Jiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.
Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
J Med Chem. 2021 Aug 12;64(15):10537-10556. doi: 10.1021/acs.jmedchem.1c00037. Epub 2021 Jul 20.
WD repeat-containing protein 5 (WDR5) is a member of the WD40 protein family, and it is widely involved in various biological activities and not limited to epigenetic regulation . WDR5 is also involved in the initiation and development of many diseases and plays a key role in these diseases. Since WDR5 was discovered, it has been suggested as a potential disease treatment target, and a large number of inhibitors targeting WDR5 have been discovered. In this review, we discussed the development of inhibitors targeting WDR5 over the years, and the biological mechanisms of these inhibitors based on previous mechanistic studies were explored. Finally, we describe the development potential of inhibitors targeting WDR5 and prospects for further applications.
WD 重复蛋白 5（WDR5）是 WD40 蛋白家族的成员，广泛参与各种生物活性，不仅限于表观遗传调控。WDR5 还参与许多疾病的发生和发展，在这些疾病中起着关键作用。自 WDR5 被发现以来，它已被提议作为一种潜在的疾病治疗靶点，并且已经发现了大量针对 WDR5 的抑制剂。在这篇综述中，我们讨论了多年来针对 WDR5 的抑制剂的发展，并根据以前的机制研究探讨了这些抑制剂的生物学机制。最后，我们描述了针对 WDR5 的抑制剂的开发潜力和进一步应用的前景。
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