2. Academic Validation
  3. Targeting WD Repeat-Containing Protein 5 (WDR5): A Medicinal Chemistry Perspective

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

  • J Med Chem. 2021 Aug 12;64(15):10537-10556. doi: 10.1021/acs.jmedchem.1c00037.
Xin Chen 1 2,  Junjie Xu 1 2,  Xianghan Wang 1 2,  Guanlu Long 1 2,  Qidong You 1 2,  Xiaoke Guo 1 2
Affiliations

Affiliations

  • 1 Jiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.
  • 2 Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
PMID: 34283608 DOI: 10.1021/acs.jmedchem.1c00037
Abstract

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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Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-148817
    WDR5-MLL1 Inhibitor