2. Academic Validation
  3. Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy

Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy

  • J Med Chem. 2019 Apr 11;62(7):3171-3183. doi: 10.1021/acs.jmedchem.8b00189.
Yepeng Luan 1,  Jerry Li,  Jean A Bernatchez,  Rongshi Li 1 2
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, School of Pharmacy , Qingdao University , Qingdao 266071 , Shandong Province , China.
  • 2 UNMC Center for Drug Discovery, Department of Pharmaceutical Sciences, College of Pharmacy, Fred and Pamela Buffett Cancer Center, and Center for Staphylococcal Research , University of Nebraska Medical Center , Omaha , Nebraska 68198 , United States.
PMID: 30418766 DOI: 10.1021/acs.jmedchem.8b00189
Abstract

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.

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