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首页> 外文期刊>Future medicinal chemistry >Structure-activity relationships of hydroxamate-based histone deacetylase-8 inhibitors: reality behind anticancer drug discovery
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Structure-activity relationships of hydroxamate-based histone deacetylase-8 inhibitors: reality behind anticancer drug discovery

机译：基于羟胺的组蛋白脱乙酰酶-8抑制剂的结构 - 活性关系：抗癌药物发现背后的现实

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摘要

The pan-histone deacetylase (HDAC) inhibitors comprise a fish-like structural orientation where hydrophobic aryl-and zinc-binding groups act as head and tail, respectively of a fish. The linker moiety correlates the body of the fish linking head and tail groups. Despite these pan-HDAC inhibitors, selective HDAC-8 inhibitors are still in demand as a safe remedy. HDAC-8 is involved in invasion and metastasis in cancer. This review deals with the rationale behind HDAC-8 inhibitory activity and selectivity along with detailed structure-activity relationships of diverse hydroxamate-based HDAC-8 inhibitors. HDAC-8 inhibitory potency may be increased by modifying the fish-like pharmacophoric features of such type of pan-HDAC inhibitors. This review may provide a preliminary basis to design and optimize new lead molecules with higher HDAC-8 inhibitory activity. This work may surely enlighten in providing useful information in the field of target-specific anticancer therapy.
机译：泛组蛋白脱乙酰化酶（HDAC）抑制剂包含一种类似鱼类的结构取向，其中疏水性芳基和锌结合基团分别用作头部和尾部。 接头部分将鱼的主体与尾部组的主体相关联。 尽管存在这些泛HDAC抑制剂，但选择性HDAC-8抑制剂仍然是一种安全的补救措施。 HDAC-8参与癌症中的侵袭和转移。 本综述涉及HDAC-8抑制活动和选择性的理由以及不同的基于羟肟酸的HDAC-8抑制剂的详细结构 - 活性关系。 通过改变这种类型的泛HDAC抑制剂的鱼类的药物特征，可以增加HDAC-8抑制效力。 该审查可以为设计和优化具有更高HDAC-8抑制活性的新铅分子提供初步依据。 这项工作可能肯定在提供目标特异性抗癌治疗领域的有用信息时开明。

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