APR-246 reactivates mutant p53 by targeting cysteines 124 and 277

The curcumin analog HO-3867 selectively kills cancer cells by converting mutant p53 protein to transcriptionally active wildtype p53

(2018) Esha Madan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

2-Sulfonylpyrimidines: Mild alkylating agents with anticancer activity toward p53-compromised cells

(2016) Matthias R. Bauer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

An open-label phase I dose-finding study of APR-246 in hematological malignancies

(2016) S Deneberg et al.   Blood Cancer Journal

TP53: an oncogene in disguise

(2015) T Soussi et al.   CELL DEATH AND DIFFERENTIATION

Ferroptosis as a p53-mediated activity during tumour suppression

(2015) Le Jiang et al.   NATURE

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

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

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

Drugging the p53 pathway: understanding the route to clinical efficacy

(2014) Kian Hoe Khoo et al.   NATURE REVIEWS DRUG DISCOVERY

Mutational landscape and significance across 12 major cancer types

(2013) Cyriac Kandoth et al.   NATURE

Small molecule induced reactivation of mutant p53 in cancer cells

(2013) Xiangrui Liu et al.   NUCLEIC ACIDS RESEARCH

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

Allele-Specific p53 Mutant Reactivation

(2012) Xin Yu et al.   CANCER 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

Identification of Two Reactive Cysteine Residues in the Tumor Suppressor Protein p53 Using Top-Down FTICR Mass Spectrometry

(2011) Jenna Scotcher et al.   JOURNAL OF THE AMERICAN SOCIETY FOR MASS SPECTROMETRY

The emerging role of p53 in stem cells

(2011) Giuseppina Bonizzi et al.   TRENDS IN MOLECULAR MEDICINE

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

Mutant p53 targeting by the low molecular weight compound STIMA-1

(2008) Nicole Zache et al.   Molecular Oncology