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Celastrol improves the therapeutic efficacy of EGFR-TKIs for non-small-cell lung cancer by overcoming EGFR T790M drug resistance

Abstract : The development of resistance to therapy continues to be a serious clinical problem in lung cancer management. Epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) is one of the most common chemotherapy drugs to treat non-small-cell lung cancer. However, almost all treatments fail after ∼1 year of treatment because of drug tolerance, probably occurring from the threonine 790 mutation (T790M) of the EGFR, resulting in overactivation of the EGFR. Celastrol is a natural compound that exhibits antiproliferative activity. In this study, we showed that celastrol combined with EGFR-TKIs significantly suppressed cell invasion of lung cancer cells with a T790M mutation by suppressing the EGFR pathway. Combined therapy with celastrol and EGFR-TKIs inhibited tumor growth in vivo. Together, these results suggested that combined therapy with EGFR-TKIs and celastrol may be a more effective treatment of patients with non-small-cell lung cancer with T790M mutations of the EGFR.
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https://www.hal.inserm.fr/inserm-02402025
Contributor : Georges Uzan <>
Submitted on : Tuesday, December 10, 2019 - 12:00:06 PM
Last modification on : Wednesday, September 16, 2020 - 5:16:20 PM

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Ying Wang, Qiuyun Liu, Haojie Chen, Jun You, Bin Peng, et al.. Celastrol improves the therapeutic efficacy of EGFR-TKIs for non-small-cell lung cancer by overcoming EGFR T790M drug resistance. Anti-Cancer Drugs, Lippincott, Williams & Wilkins, 2018, 29 (8), pp.748-755. ⟨10.1097/CAD.0000000000000647⟩. ⟨inserm-02402025⟩

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