Antitumor Effects of PRIMA-1 and PRIMA-1Met (APR246) in Hematological Malignancies: Still a Mutant P53-Dependent Affair?

TP53 dysfunction in chronic lymphocytic leukemia: clinical relevance in the era of B-cell receptors and BCL-2 inhibitors

(2020) Fortunato Morabito et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

To target the untargetable: elucidation of synergy of APR-246 and azacitidine in TP53 mutant myelodysplastic syndromes and acute myeloid leukemia

(2020) David A. Sallman   HAEMATOLOGICA

MDM2 inhibition: an important step forward in cancer therapy

(2020) Marina Konopleva et al.   LEUKEMIA

Prediction of Outcome in Patients With Chronic Lymphocytic Leukemia Treated With Ibrutinib: Development and Validation of a Four-Factor Prognostic Model

(2020) Inhye E. Ahn et al.   JOURNAL OF CLINICAL ONCOLOGY

Venetoclax plus obinutuzumab versus chlorambucil plus obinutuzumab for previously untreated chronic lymphocytic leukaemia (CLL14): follow-up results from a multicentre, open-label, randomised, phase 3 trial

(2020) Othman Al-Sawaf et al.   LANCET ONCOLOGY

Targeting Oxidative Stress With Auranofin or Prima-1Met to Circumvent p53 or Bax/Bak Deficiency in Myeloma Cells

(2019) Benoit Tessoulin et al.   Frontiers in Oncology

Autophagy induced by SAHA affects mutant P53 degradation and cancer cell survival

(2019) Giorgia Foggetti et al.   BIOSCIENCE REPORTS

Ibrutinib and Venetoclax for First-Line Treatment of CLL

(2019) Nitin Jain et al.   NEW ENGLAND JOURNAL OF MEDICINE

Final Results of a Randomized, Phase III Study of Rituximab With or Without Idelalisib Followed by Open-Label Idelalisib in Patients With Relapsed Chronic Lymphocytic Leukemia

(2019) Jeff P. Sharman et al.   JOURNAL OF CLINICAL ONCOLOGY

Ibrutinib–Rituximab or Chemoimmunotherapy for Chronic Lymphocytic Leukemia

(2019) Tait D. Shanafelt et al.   NEW ENGLAND JOURNAL OF MEDICINE

Integrated Analysis of TP53 Gene and Pathway Alterations in The Cancer Genome Atlas

(2019) Lawrence A. Donehower et al.   Cell Reports

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

(2019) Nabih Maslah et al.   HAEMATOLOGICA

Long-term efficacy and safety of first-line ibrutinib treatment for patients with CLL/SLL: 5 years of follow-up from the phase 3 RESONATE-2 study

(2019) Jan A. Burger et al.   LEUKEMIA

PRIMA-1MET cytotoxic effect correlates with p53 protein reduction in TP53-mutated chronic lymphocytic leukemia cells

(2019) Zuzana Jaskova et al.   LEUKEMIA RESEARCH

Chronic lymphocytic leukaemia

(2018) Michael Hallek et al.   LANCET

Validation of a biological score to predict response in chronic lymphocytic leukemia patients treated front-line with bendamustine and rituximab

(2018) Massimo Gentile et al.   LEUKEMIA

ERIC recommendations for TP53 mutation analysis in chronic lymphocytic leukemia—update on methodological approaches and results interpretation

(2018) J. Malcikova et al.   LEUKEMIA

Venetoclax–Rituximab in Relapsed or Refractory Chronic Lymphocytic Leukemia

(2018) John F. Seymour et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

(2018) Qiang Zhang et al.   Cell Death & Disease

Mutant p53 tunes the NRF2-dependent antioxidant response to support survival of cancer cells

(2018) Kamil Lisek et al.   Oncotarget

Gain-of-Function (GOF) Mutant p53 as Actionable Therapeutic Target

(2018) Ramona Schulz-Heddergott et al.   Cancers

Prognostic and therapeutic stratification in CLL: focus on 17p deletion and p53 mutation

