Advances in inhibitors of MDM2 and MDM4

VernacularTitle:MDM2与MDM4抑制剂的研究进展
Author: Chunhong LI ¹ ; Hongjin DU ; Xiao′an WEN ; Hongbin SUN
Author Information

1. 中国药科大学新药研究中心，江苏省代谢性疾病药物重点实验室，天然药物活性组分与药效国家重点实验室
Publication Type:Journal Article
Keywords: MDM2; MDM4; inhibitor; p53; anti-tumor drug; advances
From: Journal of China Pharmaceutical University 2015;46(1):1-15
CountryChina
Language:Chinese
Abstract: The protein p53 plays an important role in the regulation of DNA repair, cell cycle arrest, apoptosis, senescence, autophagy and metabolism. MDM2 and MDM4 are the key negative regulatory proteins of p53. Inhibition of MDM2 and MDM4 has become a research hotspot in cancer therapy. Currently, seven MDM2 inhibitors(RG7112, MI-77301, RG7388, AMG232, CGM097, MK-8242, DS-3032b)and one MDM2/MDM4 dual inhibitor(ALRN-6924)have entered clinical trials. This paper highlights small molecule discovery, pharmacological activities and clinical research advances of MDM2 inhibitors in clinical trials, in addition, this review introduces research advances of MDM2/MDM4 dual inhibitors.