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Identification of Myc translation inhibitors

Identification of Myc translation inhibitors
Myc 翻译抑制剂的鉴定
批准号:
10919694
负责人:
Alexey Zakharov
金额:
$24.08万
依托单位国家:
美国
项目类别:
财政年份:
--
资助国家:
美国
项目状态:
未结题
起止时间:
至

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中文摘要
翻译
该计划的目标是进行小分子筛选,以确定MYC表达的抑制物,并在基于细胞的正交分析中进行验证,以更好地了解其在癌症进展中的作用,并评估其在癌症中的治疗效果。在此之前,高通量筛选细胞分析被优化和小型化到1536孔格式,以支持qHTS。 在此期间,合作小组扩大了筛查范围,并确定了几种导致细胞中MYC表达减少的新化学类型。活性化合物已经在独立的测试中得到了验证,现在正在药物化学和类似物测试之前进行表征。
英文摘要
The goal of this program is to perform a small molecule screen to identify inhibitors of MYC expression and validate in orthogonal cell-based assays to better understand its role in cancer progression and assess their therapeutic efficacy in cancer. Prior to this period, high throughput screening cell-based assays were optimized and miniaturized to 1536-well format to support qHTS. During this period, the collaborative team expanded screening and identified several novel chemotypes leading to reduced MYC expression in cells. Active compounds have been validated in independent assays and are now being characterized prior to medicinal chemistry and analog testing.
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