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目的介绍以p53与人双微基因2(HDM2)结合为靶点的小分子抑制剂作为抗肿瘤候选药物的研究进展。方法查阅国内外有关文献,总结、归纳已报道的小分子抑制剂的作用特点及化学特征。结果与结论小分子抑制剂作用特点:可以模拟p53与HDM2结合,或抑制p53-HDM2复合物泛素化,或抑制HDM2的异常表达,将p53从HDM2的控制中释放出来,激活p53通路,达到抑制肿瘤细胞生长和诱导其凋亡的作用;按结构主要分为:Nutlin系列;螺环羟吲哚类;苯并二氮类;查尔酮类;降莰烷类;磺胺类;异吲哚酮类;羟基喹啉类;RITA;5-去氮杂黄素类;藤黄酸;姜黄素;模拟p53多肽类等。
Objective To introduce the research progress of small molecule inhibitors targeting p53 and human double micro-gene 2 (HDM2) as antitumor drug candidates. Methods Access to relevant literature at home and abroad, summarizes and summarizes the reported characteristics and chemical characteristics of small molecule inhibitors. RESULTS AND CONCLUSION: The small molecule inhibitors can be used to mimic p53 binding to HDM2, inhibit ubiquitination of p53-HDM2 complex, inhibit the abnormal expression of HDM2, release p53 from HDM2 and activate p53 pathway Inhibition of tumor cell growth and induction of apoptosis; according to the structure is divided into: Nutlin series; spirocyclic oxindoles; benzodiazepines; chalcones; norbornane; sulfonamides; isoindole Hydroxyquinolines, RITA, 5-deazaxanthones, gambogic acid, curcumin, mimicking p53 polypeptides, and the like.