(2018) Valeria Buccheri et al.   ANNALS OF HEMATOLOGY

Ibrutinib Regimens versus Chemoimmunotherapy in Older Patients with Untreated CLL

(2018) Jennifer A. Woyach et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

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

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

(2017) Anne Perdrix et al.   Cancers

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

2016 US lymphoid malignancy statistics by World Health Organization subtypes

(2016) Lauren R. Teras et al.   CA-A CANCER JOURNAL FOR CLINICIANS

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

Depleting stabilized GOF mutant p53 proteins by inhibiting molecular folding chaperones: a new promise in cancer therapy

(2016) Evguenia M Alexandrova et al.   CELL DEATH AND DIFFERENTIATION

Genetic profiling of CLL: a ‘TP53 addict’ perspective

(2016) L Lodé et al.   Cell Death & Disease

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

(2016) Manujendra N. Saha 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 induces death in soft-tissue sarcomas cell independent of p53

(2015) Thomas Grellety et al.   BMC CANCER

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

(2015) David S H Liu et al.   GUT

Metabolism pathways in chronic lymphocytic leukemia

(2015) Uri Rozovski et al.   LEUKEMIA & LYMPHOMA

Ibrutinib as Initial Therapy for Patients with Chronic Lymphocytic Leukemia

(2015) Jan A. Burger et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

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

Regulation of p53: a collaboration between Mdm2 and Mdmx

(2015) Dongsheng Pei et al.   Oncotarget

Gene mutations and treatment outcome in chronic lymphocytic leukemia: results from the CLL8 trial

(2014) S. Stilgenbauer et al.   BLOOD

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

(2014) B. Tessoulin et al.   BLOOD

Clinical impact of small TP53 mutated subclones in chronic lymphocytic leukemia

(2014) D. Rossi et al.   BLOOD

Wild type p53 reactivation: From lab bench to clinic

(2014) Galina Selivanova   FEBS LETTERS

TP53 Mutations in Human Cancer: Database Reassessment and Prospects for the Next Decade

(2014) Bernard Leroy et al.   HUMAN MUTATION

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

Idelalisib and Rituximab in Relapsed Chronic Lymphocytic Leukemia

(2014) Richard R. Furman et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

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

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

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

Functional Inactivation of Endogenous MDM2 and CHIP by HSP90 Causes Aberrant Stabilization of Mutant p53 in Human Cancer Cells

(2011) D. Li et al.   MOLECULAR CANCER RESEARCH

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

Rescue of the apoptotic-inducing function of mutant p53 by small molecule RITA

(2010) Carolyn Y. Zhao et al.   CELL CYCLE

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

Gambogic acid-induced degradation of mutant p53 is mediated by proteasome and related to CHIP

(2010) Jia Wang et al.   JOURNAL OF CELLULAR BIOCHEMISTRY

TP53 mutation profile in chronic lymphocytic leukemia: evidence for a disease specific profile from a comprehensive analysis of 268 mutations

(2010) T Zenz et al.   LEUKEMIA

The significance ofTP53in lymphoid malignancies: mutation prevalence, regulation, prognostic impact and potential as a therapeutic target

(2009) K-John J. Cheung et al.   BRITISH JOURNAL OF HAEMATOLOGY

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

The Prognostic Value of TP53 Mutations in Chronic Lymphocytic Leukemia Is Independent of Del17p13: Implications for Overall Survival and Chemorefractoriness

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

PRIMA-1 inhibits growth of breast cancer cells by re-activating mutant p53 protein

(2009) Hyder   INTERNATIONAL JOURNAL OF ONCOLOGY

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

(2009) J M R Lambert et al.   ONCOGENE

Mutated and non-mutated TP53 as targets in the treatment of leukaemia

(2008) H. Nahi et al.   BRITISH JOURNAL OF HAEMATOLOGY

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

A subset of Binet stage A CLL patients with TP53 abnormalities and mutated IGHV genes have stable disease

(2008) O G Best et al.   LEUKEMIA

Molecular diagnostics in chronic lymphocytic leukemia – Pathogenetic and clinical implications

(2008) Thorsten Zenz et al.   LEUKEMIA & LYMPHOMA

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