MCL-1及其抑制剂在血液恶性肿瘤靶向治疗中的研究进展

摘要

MCL-1(myeloid cell leukemia-1)蛋白是BCL-2(B-cell lymphoma-2)蛋白家族中重要的抗凋亡蛋白之一.MCL-1过表达不仅与肿瘤发生发展密切相关,而且与靶向治疗和传统化疗药物耐药密切相关,然而研发适用于临床的靶向MCL-1的小分子抑制剂目前尚具挑战性.近十几年对MCL-1及其抑制剂进行了大量深入的研究,其中MCL-1内源性配体BH3的小分子类似物的开发取得了重大突破.本文对MCL-1及其抑制剂在血液肿瘤中的研究进展做一综述.%Myeloid cell leukemia-1 (MCL-1) protein is one of the key antiapoptotic protein members of the B-cell lymphoma-2 protein family. Overexpression of MCL-1 is closely related to not only tumor progression but also resistance to targeted therapy and traditional chemotherapeutic drug. MCL-1 and its inhibitors have been studied in recent years. The mimetics of MCL-1 endogenous ligand BH3 have resulted in significant breakthroughs. In this study, the research progress on MCL-1 and its inhibitors in hematological malignan-cies is reviewed.