APR-246 Enhances Colorectal Cancer Sensitivity to Radiotherapy. [PDF]
Mol Cancer Ther, 2023 Abstract 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 ...
Xie X +10 more
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APR-246 alone and in combination with a phosphatidylserine-targeting antibody inhibits lung metastasis of human triple-negative breast cancer cells in nude mice [PDF]
Breast Cancer: Targets and Therapy, 2019 Yayun Liang,1 Cynthia Besch-Williford,2 Matthew T Cook,3 Anthony Belenchia,4 Rolf A Brekken,5 Salman M Hyder11Department of Biomedical Sciences and Dalton Cardiovascular Research Center, University of Missouri, Columbia, MO, USA; 2IDEXX BioAnalytics ...
Liang Y +5 more
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APR-246 induces ferroptosis and overcomes cisplatin resistance in ovarian cancer [PDF]
Summer Experience 2022, 2022 https://openworks.mdanderson.org/sumexp22/1137/thumbnail ...
Ayres, Mary +5 more
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PB1913: SYNERGISTIC EFFECTS OF DECITABINE AND APR-246 IN TP53 P.248Q-MUTATED MYELODYSPLASTIC SYNDROME [PDF]
HemaSphere, 2022 Y. Fang, C.-K. Chang
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Eprenetapopt (APR-246) and Azacitidine in TP53-Mutant Myelodysplastic Syndromes. [PDF]
J Clin Oncol, 2021 PURPOSE Approximately 20% of patients with TP53-mutant myelodysplastic syndromes (MDS) achieve complete remission (CR) with hypomethylating agents. Eprenetapopt (APR-246) is a novel, first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells.
Sallman DA +23 more
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Correction: Mutant p53-reactivating compound APR-246 synergizes with asparaginase in inducing growth suppression in acute lymphoblastic leukemia cells [PDF]
Cell Death and Disease, 2022 Sophia Ceder +12 more
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APR-246/PRIMA-1MET inhibits thioredoxin reductase 1 and converts the enzyme to a dedicated NADPH oxidase. [PDF]
Cell Death Dis, 2013 A large fraction of human tumors carry inactivating mutations in the TP53 tumor suppressor gene. Approximately 75% of these mutations are missense mutations and around 10% are nonsense mutations.
Peng X +7 more
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Combining APR-246 and HDAC-Inhibitors: A Novel Targeted Treatment Option for Neuroblastoma. [PDF]
Cancers (Basel), 2021 APR-246 (Eprenetapopt/PRIMA-1Met) is a very potent anti-cancer drug in clinical trials and was initially developed as a p53 refolding agent. As an alternative mode of action, the elevation of reactive oxygen species (ROS) has been proposed. Through an in silico analysis, we investigated the responses of approximately 800 cancer cell lines (50 entities;
Müller M +16 more
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Ovarian Cancers with Low CIP2A Tumor Expression Constitute an APR-246-Sensitive Disease Subtype. [PDF]
Mol Cancer Ther, 2022 Abstract Identification of ovarian cancer patient subpopulations with increased sensitivity to targeted therapies could offer significant clinical benefit. We report that 22% of the high-grade ovarian cancer tumors at diagnosis express CIP2A oncoprotein at low levels.
Cvrljevic AN +15 more
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Mutant p53 gain of function mediates cancer immune escape that is counteracted by APR-246. [PDF]
Br J Cancer, 2022 AbstractBackgroundp53 mutants contribute to the chronic inflammatory tumour microenvironment (TME). In this study, we address the mechanism of how p53 mutants lead to chronic inflammation in tumours and how to transform it to restore cancer immune surveillance.MethodsOur analysis of RNA-seq data from The Cancer Genome Atlas Breast Invasive Carcinoma ...
Zhou X +9 more
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