多发性骨髓瘤SET结构域蛋白（MMSET）作为NSD组蛋白甲基转移酶家族的成员之一，在人类胚胎发育等生理过程中发挥着重要的作用。近年来大量研究表明，MMSET在多发性骨髓瘤、前列腺癌、乳腺癌、卵巢癌、胃癌等各种恶性肿瘤中过表达，抑制MMSET的表达能够通过抑制肿瘤增殖、抑制肿瘤侵袭转移、抑制肿瘤DNA损伤修复、抑制磷酸戊糖途径及逆转肿瘤耐药等来抑制肿瘤的发展。因此发展MMSET相关靶向药物有望成为肿瘤治疗的新方向。通过查阅国内外相关文献，总结MMSET相关靶向药物可能的抗肿瘤机制及MMSET相关靶向药物的发展现状。

MMSET plays an important role in human embryonic development and other physiological processes as a member of NSD histone methyltransferase family. In recent years, a large number of evidence has shown that MMSET is frequently hyperactivated in multiple myeloma, prostate cancer, breast cancer, ovarian cancer, gastric cancer, and other malignant tumors. The expression of MMSET can be suppressed by inhibiting tumor proliferation, invasion and metastasis, DNA damage repair, pentose phosphate pathway, and reversing tumor resistance to inhibit the development of tumor. In this paper, the possible anti-tumor mechanisms and development status of MMSET related targeted drugs are summarized by referring to relevant literatures.

辽宁省卵巢癌恶性肿瘤病例信息平台的建立及诊治技术规范化推广项目（LNCCC-A01-2015）；沈阳市科技计划项目（17-230-9-10）