FL118, acting as a ‘molecular glue degrader’, binds to dephosphorylates and degrades the oncoprotein DDX5 (p68) to control c-Myc, survivin and mutant Kras against colorectal and pancreatic cancer with high efficacy,Clinical and Translational Medicine

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FL118, acting as a ‘molecular glue degrader’, binds to dephosphorylates and degrades the oncoprotein DDX5 (p68) to control c-Myc, survivin and mutant Kras against colorectal and pancreatic cancer with high efficacy
Clinical and Translational Medicine ( IF 7.919 ) Pub Date : 2022-05-23 , DOI: 10.1002/ctm2.881
Xiang Ling _{1,

2} , Wenjie Wu _{1,

2} , Ieman A. M. Aljahdali _{1,

3} , Jianqun Liao ₂ , Sreevidya Santha ₂ , Christos Fountzilas _{4,

5} , Patrick M. Boland ₄ , Fengzhi Li _{1,

5}

Affiliation

Pancreatic ductal adenocarcinoma (PDAC), a difficult-to-treat cancer, is expected to become the second-largest cause of cancer-related deaths by 2030, while colorectal cancer (CRC) is the third most common cancer and the third leading cause of cancer deaths. Currently, there is no effective treatment for PDAC patients. The development of novel agents to effectively treat these cancers remains an unmet clinical need. FL118, a novel anticancer small molecule, exhibits high efficacy against cancers; however, the direct biochemical target of FL118 is unknown.

中文翻译：

FL118，作为“分子胶降解剂”，与去磷酸盐结合并降解癌蛋白 DDX5 (p68)，以高效控制 c-Myc、survivin 和突变 Kras 对抗结肠直肠癌和胰腺癌

胰腺导管腺癌 (PDAC) 是一种难以治疗的癌症，预计到 2030 年将成为癌症相关死亡的第二大原因，而结直肠癌 (CRC) 是第三大常见癌症和第三大常见癌症。癌症死亡。目前，PDAC患者尚无有效的治疗方法。开发有效治疗这些癌症的新型药物仍然是未满足的临床需求。FL118，一种新型抗癌小分子，具有高效抗癌作用；然而，FL118的直接生化靶点尚不清楚。

更新日期：2022-05-26

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