Targeting histone deacetylases for cancer therapy: Trends and challenges

Dysregulation of histone deacetylases (HDACs) is closely related to tumor development and progression. As promising anticancer targets, HDACs have gained a great deal of research interests and two decades of effort has led to the approval of five HDAC inhibitors (HDACis). However, currently traditional HDACis, although effective in approved indications, exhibit severe off-target toxicities and low sensitivities against solid tumors, which have urged the development of next-generation of HDACi. This review investigates the biological functions of HDACs, the roles of HDACs in oncogenesis, the structural features of different HDAC isoforms, isoform-selective inhibitors, combination therapies, multitarget agents…

• NN
  National Natural Science Foundation of China

  Awards: 82003590, 92053105, 81874288
• NS
  Natural Science Foundation of Shandong Province

  Awards: ZR2020QH342, 81874288
• NS
  Natural Science Foundation of Anhui Province