4.7 Article

Targeting WD Repeat-Containing Protein 5 (WDR5): A Medicinal Chemistry Perspective

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 64, Issue 15, Pages 10537-10556

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.1c00037

Keywords

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Funding

  1. National Natural Science Foundation of China [81872799, 81930100, 81773639]
  2. Natural Science Foundation of Jiangsu Province of China [BK 20191321]
  3. Fundamental Research Funds for the Central Universities [2632018ZD14]
  4. National Science Technology Major Project Key New Drug Creation and Manufacturing Program of China [2017ZX0930200, 2018ZX09711002]
  5. Double First Class Innovation Team of China Pharmaceutical University [CPU2018GY02]
  6. Program for Outstanding Scientific and Technological Innovation Team of Jiangsu Higher Education
  7. Open Project of State Key Laboratory of Natural Medicines [SKLNMZZCX201803]
  8. Priority Academic Program Development of Jiangsu Higher Education Institutions

Ask authors/readers for more resources

WDR5, a member of the WD40 protein family, is involved in various biological activities and diseases. It is considered a potential target for disease treatment, and inhibitors targeting WDR5 have shown great development potential and application prospects.
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.

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