國家衛生研究院 NHRI:Item 3990099045/15630
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    题名: First-in-class dual EZH2-HSP90 inhibitor eliciting striking antiglioblastoma activity in vitro and in vivo
    作者: Sharma, S;Wang, SA;Yang, WB;Lin, HY;Lai, MJ;Chen, HC;Kao, TY;Hsu, FL;Nepali, K;Hsu, TI;Liou, JP
    贡献者: NHRI Graduate Student Program
    摘要: Structural analysis of tazemetostat, an FDA-approved EZH2 inhibitor, led us to pinpoint a suitable site for appendage with a pharmacophoric fragment of second-generation HSP90 inhibitors. Resultantly, a magnificent dual EZH2/HSP90 inhibitor was pinpointed that exerted striking cell growth inhibitory efficacy against TMZ-resistant Glioblastoma (GBM) cell lines. Exhaustive explorations of chemical probe 7 led to several revelations such as (i) compound 7 increased apoptosis/necrosis-related gene expression, whereas decreased M phase/kinetochore/spindle-related gene expression as well as CENPs protein expression in Pt3R cells; (ii) dual inhibitor 7 induced cell cycle arrest at the M phase; (iii) compound 7 suppressed reactive oxygen species (ROS) catabolism pathway, causing the death of TMZ-resistant GBM cells; and (iv) compound 7 elicited substantial in vivo anti-GBM efficacy in experimental mice xenografted with TMZ-resistant Pt3R cells. Collectively, the study results confirm the potential of dual EZH2-HSP90 inhibitor 7 as a tractable anti-GBM agent.
    日期: 2024-01-29
    關聯: Journal of Medicinal Chemistry. 2024 Jan 29;67(4):2963-2985.
    Link to: http://dx.doi.org/10.1021/acs.jmedchem.3c02053
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0022-2623&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:001162313100001
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85184803383
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