Department of Medicine and Medical Specialities, Faculty of Medicine and Health Sciences, University of Alcalá, 28801 Alcala de Henares, Spain.
Ramón y Cajal Institute of Sanitary Research (IRYCIS), 28034 Madrid, Spain.
Genes (Basel). 2023 Apr 14;14(4):915. doi: 10.3390/genes14040915.
Histone acetylation plays a vital role in organizing chromatin, regulating gene expression and controlling the cell cycle. The first histone acetyltransferase to be identified was histone acetyltransferase 1 (HAT1), but it remains one of the least understood acetyltransferases. HAT1 catalyzes the acetylation of newly synthesized H4 and, to a lesser extent, H2A in the cytoplasm. However, 20 min after assembly, histones lose acetylation marks. Moreover, new noncanonical functions have been described for HAT1, revealing its complexity and complicating the understanding of its functions. Recently discovered roles include facilitating the translocation of the H3H4 dimer into the nucleus, increasing the stability of the DNA replication fork, replication-coupled chromatin assembly, coordination of histone production, DNA damage repair, telomeric silencing, epigenetic regulation of nuclear lamina-associated heterochromatin, regulation of the NF-κB response, succinyl transferase activity and mitochondrial protein acetylation. In addition, the functions and expression levels of HAT1 have been linked to many diseases, such as many types of cancer, viral infections (hepatitis B virus, human immunodeficiency virus and viperin synthesis) and inflammatory diseases (chronic obstructive pulmonary disease, atherosclerosis and ischemic stroke). The collective data reveal that HAT1 is a promising therapeutic target, and novel therapeutic approaches, such as RNA interference and the use of aptamers, bisubstrate inhibitors and small-molecule inhibitors, are being evaluated at the preclinical level.
组蛋白乙酰化在组织染色质、调节基因表达和控制细胞周期方面起着至关重要的作用。第一个被鉴定的组蛋白乙酰转移酶是组蛋白乙酰转移酶 1(HAT1),但它仍然是了解最少的乙酰转移酶之一。HAT1 催化新合成的 H4 和在细胞质中较少程度的 H2A 的乙酰化。然而,在组装 20 分钟后,组蛋白失去乙酰化标记。此外,已经描述了 HAT1 的新的非典型功能,揭示了其复杂性,并使对其功能的理解复杂化。最近发现的作用包括促进 H3H4 二聚体进入细胞核的易位,增加 DNA 复制叉的稳定性,复制偶联的染色质组装,组蛋白产生的协调,DNA 损伤修复,端粒沉默,核纤层相关异染色质的表观遗传调控,NF-κB 反应的调节,琥珀酰基转移酶活性和线粒体蛋白乙酰化。此外,HAT1 的功能和表达水平与许多疾病有关,例如多种癌症、病毒感染(乙型肝炎病毒、人类免疫缺陷病毒和 viperin 合成)和炎症性疾病(慢性阻塞性肺疾病、动脉粥样硬化和缺血性中风)。综合数据表明,HAT1 是一个很有前途的治疗靶点,正在临床前水平评估新的治疗方法,如 RNA 干扰和使用适体、双底物抑制剂和小分子抑制剂。