Breast Cancer Therapy by Small-Molecule Reactivation of Mutant p53 [PDF]
Current OncologyTumor suppressor p53 is essential for maintaining DNA stability and preventing cancer. Under normal conditions, the p53 protein is either degraded or bound to a negative regulator, rendering it inactive, but when DNA damage occurs, p53 is activated ...
Simon H. Slight, Salman M. Hyder
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To target the untargetable: elucidation of synergy of APR-246 and azacitidine in TP53 mutant myelodysplastic syndromes and acute myeloid leukemia [PDF]
Haematologica, 2020 David A. Sallman
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Strong synergy with APR-246 and DNA-damaging drugs in primary cancer cells from patients with TP53 mutant High-Grade Serous ovarian cancer. [PDF]
J Ovarian Res, 2016 Fransson Å +5 more
europepmc +2 more sources
Acta Médica Portuguesa, 2021 Na página 245, cabeçalho do artigo, onde se lê (assinalado a vermelho): “Acta Med Port 2021 Apr;34(3):245-246” Deverá ler-se: “Acta Med Port 2021 Apr;34(4):245-246” Artigo publicado com erros: https://www.actamedicaportuguesa.com/revista/index.php ...
Carla de Sousa
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APR-246 reactivates mutant p53 by targeting cysteines 124 and 277. [PDF]
Cell Death Dis, 2018 Abstract The TP 53 tumor suppressor gene is frequently inactivated in human tumors by missense mutations in the DNA binding domain. TP 53 mutations lead to protein unfolding, decreased thermostability and loss of DNA binding and ...
Zhang Q +3 more
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Correction: APR-246 reactivates mutant p53 by targeting cysteines 124 and 277. [PDF]
Cell Death Dis, 2019 Since publication of this article, the authors have noticed that there was an error in Fig. 1d, third panel from left, “R273H + 200 μM MQ-H” should be “R273H + 200 μM MQ”. Our corrections do not affect the original conclusions of this paper.
Zhang Q +3 more
europepmc +4 more sources
Reactivation of wild-type and mutant p53 by tryptophanolderived oxazoloisoindolinone SLMP53-1:a novel anticancer small-molecule [PDF]
, 2015 Restoration of the p53 pathway, namely by reactivation of mutant (mut) p53, represents a valuable anticancer strategy. Herein, we report the identification of the enantiopure tryptophanol-derived oxazoloisoindolinone SLMP53-1 as a novel reactivator of ...
Bessa, Cláudia +15 more
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Variability in functional p53 reactivation by PRIMA-1(Met)/APR-246 in Ewing sarcoma. [PDF]
Br J Cancer, 2013 Though p53 mutations are rare in ES, there is a strong indication that p53 mutant tumours form a particularly bad prognostic group. As such, novel treatment strategies are warranted that would specifically target and eradicate tumour cells containing mutant p53 in this subset of ES patients.PRIMA-1(Met), also known as APR-246, is a small organic ...
Aryee DN +7 more
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Ascorbate Inhibits Proliferation and Promotes Myeloid Differentiation in TP53-Mutant Leukemia
Frontiers in Oncology, 2021 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
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Data from APR-246 Enhances Colorectal Cancer Sensitivity to Radiotherapy
, 2023 <div>Abstract<p>p53 mutation is common and highly related to radiotherapy resistance in rectal cancer. APR-246, as a small molecule, can restore the tumor-suppressor function to mutant p53. As there is currently no existing study on combining APR-246 with radiation in rectal cancer, our objective was to investigate whether APR-246 could ...
Xiao-Feng Sun +10 more
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