组蛋白去乙酰化酶抑制剂在血液系统恶性肿瘤中的治疗进展

Advances in treatment of histone deacetylase inhibitors in hematological malignancies

组蛋白乙酰化，主要由组蛋白乙酰化酶（HAT）与组蛋白去乙酰化酶（HDAC）催化完成。HAT与HDAC能够调控组蛋白乙酰化／去乙酰化平衡，从而在基因表达调控、DNA复制及修复等过程中起着重要作用，参与多种基因的转录调控，在多种血液系统恶性肿瘤发生、发展中发挥了关键作用。组蛋白去乙酰化酶抑制剂（HDACI）通过抑制HDAC发挥生物学效应。HDACI具有明确的抗肿瘤作用，在实体瘤及血液系统恶性肿瘤的治疗中，尤其在急性髓细胞白血病（AML）、多发性骨髓瘤（MM）、非霍奇金淋巴瘤（NHL）、皮肤性T细胞淋巴瘤（CTCL）等血液系统恶性肿瘤的治疗中，取得了较好的疗效。

Histone acetylation is mainly catalyzed by histone acetylase （HAT） and histone deacetylase （HDAC）. HAT and HDAC can regulate histone acetylation/deacetylation balance and play important roles in gene expression regulation, DNA replication and repair, and participate in transcriptional regulation of multiple genes, which have significant applications in a variety of blood tumors, solid tumors and autoimmune. Histone deacetylase inhibitor （HDACI） exerts biological effects by inhibiting HDAC. HDACI have definite anti-tumor effects for the treatment of solid tumors and hematologic malignancies, especially in hematological malignancies such as acute myeloid Leukemia（AML）, multiple myeloma（MM）, non-Hodgkin lymphoma（NHL）, cutaneous T cell lymphoma（CTCL） and other hematological malignancies, and it has achieved better curative effect.