Targeting of Mutant p53 and the Cellular Redox Balance by APR-246 as a Strategy for Efficient Cancer Therapy

APR-246 potently inhibits tumour growth and overcomes chemoresistance in preclinical models of oesophageal adenocarcinoma

(2015) David S H Liu et al.   GUT

APR-246 overcomes resistance to cisplatin and doxorubicin in ovarian cancer cells

(2015) N Mohell et al.   Cell Death & Disease

Small molecule restoration of wildtype structure and function of mutant p53 using a novel zinc-metallochaperone based mechanism

(2015) Xin Yu et al.   Oncotarget

PRIMA-1Met induces myeloma cell death independent of p53 by impairing the GSH/ROS balance

(2014) B. Tessoulin et al.   BLOOD

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

(2014) Vladimir J.N. Bykov et al.   FEBS LETTERS

PRIMA-1, a mutant p53 reactivator, induces apoptosis and enhances chemotherapeutic cytotoxicity in pancreatic cancer cell lines

(2014) Patricia Izetti et al.   INVESTIGATIONAL NEW DRUGS

Mutational landscape and significance across 12 major cancer types

(2013) Cyriac Kandoth et al.   NATURE

Modulation of oxidative stress as an anticancer strategy

(2013) Chiara Gorrini et al.   NATURE REVIEWS DRUG DISCOVERY

Small molecule induced reactivation of mutant p53 in cancer cells

(2013) Xiangrui Liu et al.   NUCLEIC ACIDS RESEARCH

Impaired epithelial differentiation of induced pluripotent stem cells from ectodermal dysplasia-related patients is rescued by the small compound APR-246/PRIMA-1MET

(2013) R. Shalom-Feuerstein et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

APR-246/PRIMA-1MET rescues epidermal differentiation in skin keratinocytes derived from EEC syndrome patients with p63 mutations

(2013) J. Shen et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

APR-246/PRIMA-1MET inhibits thioredoxin reductase 1 and converts the enzyme to a dedicated NADPH oxidase

(2013) X Peng et al.   Cell Death & Disease

Computational identification of a transiently open L1/S3 pocket for reactivation of mutant p53

(2013) Christopher D. Wassman et al.   Nature Communications

PRIMA-1 increases cisplatin sensitivity in chemoresistant ovarian cancer cells with p53 mutation: a requirement for Akt down-regulation

(2013) Noriko Kobayashi et al.   Journal of Ovarian Research

p53 Efficiently Suppresses Tumor Development in the Complete Absence of Its Cell-Cycle Inhibitory and Proapoptotic Effectors p21, Puma, and Noxa

(2013) Liz J. Valente et al.   Cell Reports

Hypoxia, Mn-SOD and H2O2 regulate p53 reactivation and PRIMA-1 toxicity irrespective of p53 status in human breast cancer cells

(2012) Manuel Rieber et al.   BIOCHEMICAL PHARMACOLOGY

Tumor Suppression in the Absence of p53-Mediated Cell-Cycle Arrest, Apoptosis, and Senescence

(2012) Tongyuan Li et al.   CELL

Targeting p53 in Vivo: A First-in-Human Study With p53-Targeting Compound APR-246 in Refractory Hematologic Malignancies and Prostate Cancer

(2012) Sören Lehmann et al.   JOURNAL OF CLINICAL ONCOLOGY

The Effect of Adenovirus-Mediated Gene Expression of FHIT in Small Cell Lung Cancer Cells

(2011) Roza Zandi et al.   CANCER INVESTIGATION

APR-246 exhibits anti-leukemic activity and synergism with conventional chemotherapeutic drugs in acute myeloid leukemia cells

(2010) Dina Ali et al.   EUROPEAN JOURNAL OF HAEMATOLOGY

PRIMA-1MET/APR-246 targets mutant forms of p53 family members p63 and p73

(2010) N Rökaeus et al.   ONCOGENE

Phosphate-activated glutaminase (GLS2), a p53-inducible regulator of glutamine metabolism and reactive oxygen species

(2010) S. Suzuki et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Glutaminase 2, a novel p53 target gene regulating energy metabolism and antioxidant function

(2010) W. Hu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Stabilization of mutant p53 via alkylation of cysteines and effects on DNA binding

(2010) Joel L. Kaar et al.   PROTEIN SCIENCE

PRIMA-1 Reactivates Mutant p53 by Covalent Binding to the Core Domain

(2009) Jeremy M.R. Lambert et al.   CANCER CELL

Blinded by the Light: The Growing Complexity of p53

(2009) Karen H. Vousden et al.   CELL

Mechanisms of Resistance to Imatinib and Second-Generation Tyrosine Inhibitors in Chronic Myeloid Leukemia

(2009) D. Milojkovic et al.   CLINICAL CANCER RESEARCH

Molecular Mechanisms of Thioredoxin and Glutaredoxin as Hydrogen Donors for Mammalian S Phase Ribonucleotide Reductase

(2009) Farnaz Zahedi Avval et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

An Oncogene-Induced DNA Damage Model for Cancer Development

(2008) T. D. Halazonetis et al.   SCIENCE