WebSep 10, 2024 · Several small molecule antagonists of MDM2 are in clinical trials with promising early results [49], prompting the discovery of dual-specificity peptide antagonists of both MDM2 and MDMX for robust and sustained p53 activation [15,28,29,50]. However, peptide activators of p53 are faced with major pharmacological obstacles in. Materials … WebNov 21, 2013 · Two peptides reported to disrupt the intracellular p53 and MDM2/MDMX interaction were fused to the C-terminal of HSA. Cellular and biochemical studies indicate …
Resurrecting a p53 peptide activator - ScienceDirect
WebDec 1, 2003 · Activation of the p53 protein protects the organism against the propagation of cells that carry damaged DNA with potentially oncogenic mutations. MDM2, a p53-specific E3 ubiquitin ligase, is the principal cellular antagonist of p53, acting to limit the p53 growth-suppressive function in unstressed cells. WebApr 15, 2000 · These peptides compete with p53 for MDM2 binding, whereas a similar peptide containing a phosphorylated serine 20 allows the p53–MDM2 association. While ATM is clearly required to activate p53 in response to ionising radiation, both ATM and ATR fail to phosphorylate p53 residue serine 20 in vitro, indicating that, most likely, this residue … b the succession
p53 programmes plough on - Nature
WebWe identified two angler peptides, cTAT–KD3 and cR10–KD3, able to activate the p53 pathway in cancer cells. cTAT–KD3 entered cells via endocytic pathways, escaped … WebThese results suggest that ArBu could activate ESCC cell apoptosis through activation of p53-dependent pathway. Figure 4 Activation of p53 by ArBu. ... Oelkrug C, Hartke M, Schubert A. Mode of action of anticancer peptides (ACPs) from amphibian origin. Anticancer Res. 2015;35(2):635–643. 3. Webp53 is a potent tumor suppressor, whose biological effects are largely due to its function as a transcriptional regulator. Here we report that, in addition to regulating the expression of hundreds of protein-coding genes, p53 also modulates the levels of microRNAs (miRNAs). Specifically, p53 can induce expression of microRNA-34a (miR-34a) in cultured cells as … b the trader