Identification of Myc translation inhibitors

该计划的目标是进行小分子筛选，以识别MYC表达的抑制剂，并在基于正交细胞的测定中进行验证，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，优化了高通量筛选基于细胞的测定，并将其小型化为1536孔格式以支持qHTS。 在此期间，合作团队扩大了筛选范围，并确定了几种新的化学型，导致细胞中MYC表达减少。活性化合物已在独立的试验中得到验证，目前正在进行药物化学和类似物测试之前进行表征。

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.