MicroRNA-29a plays a prominent role in PRIMA-1Met-induced apoptosis in ovarian cancer cells [PDF]
The structural analog of the small 2,2-bis(hydroxymethyl)-1-azabicyclo[2,2,2]octan-3-one molecule named PRIMA-1Metfor “p53 reactivation and induction of massive apoptosis” has been shown to inhibit cell growth and induce apoptosis in human tumor cells by
İmir Nilüfer Gülmen
doaj +4 more sources
Rescue of mutant p53 family members by the low molecular weight compound PRIMA-1MET/ APR-246 [PDF]
The tumor suppressor p53, guardian of the genome, is induced and activated by cellular stress signals such as DNA damage, hypoxia and activation of oncogenes. p53 upregulates downstream target genes, that are involved in cell cycle arrest, senescence,
Shen, Jinfeng
core +9 more sources
PRIMA-1MET induces nucleolar translocation of Epstein-Barr virus-encoded EBNA-5 protein [PDF]
Abstract The low molecular weight compound, PRIMA-1MET restores the transcriptional transactivation function of certain p53 mutants in tumor cells. We have previously shown that PRIMA-1MET induces nucleolar translocation of p53, PML, CBP and Hsp70.
Elena Kashuba, Klas G Wiman
exaly +6 more sources
Upgrade of an old drug: Auranofin in innovative cancer therapies to overcome drug resistance and to increase drug effectiveness [PDF]
Auranofin is an oral gold(I) compound, initially developed for the treatment of rheumatoid arthritis. Currently, Auranofin is under investigation for oncological application within a drug repurposing plan due to the relevant antineoplastic activity ...
Chiappetta, G. +5 more
core +4 more sources
Synergistic Antitumor Effect of BKM120 with Prima-1Met Via Inhibiting PI3K/AKT/mTOR and CPSF4/hTERT Signaling and Reactivating Mutant P53 [PDF]
Background/Aims: PI3KCA and mutant p53 are associated with tumorigenesis and the development of cancers. NVP-BKM120, a selective pan-PI3K inhibitor, exerts the antitumor activity by suppressing the PI3K signaling pathway.
Zongjuan Li +16 more
doaj +3 more sources
PRIMA-1met (APR-246) inhibits growth of colorectal cancer cells with different p53 status through distinct mechanisms. [PDF]
PRIMA-1met (APR-246) is a methylated derivative and structural analog of PRIMA-1 (p53 re-activation and induction of massive apoptosis). PRIMA-1met has been reported to restore both the wild type (wt) structure and function of mutant p53. Here, we show that PRIMA-1met is highly effective at limiting the growth of CRC cells regardless of p53 status ...
Li XL +5 more
europepmc +4 more sources
Improvement of epidermal covering on AEC patients with severe skin erosions by PRIMA-1MET/APR-246. [PDF]
AbstractP63 is a major transcription factor regulating skin development and homeostasis. It controls many genes involved in cell proliferation, adhesion, and early differentiation. P63 is mutated in several rare syndromes called p63-related ectodermal dysplasia syndromes (ED).
Aberdam E +11 more
europepmc +5 more sources
Ascorbate Inhibits Proliferation and Promotes Myeloid Differentiation in TP53-Mutant Leukemia
Loss-of-function mutations in the DNA demethylase TET2 are associated with the dysregulation of hematopoietic stem cell differentiation and arise in approximately 10% of de novo acute myeloid leukemia (AML). TET2 mutations coexist with other mutations in
Carlos C. Smith-Díaz +5 more
doaj +1 more source
PRIMA-1MET Induces Cellular Senescence and Apoptotic Cell Death in Cholangiocarcinoma Cells. [PDF]
This study examined the in vitro effects of the bile duct cancer drug PRIMA-1MET on cholangiocarcinoma (CCA) cell growth to determine its potential usefulness in CCA therapy.The effect of this drug on the expression of senescent markers (p16INK4A and p21) and the phosphorylation of p53 was investigated, as was the association between senescent markers ...
Piyawajanusorn C +5 more
europepmc +4 more sources
Mutant p53 reactivation by PRIMA-1MET induces multiple signaling pathways converging on apoptosis [PDF]
The low molecular weight compound PRIMA-1(MET) reactivates mutant p53 and triggers mutant p53-dependent apoptosis in human tumor cells. We investigated the effect of PRIMA-1(MET) on global gene expression using microarray analysis of Saos-2 cells expressing His273 mutant p53 and parental p53 null Saos-2 cells.
J M R, Lambert +4 more
openaire +2 more sources

