1. Academic Validation
  2. Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy

Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy

  • J Med Chem. 2020 Sep 10;63(17):8977-9002. doi: 10.1021/acs.jmedchem.0c00491.
Tingting Liu 1 Yichao Wan 2 Yuliang Xiao 1 Chengcai Xia 1 Guiyun Duan 1
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, School of Pharmacy, Shandong First Medical University & Shandong Academy of Medical Sciences, Taian 271016, Shandong, China.
  • 2 Key Laboratory of Theoretical Organic Chemistry and Functional Molecule, Ministry of Education, School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan 411201, Hunan, China.
Abstract

Histone deacetylases (HDACs) play an important role in regulating target gene expression. They have been highlighted as a novel category of Anticancer targets, and their inhibition can induce Apoptosis, differentiation, and growth arrest in Cancer cells. In view of the fact that HDAC inhibitors and Other antitumor agents, such as BET inhibitors, Topoisomerase inhibitors, and RTK pathway inhibitors, exert a synergistic effect on cellular processes in Cancer cells, the combined inhibition of two targets is regarded as a rational strategy to improve the effectiveness of these single-target drugs for Cancer treatment. In this review, we discuss the theoretical basis for designing HDAC-involved dual-target drugs and provide insight into the structure-activity relationships of these dual-target agents.

Figures