MLL1小分子抑制剂研究进展

Progress in Small Molecule Inhibitors of MLL1

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 a pivotal role in gene regulation, development and differentiation. Translocations involving chromosomal band l lq23ns lead to fusion of MLL1 gene to other genes and generation of various MLLI fusion proteins with N-terminus fused in- frame with distinct partner proteins, contributing to the pathogenesis and development of acute leukemogenesis. MLLI is one of the hot targets for molecular targeted cancer therapy. Rcsearch progress in MLLI inhibitors has been reviewed in this paper.