ-2384 has distinct effects on microtubule curvature and dynamics without neurotoxicity.
Article in Science translational medicine, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 21 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
21 citing papers in PubMed, 49 citations in OpenAlex.
- Measurements of neurite extension and nucleokinesis in an iPSC-derived model system following microtubule perturbation.Molecular biology of the cell · 2025Article
- The role of peptides in reversing chemoresistance of breast cancer: current facts and future prospects.Frontiers in pharmacology · 2023Review
- Research progress on antitumor activity of XRP44X and analogues as microtubule targeting agents.Frontiers in chemistry · 2023Review
- Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021.Journal of hematology & oncology · 2022Review
- The interaction of spongistatin 1 with tubulin.Archives of biochemistry and biophysics · 2022Article
- Article
- The Role of Microtubules in Pancreatic Cancer: Therapeutic Progress.Frontiers in oncology · 2021Review
- Concerted cell and in vivo screen for pancreatic ductal adenocarcinoma (PDA) chemotherapeutics.Scientific reports · 2020Article
- The quest for supernatural products: the impact of total synthesis in complex natural products medicinal chemistry.Natural product reports · 2020Review
- Interaction of diazonamide A with tubulin.Archives of biochemistry and biophysics · 2020Article
- From Seabed to Bedside: A Review on Promising Marine Anticancer Compounds.Biomolecules · 2020Review
- Design and Synthesis of Anti-Cancer Chimera Molecules Based on Marine Natural Products.Marine drugs · 2019Review
- Covalent modification of Cys-239 in β-tubulin by small molecules as a strategy to promote tubulin heterodimer degradation.The Journal of biological chemistry · 2019Article
- Natural Products in the "Marketplace": Interfacing Synthesis and Biology.Journal of the American Chemical Society · 2019Review
- An Indole-Chalcone Inhibits Multidrug-Resistant Cancer Cell Growth by Targeting Microtubules.Molecular pharmaceutics · 2018Article
- DZ-2384 has a superior preclinical profile to taxanes for the treatment of triple-negative breast cancer and is synergistic with anti-CTLA-4 immunotherapy.Anti-cancer drugs · 2018Article
- The compound millepachine and its derivatives inhibit tubulin polymerization by irreversibly binding to the colchicine-binding site in β-tubulin.The Journal of biological chemistry · 2018Article
- Ascidian Toxins with Potential for Drug Development.Marine drugs · 2018Review
- Anti-mitotic chemotherapeutics promote apoptosis through TL1A-activated death receptor 3 in cancer cells.Cell research · 2018Article
- Current Status of Marine-Derived Compounds as Warheads in Anti-Tumor Drug Candidates.Marine drugs · 2017Review
Corrections and comments
- Erratum issued
Authors and funding
25 authors at 6 institutions in 3 countries.
Funding
Abstract
Microtubule-targeting agents (MTAs) are widely used anticancer agents, but toxicities such as neuropathy limit their clinical use. MTAs bind to and alter the stability of microtubules, causing cell death in mitosis. We describe DZ-2384, a preclinical compound that exhibits potent antitumor activity in models of multiple cancer types. It has an unusually high safety margin and lacks neurotoxicity in rats at effective plasma concentrations. DZ-2384 binds the vinca domain of tubulin in a distinct way, imparting structurally and functionally different effects on microtubule dynamics compared to other vinca-binding compounds. X-ray crystallography and electron microscopy studies demonstrate that DZ-2384 causes straightening of curved protofilaments, an effect proposed to favor polymerization of tubulin. Both DZ-2384 and the vinca alkaloid vinorelbine inhibit microtubule growth rate; however, DZ-2384 increases the rescue frequency and preserves the microtubule network in nonmitotic cells and in primary neurons. This differential modulation of tubulin results in a potent MTA therapeutic with enhanced safety.
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What OpenQuestion holds
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.