西达本胺治疗肿瘤性疾病的研究进展

Research progress of chidamide in treatment of tumor diseases

组蛋白去乙酰化物酶抑制剂（HDACi）能够靶向阻断组蛋白去乙酰化酶（HDAC）的去乙酰化作用，解除低乙酰化对基因转录的抑制，使异常沉默的基因重新表达，促进细胞分化或凋亡，实现对肿瘤性疾病的治疗。近年来，vorinostat、romidepsin、belinostat等多种HDACi相继面市，并用于皮肤T细胞淋巴瘤或外周T细胞淋巴瘤的治疗。西达本胺是化学合成的新一代亚型选择性苯甲酰类HDACi,可选择性抑制第Ⅰ类HDAC的1、2、3亚型和第Ⅱb类HDAC的10亚型，是我国自主研发的广谱抗肿瘤药物。笔者拟就西达本胺在肿瘤性疾病中的研究进展进行综述。

Histone deacetylase inhibitors （HDACi） are able to target intervention of the deacetylation of histone deacetylases（HDAC）, desensitize the inhibition of gene transcription by hypoacetylation, re-express abnormally silenced genes, and promote cell differentiation or apoptosis, to achieve the treatment of neoplastic diseases. In recent years, many HDACi such as vorinostat, romidepsin and belinostat have appeared on the market and are used for the treatment of cutaneous T-cell lymphoma or peripheral T-cell lymphoma.Chidamide is entirely chemical synthesized, and it is a novel HDACi of benzamide, which aims at subtype 1, 2, 3 of classⅠHDAC and subtype 10 of class Ⅱb HDAC. Chidamide is researched and developmented independently by China, which is a broad-spectrum antitumor drug. This article summaries the studies of chidamide in treatment of tumor diseases.