p53蛋白是一种转录因子，通常分为三个功能区：氨基末端结构域、DNA结合域和羧基末端结构域。野生型p53(wt p53)通过调控多个靶基因的转录，在许多重要的生物学过程中发挥关键作用。

R175H and R273H are more prone to aggregation than wild-type (WT) p53, and their pathological aggregation can lead to various cancers. A recent study investigated the dynamic and structural properties of the R175H and R273H mutants in the p53 core domain (p53C) using extensive all-atom molecular dynamics simulations.

2021年5月25日 · Here, we reported that a new quinolone compound RYL-687 significantly inhibited non-small cell lung cancer (NSCLC) cells which express wild type (wt) p53, in contract to its much weaker...

p53蛋白是细胞周期中的关键蛋白之一，针对DNA损伤，p53 WT可以激活p21，进而阻滞G1期来促进DNA损伤的修复。 在p53突变的情况下，癌细胞更多地依赖于阻滞S期和G2期来进行 DNA 修复。

在含有p53错义突变的肿瘤中，apr-246、coti-2 和pat等能够恢复许多p53突变体的wt构象。 特定的药物如 PhiKan083 、 PK7088 和 MS78 则针对p53 Y220C突变，而 ZMC1 用于p53 R175H突变。

2024年5月9日 · Here, we review the complexity of different layers of p53 regulation, and the recent advance of the p53 pathway in metabolism, ferroptosis, immunity, and others that contribute to tumor suppression.

2024年3月28日 · However, when bona fide wild-type (WT) p53 was finally tested, it not only failed to elicit oncogenic transformation of cultured cells—it actually potently suppressed transformation driven by classical oncoproteins, including MYC and RAS. Hence, authentic WT p53 behaved as a tumor suppressor, not an oncoprotein .

In contrast, knockdown of p53 using two independent siRNAs significantly reduced the expression of circASCC3 and ASCC3 in cancer cells when treated with Cisplatin or Nutlin-3 (Fig. 2 E–G and SI Appendix, Fig. S2 B–D). We also tested whether WT p53 was required for this regulation by employing cancer cells without p53 or expressing a mutant p53.

2018年8月8日 · Human p53 protein acts as a transcription factor predominantly in a tetrameric form. Single residue changes, caused by hot-spot mutations of the TP53 gene in human cancer, transform wild-type (wt) p53 tumor suppressor proteins into potent oncoproteins - with gain-of-function, tumor-promoting activity. Oligomerization of p53 allows for a direct ...

p53 consists of 393 amino acids, which has a molecular weight of approximately 53 KD. p53 has seven major functional domains. The central DNA binding domain (DBD) and the regulatory C-terminal domain (CTD) mediate the binding of p53 to DNA. The oligomerization domain (OD) is required for the formation of p53 tetramers, which is a prerequisite ...