Despite the potential of PROTACs, limited research has been directed toward the degradation of the p53-R175H mutant protein. In this study, we developed a series of peptide-based PROTACs, leveraging known peptide ligands for both the p53-R175H mutation and the E3 ubiquitin ligase VHL. Our ...
While the prognostic impact of individual TP53 mutations is influenced by the cohort being studied, it has been shown that the R175H mutation is correlated with worse overall survival than wild-type TP53, but is not as detrimental as the R248W variant. This variant is rare in population ...
of oncogenic mutp53 protein will pave way for effective personalized treatment of cancer patients, depending on their p53 mutation status. Methods Cell lines and cell culture HEK293T, SKOV3, and SK-BR-3 cells were purchased from ATCC. TYK-Nu cells were a kind gift from Dr. Hilary Kenny, ...
A mutation within one allele of the p53 tumor suppressor gene can inactivate the remaining wild-type allele in a dominant-negative manner and in some cases can exert an additional oncogenic activity, known as mutant p53 ‘gain of function’ (GOF). To study the role of p53 mutations in prost...
Establishanewmethodtodetectearlystagemutationof TP53(R175H)genebasedonanewgenetransfersystem 研究生姓名** 指导教师姓名**祥副教授 专业名称肿瘤学 研究方向分子诊断学 所在院部苏州大学附属第二医院 论文提交日期2016年5月 建立基于新型基因转换系统的检测TP53基因(R175H)早期突变的新方法中文摘要 ...
The tumor suppressor protein p53 is among the most commonly mutated proteins across a variety of cancer types. Notably, the p53 R175H mutation ranks as one of the most prevalent hotspot mutations. Proteolysis-targeting chimeras (PROTACs) represent a class of bifunctional molecules capable of harness...
we identified BACH1 as a cellular factor that recognizes the p53 DNA-binding domain depending on its mutation status. BACH1 strongly interacts with p53R175Hbut fails to effectively bind wild-type p53 or other hotspot mutants in vivo for functional regulation. Notably, p53R175Hacts as a repress...
(A and B) miR-21 (A) and p53 (B) levels. The cutoff values of miR-21 were 2−ΔΔCt values <10 for low expression and >10 for high expression; the cutoff values of p53 were <3 for low expression and >3 for high expression. Mutation Sites of R175H and R248Q A total of ...
mutation of the hydrophobic FWL (F16A, W20A and L23A) motif within the TA domain result in the formation of open tetramers rendering the C-terminal TI domain accessible for intermolecular interactions.35(b) Co-IP efficiency of the closed dimeric TAp63αwith wtp53 and p53R175H was ...
Rieber M, Strasberg Rieber M: DN-R175H p53 mutation is more effective than p53 interference in inducing epithelial disorganization and activation of proliferation signals in human carcinoma cells: role of E- cadherin. Int J Cancer 2009;125:1604-1612....