MDM2-P53蛋白质相互作用的小分子抑制物

Small Molecules Inhibitor of MDM2-P53 Interaction

p53作为重要的抑癌基因已经成为一个治疗癌症重点的突破目标之一。直接调节p53基因或调节P53和MDM2蛋白质相互作用是再激活p53基因的两种重要机制。对于表达野生型P53的癌症设计小分子阻断剂阻断MDM2与P53蛋白相互作用是一个很有前景的治疗癌症的方向。文章主要总结了作为治疗癌症的新方法-MDM2-P53蛋白相互作用小分子抑制物的最新研究进展，其中最新的是人工合成化合物Nutlin-3和MI-219。

Gene p53, as a tumor suppressor, has become a main target for cancer treatment. Direct regulation of p53 gene and regulation of interaction between p53 and MDM2 proteins are two alternative mechanisms of p53 function. Designing small molecule inhibitors blocking MDM2-P53 interaction is a promising strategy for treatment of cancers containing wild-type p53. Here we conelude the recent development of small-molecule inhibitors, particularly the newly developed two MDM2 inhibitors, named Nutlin-3 and MI-219.