Overexpression of ABCG2 confers resistance to pevonedistat, an NAE inhibitor.


:Pevonedistat is a potent, selective, first-in-class NEDD8 activating enzyme inhibitor. It is now under multiple clinical trials that investigate its anticancer effect against solid tumors and leukemia. ATP-binding cassette (ABC) transporters are membrane proteins that are involved in mediating multidrug resistance (MDR). In this article, we reveal that pevonedistat is a substrate of ABCG2 which decreases the therapeutic effect of pevonedistat. The cytotoxicity of pevonedistat was significantly weakened in ABCG2-overexpressing cells, and the drug resistance can be reversed by ABCG2 inhibitors. The ATPase assay suggested that pevonedistat can stimulate ABCG2 ATPase activity in a concentration-dependent manner. Pevonedistat showed little effect on the expression level or subcellular localization of ABCG2 after 72 h treatment. Furthermore, a pevonedistat resistance cell line S1-PR was established and overexpressed ABCG2. Generally, our study provides evidence that ABCG2 can be a prominent factor leading to pevonedistat-resistance. Furthermore, ABCG2 may also be utilized as a biomarker to monitor the development of pevonedistat resistance during cancer treatment.


Exp Cell Res


Wei LY,Wu ZX,Yang Y,Zhao M,Ma XY,Li JS,Yang DH,Chen ZS,Fan YF




Has Abstract


2020-03-15 00:00:00














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    journal_title:Experimental cell research

    pub_type: 杂志文章


    authors: Meighan-Mantha RL,Wellstein A,Riegel AT

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  • C-banding of Peromyscus constitutive heterochromatin persists following histone hyperacetylation.

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    journal_title:Experimental cell research

    pub_type: 杂志文章


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    journal_title:Experimental cell research

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    journal_title:Experimental cell research

    pub_type: 杂志文章


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  • Cytosolic free calcium spiking affected by intracellular pH change.

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    journal_title:Experimental cell research

    pub_type: 杂志文章


    authors: Tsunoda Y

    更新日期:1990-06-01 00:00:00

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    journal_title:Experimental cell research

    pub_type: 杂志文章


    authors: Castro-Muñozledo F,Beltrán-Langarica A,Kuri-Harcuch W

    更新日期:2003-04-01 00:00:00

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    journal_title:Experimental cell research

    pub_type: 杂志文章


    authors: Szabó G Jr

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    journal_title:Experimental cell research

    pub_type: 杂志文章


    authors: Teifel M,Friedl P

    更新日期:1996-10-10 00:00:00