1. Academic Validation
  2. Perspectives and new aspects of histone deacetylase inhibitors in the therapy of CNS diseases

Perspectives and new aspects of histone deacetylase inhibitors in the therapy of CNS diseases

  • Eur J Med Chem. 2023 Oct 5:258:115613. doi: 10.1016/j.ejmech.2023.115613.
Bo Han 1 Mengfei Wang 1 Jiayi Li 2 Qiushi Chen 2 Niubing Sun 2 Xuezhi Yang 3 Qingwei Zhang 4
Affiliations

Affiliations

  • 1 Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry Co., Ltd., China State Institute of Pharmaceutical Industry, Shanghai, 201203, China.
  • 2 Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry Co., Ltd., China State Institute of Pharmaceutical Industry, Shanghai, 201203, China; School of Chemistry & Chemical Engineering, Shanghai University of Engineering Science, Shanghai, 201620, China.
  • 3 Department of Neurology, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, 325000, China.
  • 4 Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry Co., Ltd., China State Institute of Pharmaceutical Industry, Shanghai, 201203, China. Electronic address: sipiqingwei@163.com.
Abstract

Many populations worldwide are suffering from central nervous system (CNS) diseases such as brain tumors, neurodegenerative diseases (Alzheimer's disease, Parkinson's disease and Huntington's disease) and stroke. There is a shortage of effective drugs for most CNS diseases. As one of the regulatory mechanisms of Epigenetics, the particular role and therapeutic benefits of histone deacetylases (HDACs) in the CNS have been extensively studied. In recent years, HDACs have attracted increasing attention as potential drug targets for CNS diseases. In this review, we summarize the recent applications of representative histone deacetylases inhibitors (HDACis) in CNS diseases and discuss the challenges in developing HDACis with different structures and better blood-brain barrier (BBB) permeability, hoping to promote the development of more effective bioactive HDACis for the treatment of CNS diseases.

Keywords

BBB; CNS diseases; Epigenetics; HDAC inhibitors.

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