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Synthesis and Investigation of Therapeutic Potential of Isoform-Specific HDAC8 Inhibitors for the Treatment of Cutaneous T Cell Lymphoma

机译:同种型HDAC8抑制剂治疗皮肤T细胞淋巴瘤的合成与调查

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Background: The available treatment option for any type of cancer including CTCL is chemotherapy and radiation therapy which indiscriminately persuade on the normal cells. One way out for selective destruction of CTCL cells without damaging normal cells is the use of histone deacetylase inhibitors (HDACi). Despite promising results in the treatment of CTCL, these HDACi have shown a broadband inhibition profile, moderately selective for one HDAC class but not for a particular isotype. The prevalence of drug-induced side effects leaves open a narrow window of speculation that the decreased therapeutic efficacy and observed side effects may be most likely due to non specific HDAC isoform inhibition. The aim of this paper is to synthesis and evaluates HDAC8 isoform specific inhibitors.
机译:背景:包括CTCL的任何类型癌症的可用治疗选择是化疗和放射治疗,其在正常细胞上不分青红皂白地性说服。 在不损害正常细胞的情况下选择性地破坏CTCl细胞的一种方法是使用组蛋白脱乙酰化酶抑制剂(HDACI)。 尽管有前途的结果在治疗CTCl,但这些HDACI显示了宽带抑制曲线,适度选择一个HDAC类,但不适用于特定同种型。 药物诱导的副作用的患病率叶片打开一个狭窄的猜测窗口,即由于非特异性HDAC同种型抑制而降低的治疗效果和观察到的副作用可能很可能是最有可能的。 本文的目的是合成和评估HDAC8同种型特异性抑制剂。

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