PRIMA-1 and PRIMA-1Met (APR-246): From Mutant/Wild Type p53 Reactivation to Unexpected Mechanisms Underlying Their Potent Anti-Tumor Effect in Combinatorial Therapies

P53 and MITF/Bcl-2 identified as key pathways in the acquired resistance of NRAS-mutant melanoma to MEK inhibition

(2017) Ahmad Najem et al.   EUROPEAN JOURNAL OF CANCER

Inhibiting the system xC−/glutathione axis selectively targets cancers with mutant-p53 accumulation

(2017) David S. Liu et al.   Nature Communications

Hypoxic resistance of KRAS mutant tumor cells to 3-Bromopyruvate is counteracted by Prima-1 and reversed by N-acetylcysteine

(2016) Andrea Orue et al.   BMC CANCER

Anti-leukaemic effects induced by APR-246 are dependent on induction of oxidative stress and the NFE2L2/HMOX1 axis that can be targeted by PI3K and mTOR inhibitors in acute myeloid leukaemia cells

(2016) Dina Ali et al.   BRITISH JOURNAL OF HAEMATOLOGY

APR-246 (PRIMA-1 MET ) strongly synergizes with AZD2281 (olaparib) induced PARP inhibition to induce apoptosis in non-small cell lung cancer cell lines

(2016) Christophe Deben et al.   CANCER LETTERS

p53 Reactivation by PRIMA-1Met (APR-246) sensitises V600E/KBRAF melanoma to vemurafenib

(2016) Mohammad Krayem et al.   EUROPEAN JOURNAL OF CANCER

TP53Variations in Human Cancers: New Lessons from the IARC TP53 Database and Genomics Data

(2016) Liacine Bouaoun et al.   HUMAN MUTATION

Mutant p53: a novel target for the treatment of patients with triple-negative breast cancer?

(2016) N.C. Synnott et al.   INTERNATIONAL JOURNAL OF CANCER

PRIMA-1MET induces apoptosis through accumulation of intracellular reactive oxygen species irrespective of p53 status and chemo-sensitivity in epithelial ovarian cancer cells

(2016) NOBUHISA YOSHIKAWA et al.   ONCOLOGY REPORTS

Strong synergy with APR-246 and DNA-damaging drugs in primary cancer cells from patients with TP53 mutant High-Grade Serous ovarian cancer

(2016) Åsa Fransson et al.   Journal of Ovarian Research

miRNA-29a as a tumor suppressor mediates PRIMA-1Met-induced anti-myeloma activity by targeting c-Myc

(2016) Manujendra N. Saha et al.   Oncotarget

Sensitivity to PRIMA-1MET is associated with decreased MGMT in human glioblastoma cells and glioblastoma stem cells irrespective of p53 status

(2016) Mariia Patyka et al.   Oncotarget

PRIMA-1 targets the vulnerability of multiple myeloma of deregulated protein homeostasis through the perturbation of ER stress via p73 demethylation

(2016) Phaik Ju Teoh et al.   Oncotarget

PRIMA-1Met suppresses colorectal cancer independent of p53 by targeting MEK

(2016) Tao Lu et al.   Oncotarget

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

(2016) Vladimir J. N. Bykov et al.   Frontiers in Oncology

PRIMA-1MET induces death in soft-tissue sarcomas cell independent of p53

(2015) Thomas Grellety et al.   BMC CANCER

PRIMA-1Met induces apoptosis in Waldenström's Macroglobulinemia cells independent of p53

(2015) Mona Sobhani et al.   CANCER BIOLOGY & THERAPY

Stimulation of Suicidal Erythrocyte Death by PRIMA-1

(2015) Caterina Faggio et al.   CELLULAR PHYSIOLOGY AND BIOCHEMISTRY

Silencing of CD24 Enhances the PRIMA-1-Induced Restoration of Mutant p53 in Prostate Cancer Cells

