國家衛生研究院 NHRI:Item 3990099045/11897
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    题名: Insights for the design of protein lysine methyltransferase G9a inhibitors
    作者: Charles, MRC;Dhayalan, A;Hsieh, HP;Coumar, MS
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: The epigenetic control of gene expression could be affected by addition and/or removal of post-translational modifications such as phosphorylation, acetylation and methylation of histone proteins, as well as methylation of DNA (5-methylation on cytosines). Misregulation of these modifications is associated with altered gene expression, resulting in various disease conditions. G9a belongs to the protein lysine methyltransferases that specifically methylates the K9 residue of histone H3, leading to suppression of several tumor suppressor genes. In this review, G9a functions, role in various diseases, structural biology aspects for inhibitor design, structure-activity relationship among the reported inhibitors are discussed which could aid in the design and development of potent G9a inhibitors for cancer treatment in the future.
    日期: 2019-05-29
    關聯: Future Medicinal Chemistry. 2019 May 29;11(9):993-1014.
    Link to: http://dx.doi.org/10.4155/fmc-2018-0396
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=1756-8919&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000474891700007
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85067607880
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