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

p53-stabilizing Agent CP-31398 Prevents Growth and Invasion of Urothelial Cancer of the Bladder in Transgenic UPII-SV40T Mice

(2015) Venkateshwar Madka et al.   NEOPLASIA

Chemopreventive Effects of the p53-Modulating Agents CP-31398 and Prima-1 in Tobacco Carcinogen-Induced Lung Tumorigenesis in A/J Mice

(2015) Chinthalapally V. Rao et al.   NEOPLASIA

Mutant p53 in Cancer: New Functions and Therapeutic Opportunities

(2014) Patricia A.J. Muller et al.   CANCER CELL

Identification and Characterization of Small Molecules That Inhibit Nonsense-Mediated RNA Decay and Suppress Nonsense p53 Mutations

(2014) L. Martin et al.   CANCER RESEARCH

Drugging the p53 pathway: understanding the route to clinical efficacy

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

Variability in functional p53 reactivation by PRIMA-1Met/APR-246 in Ewing sarcoma

(2013) D N T Aryee et al.   BRITISH JOURNAL OF CANCER

PRIMA-1Met/APR-246 Displays High Antitumor Activity in Multiple Myeloma By Induction of p73 and Noxa

(2013) Manujendra N. Saha et al.   MOLECULAR CANCER THERAPEUTICS

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

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

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

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

PRIMA-1Met/APR-246 induces wild-type p53-dependent suppression of malignant melanoma tumor growth in 3D culture and in vivo

(2011) Wenjie Bao et al.   CELL CYCLE

PRIMA-1Met/APR-246 Induces Apoptosis and Tumor Growth Delay in Small Cell Lung Cancer Expressing Mutant p53

(2011) R. Zandi et al.   CLINICAL CANCER RESEARCH

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

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

SCH529074, a Small Molecule Activator of Mutant p53, Which Binds p53 DNA Binding Domain (DBD), Restores Growth-suppressive Function to Mutant p53 and Interrupts HDM2-mediated Ubiquitination of Wild Type p53

(2010) Mark Demma et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Rescue of non-sense mutated p53 tumor suppressor gene by aminoglycosides

(2010) Célia Floquet et al.   NUCLEIC ACIDS RESEARCH

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

(2010) N Rökaeus et al.   ONCOGENE

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 Drives Invasion by Promoting Integrin Recycling

(2009) Patricia A.J. Muller et al.   CELL

Mutant p53 drives metastasis and overcomes growth arrest/senescence in pancreatic cancer

(2009) J. P. Morton et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A novel p53 rescue compound induces p53-dependent growth arrest and sensitises glioma cells to Apo2L/TRAIL-induced apoptosis

(2008) L Weinmann et al.   CELL DEATH AND DIFFERENTIATION

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

(2008) Nicole Zache et al.   Molecular Oncology

Small-molecule RETRA suppresses mutant p53-bearing cancer cells through a p73-dependent salvage pathway

(2008) J. E. Kravchenko et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeted rescue of a destabilized mutant of p53 by an in silico screened drug

(2008) F. M. Boeckler et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA