Wu Xia, Ye Wu, Gong Yuping
Department of Hematology, West China Hospital, Sichuan University, Chengdu, China.
Front Oncol. 2022 Apr 28;12:873903. doi: 10.3389/fonc.2022.873903. eCollection 2022.
mA modification is the most common modification in eukaryotes. , as a core methyltransferase of mA modification, plays a vital role in normal and malignant hematopoiesis. Recent studies have shown that is required for normal and symmetric differentiation of hematopoietic stem/progenitor cells (HSPCs). Moreover, strongly impacts the process and development of hematological neoplasms, including the differentiation, apoptosis, proliferation, chemoresistance, and risk of tumors. Novel inhibitors of have been identified and studied in acute myeloid leukemia (AML) cells. STM2457, a selective inhibitor of , has been identified to block proliferation and promote differentiation and apoptosis of AML cells without impacting normal hematopoiesis. Therefore, in our present review, we focus on the structure of , the role of in both normal and malignant hematopoiesis, and the potential of for treating hematological neoplasms.
mA修饰是真核生物中最常见的修饰。作为mA修饰的核心甲基转移酶,在正常和恶性造血过程中起着至关重要的作用。最近的研究表明,造血干/祖细胞(HSPCs)的正常和对称分化需要(该酶)。此外,(该酶)对血液肿瘤的发生发展过程有强烈影响,包括肿瘤的分化、凋亡、增殖、化疗耐药性及风险。已在急性髓系白血病(AML)细胞中鉴定并研究了该酶的新型抑制剂。STM2457是该酶的一种选择性抑制剂,已被证实可阻断AML细胞的增殖并促进其分化和凋亡,而不影响正常造血。因此,在我们当前的综述中,我们聚焦于该酶的结构、其在正常和恶性造血中的作用以及其在治疗血液肿瘤方面的潜力。