Elraglusib Induces Cytotoxicity via Direct Microtubule Destabilization Independently of GSK3 Inhibition

Elraglusib 通过直接微管不稳定诱导细胞毒性,而不依赖于 GSK3 抑制

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作者:Josh T Coats, Shuyu Li, Tomoyuki U Tanaka, Sudhir Tauro, Calum Sutherland, Adrian T Saurin

Abstract

Elraglusib was designed as a GSK3 inhibitor and is currently in clinical trials for several cancers. We show conclusively that the target of elraglusib that leads to cytotoxicity is MTs and not GSK3. This has significant implications for ongoing clinical trials of the compound and will help in understanding off-target side effects, inform future clinical trial design, and facilitate the development of biomarkers to predict response.

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