The oncogene Myc is deregulated in the majority of human tumors and drives numerous hallmarks of cancer. Despite its indisputable role in cancer development and maintenance, Myc is still undrugged. Developing a clinical inhibitor for Myc has been particularly challenging owing to its intrinsically disordered nature and lack of a binding pocket, coupled with concerns regarding potentially deleterious side effects in normal proliferating tissues. However, major breakthroughs in the development of Myc inhibitors have arisen in the last couple of years. Notably, the direct Myc inhibitor that we developed has just entered clinical trials. Celebrating this milestone, with this Perspective, we pay homage to the different strategies developed so far against Myc and all of the researchers focused on developing treatments for a target long deemed undruggable.

中文翻译：

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将 Myc 抑制剂推向临床的漫长旅程

癌基因 Myc 在大多数人类肿瘤中不受管制，并导致许多癌症特征。尽管 Myc 在癌症的发展和维持中发挥着无可争议的作用，但它仍然没有被药物化。由于 Myc 本质上无序且缺乏结合袋，再加上对正常增殖组织中潜在有害副作用的担忧，开发 Myc 的临床抑制剂特别具有挑战性。然而，Myc 抑制剂的开发在过去几年中出现了重大突破。值得注意的是，我们开发的直接Myc抑制剂刚刚进入临床试验。为了庆祝这一里程碑，我们从这个角度向迄今为止针对 Myc 开发的不同策略以及所有专注于为长期被认为无法成药的目标开发治疗方法的研究人员致敬。