Tubulin as a Well-Established Yet Underexploited Target: New Opportunities for Drugs Repurposing?

Drug repurposing can accelerate oncology translation by leveraging approved compounds with known pharmacology; success depends on a plausible mechanism for the new indication. The microtubule cytoskeleton is a validated anticancer target, yet tubulin-directed activity is often overlooked for non-oncology drugs. Using nanoDSF, FDA-approved compounds were recently screened for effects on tubulin polymerization, identifying multiple previously unrecognized microtubule-targeting agents (MTA) including Auranofin, Ebselen, Riboflavin, Aprepitant, Benzarone and Nifedipine derivatives, etc. Many hits match reported microtubule perturbation or cancer-relevant phenotypes, and several have been considered for oncology repositioning. These observations suggest microtubule targeting may contribute to anticancer effects more often than appreciated and that tubulin remains an underexploited repurposing target. The aim of this review is to place these newly identified MTAs in the context of current knowledge and to discuss their potential for drug repurposing in oncology.

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Publication Details

Journal
Journal of drug targeting
Published
2026-06-29
DOI
https://doi.org/10.1080/1061186x.2026.2695854
Primary Topic
Microtubule and mitosis dynamics
Type
article
Field-Weighted Citation Impact
0.00
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article

Tubulin as a Well-Established Yet Underexploited Target: New Opportunities for Drugs Repurposing?

Philipp O. Tsvetkov
Journal of drug targeting
Microtubule and mitosis dynamics
article

Tubulin as a Well-Established Yet Underexploited Target: New Opportunities for Drugs Repurposing?

Philipp O. Tsvetkov
article en

Abstract

Drug repurposing can accelerate oncology translation by leveraging approved compounds with known pharmacology; success depends on a plausible mechanism for the new indication. The microtubule cytoskeleton is a validated anticancer target, yet tubulin-directed activity is often overlooked for non-oncology drugs. Using nanoDSF, FDA-approved compounds were recently screened for effects on tubulin polymerization, identifying multiple previously unrecognized microtubule-targeting agents (MTA) including Auranofin, Ebselen, Riboflavin, Aprepitant, Benzarone and Nifedipine derivatives, etc. Many hits match reported microtubule perturbation or cancer-relevant phenotypes, and several have been considered for oncology repositioning. These observations suggest microtubule targeting may contribute to anticancer effects more often than appreciated and that tubulin remains an underexploited repurposing target. The aim of this review is to place these newly identified MTAs in the context of current knowledge and to discuss their potential for drug repurposing in oncology.

Journal of drug targeting
Institut de Neurophysiopathologie (FR)
Good health and well-being
Openalex Percentile: Top 10%
Microtubule and mitosis dynamics
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