ArticleCancer letters2020
Orally available tubulin inhibitor VERU-111 enhances antitumor efficacy in paclitaxel-resistant lung cancer.
Article in Cancer letters, 2020. 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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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.
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Who cites it
20 citing papers in PubMed, 34 citations in OpenAlex.
- A Phase Ib/II Study of Sabizabulin, a Novel Oral Cytoskeleton Disruptor, in Men with Metastatic Castration-resistant Prostate Cancer with Progression on an Androgen Receptor-targeting Agent.Clinical cancer research : an official journal of the American Association for Cancer Research · 2022Trial
- QW-5-70 targets the colchicine site and demonstrates antitumor activity in P-gp-overexpressing cancer models.Molecular cancer therapeutics · 2026Article
- Article
- Design and synthesis of novel 4-aryl-2-benzoyl-imidazoles as colchicine binding site inhibitors.European journal of medicinal chemistry · 2025Article
- Isoxazole-Based Compounds Targeting the Taxane-Binding Site of Tubulin.Archiv der Pharmazie · 2025Article
- VERU-111, an orally available tubulin inhibitor, suppresses ovarian tumor growth and metastasis.The Journal of pharmacology and experimental therapeutics · 2025Article
- The Impact of Genetic Mutations on the Efficacy of Immunotherapies in Lung Cancer.International journal of molecular sciences · 2024Review
- Biological activity of a stable 6-aryl-2-benzoyl-pyridine colchicine-binding site inhibitor, 60c, in metastatic, triple-negative breast cancer.Cancer letters · 2024Article
- Design, synthesis, and bioevaluation of diarylpyrimidine derivatives as novel microtubule destabilizers.Frontiers in chemistry · 2024Article
- Synthesis and biological evaluation of dual MDM2/XIAP inhibitors based on the tetrahydroquinoline scaffold.European journal of medicinal chemistry · 2023Article
- Inhalable CAR-T cell-derived exosomes as paclitaxel carriers for treating lung cancer.Journal of translational medicine · 2023Article
- S-72, a Novel Orally Available Tubulin Inhibitor, Overcomes Paclitaxel Resistance via Inactivation of the STING Pathway in Breast Cancer.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Combination of Paclitaxel and PXR Antagonist SPA70 Reverses Paclitaxel-Resistant Non-Small Cell Lung Cancer.Cells · 2022Article
- Colchicine-Binding Site Agent CH-2-77 as a Potent Tubulin Inhibitor Suppressing Triple-Negative Breast Cancer.Molecular cancer therapeutics · 2022Article
- Design, Synthesis, and Biological Evaluation of Apcin-Based CDC20 Inhibitors.ACS medicinal chemistry letters · 2022Article
- Molecular mechanisms associated with chemoresistance in esophageal cancer.Cellular and molecular life sciences : CMLS · 2022Review
- Carbon quantum dots-Annexin V probe: photoinduced electron transfer mechanism, phosphatidylserine detection, and apoptotic cell imaging.Mikrochimica acta · 2022Article
- [Targeted killing of CD133Nan fang yi ke da xue xue bao = Journal of Southern Medical University · 2022Article
- The Tubulin Inhibitor VERU-111 in Combination With Vemurafenib Provides an Effective Treatment of Vemurafenib-Resistant A375 Melanoma.Frontiers in pharmacology · 2021Article
- Challenges and opportunities in delivering oral peptides and proteins.Expert opinion on drug deliveryReview
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Lung cancer is the most common cause of cancer associated mortality. Chemotherapeutic agents, such as paclitaxel, are important treatment options but drug resistance often develops upon prolonged use. We report here the preclinical evaluation of a new orally available tubulin inhibitor, VERU-111, which can overcome several ABC-transporters mediated multi-drug resistance associated with taxane treatment. In vitro, VERU-111 prevents cell proliferation, invasion, migration and colony formation in both paclitaxel-sensitive and paclitaxel-resistant A549 lung cancer cells. VERU-111 effectively inhibits tubulin polymerization, arrests cells in G2/M phase, and induces cancer cell apoptosis. Further evaluation of various apoptotic proteins revealed that treatment of VERU-111 increases the expression of cleaved-PARP, cleaved-caspase-3 and p-histone H3 proteins. In vivo, orally administered VERU-111 in a paclitaxel-sensitive A549 xenograft model strongly inhibits tumor growth in a dose-dependent manner and is equally potent with paclitaxel. When tested in a highly paclitaxel-resistant A549/TxR tumor model, VERU-111 is as effective as the parental A549 model in significantly reducing the tumor volume, whereas paclitaxel is essentially ineffective. Collectively, this study showed that VERU-111 is a promising new generation of anti-tubulin agent for the treatment of taxane-resistant lung 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.