ArticleThe Journal of biological chemistry2019
Reversible binding of the anticancer drug KXO1 (tirbanibulin) to the colchicine-binding site of β-tubulin explains KXO1's low clinical toxicity.
Article in The Journal of biological chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed, 65 citations in OpenAlex.
- Illuminating microtubule functions with small molecules: past, present and future of fluorescent tubulin-binding probes.RSC chemical biology · 2026Review
- Real-World Efficacy of Tirbanibulin in Actinic Keratosis Treatment: Expert Consensus and Clinical Insights.Dermatology practical & conceptual · 2025Review
- Synthesis of Epoxyoxirenes: Phytotoxic Activity and Enzymatic Target Identification.Plants (Basel, Switzerland) · 2025Article
- Treatment of Condyloma Acuminata with Tirbanibulin 1% Ointment in People Living with HIV: A Case Series with Literature Review.Infectious disease reports · 2025Review
- Clinical and experimental aspects of tirbanibulin treatments.Archives of dermatological research · 2025Review
- Cost-Effectiveness Analysis of Topical Treatments for Actinic Keratosis in Italian National Health System.Journal of clinical medicine · 2024Article
- Synthesis and Biological Evaluation of Novel 2-Aroyl Benzofuran-Based Hydroxamic Acids as Antimicrotubule Agents.International journal of molecular sciences · 2024Article
- Topical Pharmacological Treatment of Actinic Keratoses: Focus on Tirbanibulin 1% Ointment.Dermatology practical & conceptual · 2024Review
- Anti-tumor effects of tirbanibulin in squamous cell carcinoma cells are mediated via disruption of tubulin-polymerization.Archives of dermatological research · 2024Article
- Development of a Stability Indicating UPLC Method for the Determination of Tirbanibulin in Bulk and Its Pharmaceutical Dosage Form.Turkish journal of pharmaceutical sciences · 2024Article
- PM534, an Optimized Target-Protein Interaction Strategy through the Colchicine Site of Tubulin.Journal of medicinal chemistry · 2024Article
- Novel Brain-Penetrant, Small-Molecule Tubulin Destabilizers for the Treatment of Glioblastoma.Biomedicines · 2024Article
- Frentizole, a Nontoxic Immunosuppressive Drug, and Its Analogs Display Antitumor Activity via Tubulin Inhibition.International journal of molecular sciences · 2023Article
- Preliminary Evidence of Efficacy, Safety, and Treatment Satisfaction with Tirbanibulin 1% Ointment: A Clinical Perspective on Actinic Keratoses.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Synthesis and evaluation of tirbanibulin derivatives: a detailed exploration of the structure-activity relationship for anticancer activity.RSC advances · 2023Article
- Real-world experience with histological confirmation of clinical response of squamous cell carcinoma to topical tirbanibulin.JAAD case reports · 2023Article
- Exploring Pyrrolo-Fused Heterocycles as Promising Anticancer Agents: An Integrated Synthetic, Biological, and Computational Approach.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Profile of Tirbanibulin for the Treatment of Actinic Keratosis.The Journal of clinical and aesthetic dermatology · 2022Article
- Design, Synthesis and Biological Investigation of 2-Anilino Triazolopyrimidines as Tubulin Polymerization Inhibitors with Anticancer Activities.Pharmaceuticals (Basel, Switzerland) · 2022Article
- 1% Tirbanibulin Ointment for the Treatment of Actinic Keratoses.The Annals of pharmacotherapy · 2022Review
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
KXO1 (tirbanibulin or KX2-391) is as a non-ATP-competitive inhibitor of SRC proto-oncogene nonreceptor tyrosine kinase (SRC) and is being clinically investigated for the management of various cancers and actinic keratosis. Recently, KXO1 has also been shown to strongly inhibit tubulin. Interestingly, unlike conventional tubulin-targeting drugs, KXO1 has exhibited low toxicity in preclinical and clinical studies, but the reason for this remains elusive, as are the KXO1-binding site and other details of the interaction of KXO1 with tubulin. Here, cell-based experiments revealed that KXO1 induces tubulin depolymerization and G
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