國家衛生研究院 NHRI:Item 3990099045/16735
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    题名: Repurposing linezolid in conjunction with histone deacetylase inhibitor access in the realm of glioblastoma therapies
    作者: Chen, IC;Lin, HY;Liu, ZY;Cheng, WJ;Yeh, TY;Yang, WB;Tran, HY;Lai, MJ;Wang, CH;Kao, TY;Hung, CY;Huang, YL;Liou, KC;Hsieh, CM;Hsu, T;Liou, JP
    贡献者: NHRI Graduate Student Program
    摘要: Since decades after temozolomide was approved, no effective drugs have been developed. Undoubtedly, blood-brain barrier (BBB) penetration is a severe issue that should be overcome in glioblastoma multiforme (GBM) drug development. In this research, we were inspired by linezolid through structural modification with several bioactive moieties to achieve the desired brain delivery. The results indicated that the histone deacetylase modification, referred to as compound 1, demonstrated promising cytotoxic effects in various brain tumor cell lines. Further comprehensive mechanism studies indicated that compound 1 induced acetylation, leading to DNA double-strand breaks, and induced the ubiquitination of RAD51, disrupting the DNA repair process. Furthermore, compound 1 also exhibited dramatic improvement in the orthotopic GBM mouse model, demonstrating its efficacy and satisfying BBB penetration. Therefore, the reported compound 1, provided with an independent therapeutic pathway, satisfying elongation in survival and tumor size reduction, and the ability to penetrate the BBB, was potent to achieve further development.
    日期: 2025-01-21
    關聯: Journal of Medicinal Chemistry. 2025 Jan 21;Article in Press.
    Link to: http://dx.doi.org/10.1021/acs.jmedchem.4c02086
    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:001401408300001
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85215829210
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