Here, we demonstrate that gain-of-function (GOF) p53 protein can be packaged into small EVs and transferred to fibroblasts. GOF p53 protein is selectively bound by heat shock protein 90 (HSP90), a chaperone protein, and packaged into small EVs. Inhibition of HSP90 activity blocks packaging ...
1.《Drugging p53 in cancer: one protein, many targets》, 2022, Nature Reviews Drug Discovery 2.《p53 signaling in cancer progression and therapy》, 2021, BMC 3.《Heterogeneity of TP53 Mutations and P53 Protein Residual Function in Cancer: Does It Matter?》, 2020, Frontiers in Oncology 4.《...
As p53 is such a potent inhibitor of cell growth, its function must be tightly controlled to allow normal growth development. This is achieved through several mechanisms that include regulation of p53 transcription and translation, protein stability, subcellular localization and activity [19]. Rapid ...
little is known about p53 turnover through proteasome-independent pathway(s). The digestive organ expansion factor (Def) protein is essential for the development of digestive organs. In zebrafish, loss of function of def selectively upregulates the expression...
英文名称Anti-P53 protein(wt-p53) 中文名称抑制基因P53蛋白抗体(野生型P53)费用 别名Widespread p53; Wtp53; Antigen NY-CO-13; Cellular tumor antigen p53; Cys 51 Stop; HGNC11998; LFS1; p53; p53 Cellular Tumor Antigen; p53 Tumor Suppressor; Phosphoprotein p53; TP53; Transformation related protein ...
然而,PPI(protein-protein interaction)抑制剂的开发是很困难的一件事情。小分子难以结合在两个蛋白之间...
unlike the wild–type p53 protein, could also enhance the expression of a test gene regulated by the multi–drug resistance enhancer–promoter element. These data demonstrate a gain of function associated with p53 mutations in addition to the loss of function shown previously to be associated with...
Covalent modification adding acetyl groups to the C terminus of the p53 protein has been suggested to be required for its functional activation as a tumour suppressor. However, it remains largely unknown how p53 acetylation is deregulated in colorectal cancer (CRC), which is the third most commonl...
此泛素化过程依赖于MDM2和p53的直接结合,因此开发MDM2抑制剂,阻断MDM2-p53 PPI (protein-protein interaction)作用成为主流策略。RG7112、APG-115、AMG-232等MDM2纷纷进入临床,但最大的挑战是获得性耐药和由于p53分布广泛性而带来的毒性。目前对这两个问题的解决建议分别是将MDM2抑制剂与传统化疗药或其他靶向药联用,...
被称为金属伴侣(metallochaperons)的药物能够帮助展开的蛋白(unfolded protein)与锌离子结合并且形成一个较为正常的构像,从而恢复与DNA结合的能力。而另一种策略利用了一个意想不到的发现,那就是有些p53突变蛋白有形成像淀粉样蛋白一样的聚合物的倾向,当聚合过程被扰乱后,p53的功能可以得到恢复并且在异种移植模型中...