Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy

Yepeng Luan, Jerry Li, Jean A. Bernatchez, Rongshi Li

Research output: Contribution to journalArticlepeer-review

104 Scopus citations


Histone deacetylases (HDACs), encompassing at least 18 members, are promising targets for anticancer drug discovery and development. To date, five histone deacetylase inhibitors (HDACis) have been approved for cancer treatment, and numerous others are undergoing clinical trials. It has been well validated that an agent that can simultaneously and effectively inhibit two or more targets may offer greater therapeutic benefits over single-acting agents in preventing resistance to treatment and in potentiating synergistic effects. A prime example of a bifunctional agent is the hybrid HDAC inhibitor. In this perspective, the authors review the majority of reported kinase/HDAC hybrid inhibitors.

Original languageEnglish (US)
Pages (from-to)3171-3183
Number of pages13
JournalJournal of Medicinal Chemistry
Issue number7
StatePublished - Apr 11 2019

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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