调节器
负调节器
癌症研究
胰腺癌
突变体
平方毫米
免疫沉淀
细胞生物学
生物
化学
癌症
泛素
细胞培养
遗传学
基因
信号转导
作者
Jieqiong Wang,Yajie Chen,Canhua Huang,Qian Hao,Shelya X. Zeng,Sara Omari,Yu Zhang,Xiang Zhou,Hua Lu
出处
期刊:Cancer Research
[American Association for Cancer Research]
日期:2021-06-07
卷期号:81 (15): 4041-4053
被引量:11
标识
DOI:10.1158/0008-5472.can-20-3855
摘要
Approximately 80% of human pancreatic ductal adenocarcinomas (PDAC) harbor TP53 mutations, among which, R273H is the most frequent. Although p53-R273H is known to possess gain-of-function properties, how it is regulated in PDAC has not been extensively explored. Here we identify valosin-containing protein (VCP) as a regulator of p53-R273H by conducting immunoprecipitation-tandem mass spectrometry analysis. VCP bound p53-R273H at its DNA binding domain. Ectopic or endogenous VCP stabilized p53-R273H by binding to MDM2 and disrupting its association with mutant p53. Inhibition of VCP either by genetic depletion or the pharmacologic inhibitor CB-5083 increased ubiquitination and degradation of p53-R273H, leading to cell death. Consistently, ablation of VCP markedly retarded growth of cultured PDAC cells and xenograft PDAC tumors. Together, these results unveil VCP as a novel partner of p53-R273H in promoting PDAC growth and as a potential target for developing anti-PDAC therapy. SIGNIFICANCE: These findings identify valosin-containing protein (VCP) as a novel regulator of p53-R273H stability and suggest VCP as a potential target for development of pancreatic cancer therapy.
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