组蛋白H3K4甲基转移酶MLL1在基因调控、细胞增殖、生长分化等正常生理功能中发挥着重要作用。染色体带11q23异位可导致MLL1基因与其他基因融合而产生多种N端与融合伙伴结合的MLL1融合蛋白,与急性白血病的发生发展密切相关。MLL1是目前肿瘤分子靶向治疗的热门靶标之一。综述了近年来MLL1抑制剂的研究进展。 Histone H3K4 methyltransferase MLL1 plays an important role in normal physiological functions such as gene regulation, cell proliferation, growth and differentiation. Ectopic chromosome 11q23 can lead to MLL1 gene fusion with other genes to produce a variety of N-terminal fusion partners MLL1 fusion protein, and the occurrence and development of acute leukemia are closely related. MLL1 is currently one of the hot targets for tumor molecular targeted therapy. The research progress of MLL1 inhibitors in recent years is reviewed.