Results 231 to 237 of about 10,910 (237)
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p53 Reactivation by PRIMA-1Met (APR-246) sensitises V600E/KBRAF melanoma to vemurafenib
European Journal of Cancer, 2016Intrinsic and acquired resistance of metastatic melanoma to (V600E/K)BRAF and/or MEK inhibitors, which is often caused by activation of the PI3K/AKT survival pathway, represents a major clinical challenge. Given that p53 is capable of antagonising PI3K/AKT activation we hypothesised that pharmacological restoration of p53 activity may increase the ...
Krayem, Mohammad +10 more
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Abstract 631: Functional genetics of APR-246 rescuable TP53 mutants
Cancer ResearchAbstract TP53, often referred to as the guardian of the genome, encodes for the p53 tumor suppressor protein, and is one of the most frequently mutated genes in human cancers. Some cancer sub-types, such as non-small cell lung carcinoma (NSCLC) and high grade serous carcinoma (HGSC), have high TP53 mutation rates reaching up to 56% and ...
Anais Saunders +4 more
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APR-246, a new class anticancer compound in phase l/lla clinical trials.
Journal of Clinical Oncology, 2010TPS183 Background: APR-246 belongs to a new class of small molecules that is currently being tested in a phase I/IIa clinical trial. The goal of the study is to evaluate safety and pharmacokinetic (PK) properties of APR-246, but efficacy parameters will also be included.
C. Liljebris +5 more
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Blood
Introduction: Cancer cells rely on metabolic reprogramming to meet the increased bioenergetic and biosynthetic demand required for tumor initiation and progression. L-asparaginase (ASNase), an enzymatic drug depleting plasmatic asparagine (ASN), is the only clinically approved targeted therapy of a specific amino ...
Amira Marouf +18 more
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Introduction: Cancer cells rely on metabolic reprogramming to meet the increased bioenergetic and biosynthetic demand required for tumor initiation and progression. L-asparaginase (ASNase), an enzymatic drug depleting plasmatic asparagine (ASN), is the only clinically approved targeted therapy of a specific amino ...
Amira Marouf +18 more
openaire +1 more source
Mechanisms of cancer cell death by mutant p53-reactivating compound APR-246
2021Tumor suppressor TP53 is the most frequently mutated gene in cancer. A majority of TP53 mutations result in a mutant p53 that disrupts its DNA binding capabilities but may also acquire novel gain-of-function activities that contribute to tumor growth.
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903 APR-246 induces an increase in tumor immunogenicity in a p53 independent manner
Regular and Young Investigator Award Abstracts, 2022Divya Venkatesh +9 more
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APR-246 in Combination With Venetoclax and Azacitidine in TP53-Mutant Myeloid Malignancies
Case Medical Research, 2019openaire +1 more source