(2015) W. Zhang et al.   CLINICAL CANCER RESEARCH

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

(2015) David S H Liu et al.   GUT

Zn(II)-curc targets p53 in thyroid cancer cells

(2015) ALESSIA GARUFI et al.   INTERNATIONAL JOURNAL OF ONCOLOGY

3-BrPA eliminates human bladder cancer cells with highly oncogenic signatures via engagement of specific death programs and perturbation of multiple signaling and metabolic determinants

(2015) Eumorphia G. Konstantakou et al.   Molecular Cancer

CRISPR-Cas9–based target validation for p53-reactivating model compounds

(2015) Michael Wanzel et al.   Nature Chemical Biology

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

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

PRIMA-1met (APR-246) inhibits growth of colorectal cancer cells with different p53 status through distinct mechanisms

(2015) Xiao-Lan Li et al.   Oncotarget

Involvement of p53 in insulin-like growth factor binding protein-3 regulation in the breast cancer cell response to DNA damage

(2015) Kamila A. Marzec et al.   Oncotarget

TP53 transcription factor for the NEDD9/HEF1/Cas-L gene: potential targets in Non-Small Cell Lung Cancer treatment

(2015) Bénédicte ROUSSEAU et al.   Scientific Reports

Array-based genome-wide RNAi screening to identify shRNAs that enhance p53-related apoptosis in human cancer cells

(2015) Masashi Idogawa 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 in Cancer: New Functions and Therapeutic Opportunities

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

Wild type p53 reactivation: From lab bench to clinic

(2014) Galina Selivanova   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

PRIMA-1 Selectively Induces Global DNA Demethylation in p53 Mutant-Type Thyroid Cancer Cells

(2014) Wei Qiang et al.   Journal of Biomedical Nanotechnology

PRIMA-1, a Mutant p53 Reactivator, Restores the Sensitivity ofTP53Mutant-Type Thyroid Cancer Cells to the Histone Methylation Inhibitor 3-Deazaneplanocin A

(2014) Bo Cui et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

PRIMA-1 induces autophagy in cancer cells carrying mutant or wild type p53

(2013) Debora Russo et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

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-1 induces apoptosis in bladder cancer cell lines by activating p53

(2013) CB Piantino et al.   Clinics

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

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

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

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

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

Reactivation of p53 mutants by p53 reactivation and induction of massive apoptosis in thyroid cancer cells

(2011) Rosa Linda Messina et al.   INTERNATIONAL JOURNAL OF CANCER

PRIMA-1 cytotoxicity correlates with nucleolar localization and degradation of mutant p53 in breast cancer cells

(2010) Debora Russo et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Targeting mutant p53 protein and the tumor vasculature: an effective combination therapy for advanced breast tumors

(2010) Yayun Liang et al.   BREAST CANCER RESEARCH AND TREATMENT

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

p53-Reactivating small molecules induce apoptosis and enhance chemotherapeutic cytotoxicity in head and neck squamous cell carcinoma

(2010) Jong-Lyel Roh et al.   ORAL ONCOLOGY

Therapeutic targeting of p53 by small molecules

(2010) Galina Selivanova   SEMINARS IN CANCER BIOLOGY

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

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

MicroRNA-34a is an important component of PRIMA-1-induced apoptotic network in human lung cancer cells

(2009) Wenrui Duan et al.   INTERNATIONAL JOURNAL OF CANCER

PRIMA-1MET induces nucleolar translocation of Epstein-Barr virus-encoded EBNA-5 protein

(2009) György Stuber et al.   Molecular Cancer

Mutant p53 reactivation by PRIMA-1MET induces multiple signaling pathways converging on apoptosis

(2009) J M R Lambert et al.   ONCOGENE

PRIMA-1 synergizes with adriamycin to induce cell death in non-small cell lung cancer cells

(2008) R. Magrini et al.   JOURNAL OF CELLULAR BIOCHEMISTRY

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

PRIMA-1met radiosensitizes prostate cancer cells independent of their MTp53-status

(2008) Stéphane Supiot et al.   RADIOTHERAPY AND ONCOLOGY

In vitro and in vivo cytotoxic effects of PRIMA-1 on hepatocellular carcinoma cells expressing mutant p53ser249

(2007) H. Shi et al.   CARCINOGENESIS