Title:Hybrid Histone Deacetylase Inhibitor: An Effective Strategy for
Cancer Therapy
Volume: 30
Issue: 20
关键词:
组蛋白脱乙酰酶,杂交,多靶点抑制剂,抗肿瘤,癌症治疗,双功能剂。
摘要: Inhibition of histone deacetylases (HDACs) has proven to be an effective strategy
for cancer therapy. To date, five histone deacetylase inhibitors (HDACis) have been
approved for cancer treatment, and numerous others are undergoing clinical trials. 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 potentiating
synergistic effects. A prime example of a bifunctional agent is the hybrid
HDACi. Representative classes of reported hybrid HDACis are reviewed here to shed
light on the design of novel hybrid HDACis for cancer therapy.