摘要
RITA(reactivation of p53 and induction of tumor cell apoptosis)是经筛选得到的小分子化合物,它主要通过抑制鼠双微体2(murine double minute 2,MDM2)和p53的结合激活p53功能。RITA通过调控细胞内参与细胞增殖、凋亡、衰老和代谢等过程的信号通路,抑制肿瘤的发生和发展,提高耐药细胞对化疗药物的敏感性。本文主要从靶向MDM2和p53结合位点的抑癌小分子概况、RITA的结构与作用机制以及RITA的功能研究进展三个方面进行论述,为进一步推进抑癌小分子化合物RITA在抗肿瘤中发挥作用的研究提供理论参考。
R:ITA(reactivation of p53 and induction of tumor cell apoptosis)is a small molecule compound obtained by screening,which mainly activates p53 by inhibiting the binding of murine double minute 2(MDM2)and p53.RITA inhibits tumorigenesis and development and improves the sensitivity of drug-resistant cells to chemotherapeutic drugs by regulating intracellular signaling pathways involved in cell proliferation,apoptosis,senescence and metabolism.This paper focuses on three aspects of the small molecule profile:cancer suppressor small molecules targeting MDM2 and p53 binding sites,the structure and mechanism of action:RITA,and the progress of functional studies of RITA,to provide theoretical references for further advancing the role of the anticancer small molecule RITA in antitumor research.
作者
史林超
柳辉
SHI Linchao;LIU Hui(Institute of Biophysics,School of Science,Hebei University of Technology,Tianjin 300401,China)
出处
《生命的化学》
CAS
2024年第2期300-306,共7页
Chemistry of Life
基金
国家自然科学基金项目(11547013)。