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Recent advances in the development of histone deacylase SIRT2 inhibitors

机译:组蛋白脱酰基酶SIRT2抑制剂的开发的最新进展

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摘要

Sirtuin 2 (SIRT2) is an important and special member of the atypical histone deacetylase Sirtuin (SIRT) family. Due to its extensive catalytic effects, SIRT2 can regulate autophagy, myelination, immunity, inflammation and other physiological processes. Recent evidence revealed that dysregulation of human SIRT2 activity is associated with the pathogenesis and prognosis of cancers, Parkinson's disease and other disorders; thus SIRT2 is a promising target for potential therapeutic intervention. This review presents a systematic summary of nine chemotypes of small-molecule SIRT2 inhibitors, particularly including the discovery and structural optimization strategies, which will be useful for future efforts to develop new inhibitors targeting SIRT2 and associated target proteins.
机译:Sirtuin 2(Sirt2)是非典型组蛋白脱乙酰酶Sirtuin(Sirt)家族的重要和特殊成员。 由于其广泛的催化作用,SIRT2可以调节自噬,髓鞘,免疫,炎症和其他生理过程。 最近的证据表明,人体SIRT2活性的失调与癌症,帕金森病等疾病的发病机制和预后有关; 因此,Sirt2是潜在治疗介入的有希望的目标。 本综述介绍了九分型SIRT2抑制剂的九个趋化型,特别是包括发现和结构优化策略,这对于未来的努力开发靶向SIRT2和相关靶蛋白的新抑制剂是有用的。

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  • 来源
    《RSC Advances》 |2020年第61期|共9页
  • 作者单位

    Xihua Univ Coll Food &

    Bioengn Chengdu 610039 Peoples R China;

    Xihua Univ Coll Food &

    Bioengn Chengdu 610039 Peoples R China;

    Xihua Univ Coll Food &

    Bioengn Chengdu 610039 Peoples R China;

    Xihua Univ Coll Food &

    Bioengn Chengdu 610039 Peoples R China;

    Xihua Univ Coll Food &

    Bioengn Chengdu 610039 Peoples R China;

    Xihua Univ Coll Sci Chengdu 610039 Sichuan Peoples R China;

    Xihua Univ Coll Food &

    Bioengn Chengdu 610039 Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
  • 关键词

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