Allele-specific p53 mutant reactivation
WebJun 29, 2012 · Mutant tumour suppressor p53 proteins are expressed in and regulate tumour biology in many human cancers, and so restoration of p53 function could be a … WebJul 10, 2012 · The identification of thiosemicarbazone compounds as selective inhibitors of p53-mutant cells that restore wild-type p53 structure and function suggests that targeting specific p53 mutant alleles may be a viable therapeutic option. Yu X, Vazquez A, Levine AJ, Carpizo DR. Allele-specific p53 mutant reactivation. Cancer Cell 2012;21:614–25.
Allele-specific p53 mutant reactivation
Did you know?
WebPRIMA-1 (p53 reactivation and induction of mass apoptosis) was identified as a non-toxic, low-molecular weight compound that causes mtp53 protein to undergo conformational change that facilitates its binding to DNA in a sequence-specific manner in order to induce apoptosis. 16,20 PRIMA-1 was shown to preferentially induce cell cycle arrest and ... WebSep 15, 2024 · Interestingly, a majority (74%) of these TP53 mutations are specific missense mutations that occur at six hotspot residues (R175, G245, R248, R249, R273, and R282) within the p53 DNA-binding region. Missense mutations in p53 generate a defective but abundant p53 protein ( Sigal and Rotter, 2000 ).
WebMay 25, 2012 · Mechanistic studies reveal that NSC319726 restores WT structure and function to the p53 (R175) mutant. This compound kills p53 (R172H) knockin mice with … WebAug 19, 2014 · Most TP53 mutations are missense mutations that result in single amino acid substitutions in p53 and expression of high levels of dysfunctional p53 protein. …
WebApr 27, 2013 · Most p53 mutations are missense mutations in its DNA-binding (also called core) domain, which can be divided into two classes: contact mutations that interfere with p53-DNA contacts, and structural mutations that destabilize the protein, causing it to unfold and aggregate rapidly at physiological conditions ( 6 ).
WebFeb 14, 2024 · Categorizing the spectrum of p53 mutations into discrete classes based on their inactivation mechanisms is the initial step toward personalized cancer therapy …
WebJan 9, 2024 · The tumor suppressor p53 is the most mutated gene in cancer, and yet no therapeutics to date directly target the mutated protein to rescue wild-type function. In this study, we identify the first allele-specific compound that selectively reacts with the cysteine p53 Y220C to rescue wild-type thermal … is stray kids going on tour 2022WebNov 18, 2024 · The tumor suppressor gene TP53 is the most frequently mutated gene in human cancers. Approximately 80% of TP53 mutations are missense mutations … iforward logoWebWhile the authors present a series of data to show that the compounds can restore the activity of p53 (R175H) mutant in vitro and in vivo, like many previous studies of this … iforward school calendarWebTP53 is the most frequently mutated gene in a large fraction of human cancers. Interestingly, a majority (74%) of these TP53 mutations are specific missense mutations that occur at … is stray on nintendoWebApr 11, 2024 · HMTEVVRHC peptide (mutant amino acid underlined), derived from p53-R175H mutant, binds to the HLA allele A*02:01 that is present in more than 40% of U.S. Caucasians [139,141]. Very recently, Han-Chung Hsiue et al. described the development of a TCR-mimic antibody highly specific to the HLA A*02:01-restricted p53-R175H-derived … iforward online school wisconsinWebAug 27, 2015 · Thus, CTM acts as a specific reactivator of the p53 R175H mutant form through Hsp40. These results provide new insights into the mechanism of reactivation of this specific p53 mutant. Show less is stray on nintendo switchWebMay 1, 2012 · The Cancer Institute of New Jersey, New Brunswick, NJ 08903, USA; Institute for Advanced Study, Princeton, NJ 08540, USA; Department of Pediatrics, … i forward sono