Drugging p53 in cancer: one protein, many targets

O Hassin, M Oren - Nature Reviews Drug Discovery, 2023 - nature.com
Mutations in the TP53 tumour suppressor gene are very frequent in cancer, and attempts to
restore the functionality of p53 in tumours as a therapeutic strategy began decades ago …

Targeting p53 pathways: mechanisms, structures, and advances in therapy

H Wang, M Guo, H Wei, Y Chen - Signal transduction and targeted …, 2023 - nature.com
The TP53 tumor suppressor is the most frequently altered gene in human cancers, and has
been a major focus of oncology research. The p53 protein is a transcription factor that can …

Modulating ROS to overcome multidrug resistance in cancer

Q Cui, JQ Wang, YG Assaraf, L Ren, P Gupta… - Drug Resistance …, 2018 - Elsevier
The successful treatment of cancer has significantly improved as a result of targeted therapy
and immunotherapy. However, during chemotherapy, cancer cells evolve and can acquire …

Targeting mutant p53 for efficient cancer therapy

VJN Bykov, SE Eriksson, J Bianchi… - Nature Reviews Cancer, 2018 - nature.com
The tumour suppressor gene TP53 is the most frequently mutated gene in cancer. Wild-type
p53 can suppress tumour development by multiple pathways. However, mutation of TP53 …

[HTML][HTML] Mutant p53 as a target for cancer treatment

MJ Duffy, NC Synnott, J Crown - European journal of cancer, 2017 - Elsevier
Abstract TP53 (p53) is the single most frequently altered gene in human cancers, with
mutations being present in approximately 50% of all invasive tumours. However, in some of …

APR-246 induces early cell death by ferroptosis in acute myeloid leukemia

R Birsen, C Larrue, J Decroocq, N Johnson… - …, 2021 - pmc.ncbi.nlm.nih.gov
APR-246 is a promising new therapeutic agent that targets p53 mutated proteins in
myelodysplastic syndromes and in acute myeloid leukemia (AML). APR-246 reactivates the …

TP53 copy number and protein expression inform mutation status across risk categories in acute myeloid leukemia

M Tashakori, T Kadia, S Loghavi… - Blood, The Journal …, 2022 - ashpublications.org
Mutant TP53 is an adverse risk factor in acute myeloid leukemia (AML), but large-scale
integrated genomic-proteomic analyses of TP53 alterations in patients with AML remain …

Targeting p53 in vivo: a first-in-human study with p53-targeting compound APR-246 in refractory hematologic malignancies and prostate cancer

S Lehmann, VJN Bykov, D Ali, O Andrén… - Journal of clinical …, 2012 - ascopubs.org
Purpose APR-246 (PRIMA-1MET) is a novel drug that restores transcriptional activity of
unfolded wild-type or mutant p53. The main aims of this first-in-human trial were to …

Synergistic effects of PRIMA-1Met (APR-246) and 5-azacitidine in TP53-mutated myelodysplastic syndromes and acute myeloid leukemia

N Maslah, N Salomao, L Drevon, E Verger… - …, 2019 - pmc.ncbi.nlm.nih.gov
Myelodysplastic syndromes and acute myeloid leukemia with TP53 mutations are
characterized by frequent relapses, poor or short responses, and poor survival with the …

[HTML][HTML] Mutant p53 reactivation by small molecules makes its way to the clinic

VJN Bykov, KG Wiman - FEBS letters, 2014 - Elsevier
The TP53 tumor suppressor gene is mutated in many human tumors, including common
types of cancer such as colon and ovarian cancer. This illustrates the key role of p53 as …