APR-246 induces apoptosis and enhances chemo-sensitivity via activation of ROS and TAp73-Noxa signal in oesophageal squamous cell cancer with TP53 missense mutation.
Sign Up to like & getrecommendations! Published in 2021 at "British journal of cancer"
DOI: 10.1038/s41416-021-01561-0
Abstract: BACKGROUND Mutations in p53, identified in 90% of oesophageal squamous cell carcinoma (ESCC), are associated with unfavourable prognosis and chemo-resistance. APR-246 induces apoptosis by restoring transcriptional ability of mutant p53, and may be a promising… read more here.
Keywords: apr 246; apoptosis; oesophageal squamous; missense ... See more keywords
Ovarian cancers with low CIP2A tumor expression constitute an APR-246 sensitive disease subtype.
Sign Up to like & getrecommendations! Published in 2022 at "Molecular cancer therapeutics"
DOI: 10.1158/1535-7163.mct-21-0622
Abstract: Identification of ovarian cancer (OvCa) patient subpopulations with increased sensitivity to targeted therapies could offer significant clinical benefit. We report that 22 % of the high grade OvCa tumors at diagnosis express CIP2A oncoprotein at… read more here.
Keywords: disease; apr 246; cip2a deficient; tumor ... See more keywords
APR-246 enhances colorectal cancer sensitivity to radiotherapy.
Sign Up to like & getrecommendations! Published in 2023 at "Molecular cancer therapeutics"
DOI: 10.1158/1535-7163.mct-22-0275
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. There is no study on combining APR-246 with radiation… read more here.
Keywords: apr 246; colorectal cancer; combination treatment; rectal cancer ... See more keywords
Impact of combined MRP1 inhibition and mutant p53-targeting compound APR-246.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2019.37.15_suppl.e14712
Abstract: e14712 Background: The tumor suppressor gene TP53 is the most frequently mutated gene in cancer. Mutant p53 protein is often expressed at high levels and accompanied with gain-of-function activities that promote tumor development and resistance… read more here.
Keywords: apr 246; p53; mrp1 inhibition; mutant p53 ... See more keywords
PARP-1 inhibitors sensitize HNSCC cells to APR-246 by inactivation of thioredoxin reductase 1 (TrxR1) and promotion of ROS accumulation
Sign Up to like & getrecommendations! Published in 2018 at "Oncotarget"
DOI: 10.18632/oncotarget.21277
Abstract: Head and neck squamous cell carcinoma (HNSCC) is the sixth most common cancer worldwide. Mutations of TP53 may reach 70% - 85% in HNSCC patients without human papillomavirus (HPV) infection. Recurrence rate remains particularly high… read more here.
Keywords: apr 246; hnscc cells; trxr1; inactivation ... See more keywords
Therapeutic targeting of mutant p53 in pediatric acute lymphoblastic leukemia
Sign Up to like & getrecommendations! Published in 2019 at "Haematologica"
DOI: 10.3324/haematol.2018.199364
Abstract: Alterations of the tumor suppressor gene TP53 are found in different cancers, in particular in carcinomas of adults. In pediatric acute lymphoblastic leukemia (ALL), TP53 mutations are infrequent but enriched at relapse. As in most… read more here.
Keywords: apr 246; mutant p53; p53; pediatric acute ... See more keywords
Immunotherapy against the Cystine/Glutamate Antiporter xCT Improves the Efficacy of APR-246 in Preclinical Breast Cancer Models
Sign Up to like & getrecommendations! Published in 2022 at "Biomedicines"
DOI: 10.3390/biomedicines10112843
Abstract: Breast cancer is the most frequent cancer in women. Despite recent clinical advances, new therapeutic approaches are still required. The cystine-glutamate antiporter xCT, encoded by the SLC7A11 gene, which imports cystine in exchange with glutamate,… read more here.
Keywords: glutamate; apr 246; breast cancer; xct ... See more keywords
Targeted Therapy with PI3K, PARP, and WEE1 Inhibitors and Radiotherapy in HPV Positive and Negative Tonsillar Squamous Cell Carcinoma Cell Lines Reveals Synergy while Effects with APR-246 Are Limited
Sign Up to like & getrecommendations! Published in 2022 at "Cancers"
DOI: 10.3390/cancers15010093
Abstract: Simple Summary Human papillomavirus positive tonsillar and base of tongue cancers are rising in incidence but chemoradiotherapy has not improved survival, so novel treatments are needed. Therefore, targeted therapy with phosphoinositide 3-kinase, poly-ADP-ribose-polymerase, and WEE1… read more here.
Keywords: cell; targeted therapy; apr 246; bmn 673 ... See more keywords
Therapeutic Targeting of P53: A Comparative Analysis of APR-246 and COTI-2 in Human Tumor Primary Culture 3-D Explants
Sign Up to like & getrecommendations! Published in 2023 at "Genes"
DOI: 10.3390/genes14030747
Abstract: Background: TP53 is the most commonly mutated gene in human cancer with loss of function mutations largely concentrated in “hotspots” affecting DNA binding. APR-246 and COTI-2 are small molecules under investigation in P53 mutated cancers.… read more here.
Keywords: apr 246; activity; p53; 246 coti ... See more keywords
p53 reactivating small molecule PRIMA‑1MET/APR‑246 regulates genomic instability in MDA‑MB‑231 cells.
Sign Up to like & getrecommendations! Published in 2022 at "Oncology reports"
DOI: 10.3892/or.2022.8296
Abstract: Pharmacological reactivation of tumor‑suppressor protein p53 has acted as a promising strategy for more than 50% of human cancers that carry a non‑functional mutant p53 (mutp53). p53 plays a critical role in preserving genomic integrity… read more here.
Keywords: genomic instability; apr 246; p53; mda 231 ... See more keywords