Recent Advances with KDM4 Inhibitors and Potential Applications

  • J Med Chem. 2022 Jul 28;65(14):9564-9579. doi: 10.1021/acs.jmedchem.2c00680.
Qiong Wu  1 ,  Brandon Young  2 ,  Yan Wang  3 ,  Andrew M Davidoff  1 ,  Zoran Rankovic  2 ,  Jun Yang  1  4
Affiliations
  • 1. Department of Surgery, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • 2. Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
  • 3. Department of Geriatrics and Occupational Disease, Qingdao Central Hospital, Qingdao 266044, China.
  • 4. Department of Pathology and Laboratory Medicine, College of Medicine, The University of Tennessee Health Science Center, 930 Madison Avenue, Suite 500, Memphis, Tennessee 38163, United States.
PMID: 35838529 DOI: 10.1021/acs.jmedchem.2c00680
Abstract

The histone lysine demethylase 4 (KDM4) family plays an important role in regulating gene transcription, DNA repair, and metabolism. The dysregulation of KDM4 functions is associated with many human disorders, including Cancer, obesity, and cardiovascular diseases. Selective and potent KDM4 inhibitors may help not only to understand the role of KDM4 in these disorders but also to provide potential therapeutic opportunities. Here, we provide an overview of the field and discuss current status, challenges, and opportunities lying ahead in the development of KDM4-based Anticancer therapeutics.

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