Li Jianglei, Yu Meihong, Fu Shifeng, Liu Deliang, Tan Yuyong
Department of Gastroenterology, The Second Xiangya Hospital of Central South University, Changsha, China.
Research Center of Digestive Disease, Central South University, Changsha, China.
Front Pharmacol. 2022 May 16;13:907981. doi: 10.3389/fphar.2022.907981. eCollection 2022.
The deacetylation process regulated by histone deacetylases (HDACs) plays an important role in human health and diseases. HDAC6 belongs to the Class IIb of HDACs family, which mainly modifies non-histone proteins located in the cytoplasm. HDAC6 plays a key role in tumors, neurological diseases, and inflammatory diseases. Therefore, targeting HDAC6 has become a promising treatment strategy in recent years. ACY-1215 is the first orally available highly selective HDAC6 inhibitor, and its efficacy and therapeutic effects are being continuously verified. This review summarizes the research progress of ACY-1215 in cancer and other human diseases, as well as the underlying mechanism, in order to guide the future clinical trials of ACY-1215 and more in-depth mechanism researches.
由组蛋白去乙酰化酶(HDACs)调控的去乙酰化过程在人类健康和疾病中发挥着重要作用。HDAC6属于HDACs家族的IIb类,主要修饰位于细胞质中的非组蛋白。HDAC6在肿瘤、神经疾病和炎症性疾病中起关键作用。因此,近年来靶向HDAC6已成为一种有前景的治疗策略。ACY-1215是首个口服可用的高选择性HDAC6抑制剂,其疗效和治疗效果正在不断得到验证。本综述总结了ACY-1215在癌症和其他人类疾病中的研究进展及其潜在机制,以指导ACY-1215未来的临床试验和更深入的机制研究。