Targeting WD Repeat-Containing Protein 5 (WDR5): A Medicinal Chemistry Perspective
Targeting WD Repeat-Containing Protein 5 (WDR5): A Medicinal Chemistry Perspective
复制标题
靶向含有 WD 重复序列的蛋白 5 (WDR5)：药物化学视角
DOI：
10.1021/acs.jmedchem.1c00037
复制
发表时间：
2021-07-20
影响因子：
7.3
通讯作者：
Guo, Xiaoke
中科院分区：
文献类型：
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作者：
Chen, Xin;Xu, Junjie;Guo, Xiaoke
WDR5 （WD repeat-containing protein 5, WDR5）是WD40蛋白家族的一员，在体内广泛参与各种生物活动，并不局限于表观遗传调控。WDR5还参与许多疾病的发生和发展，并在这些疾病中发挥关键作用。自WDR5被发现以来，它就被认为是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。本文综述了近年来针对WDR5的抑制剂的研究进展，并在前人机制研究的基础上探讨了这些抑制剂的生物学机制。最后，介绍了靶向WDR5的抑制剂的发展潜力和进一步的应用前景。
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 in vivo. 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.