CX-5461 Enhances the Efficacy of APR-246 via Induction of DNA Damage and Replication Stress in Triple-Negative Breast Cancer

CARM1 regulates replication fork speed and stress response by stimulating PARP1

(2021) Marie-Michelle Genois et al.   MOLECULAR CELL

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

(2021) Paola Menichini et al.   Cells

The primary mechanism of cytotoxicity of the chemotherapeutic agent CX-5461 is topoisomerase II poisoning

(2020) Peter M. Bruno et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeting the RNA Polymerase I Transcription for Cancer Therapy Comes of Age

(2020) Rita Ferreira et al.   Cells

CX-5461 activates the DNA damage response and demonstrates therapeutic efficacy in high-grade serous ovarian cancer

(2020) Elaine Sanij et al.   Nature Communications

Patterns of Genomic Instability in Breast Cancer

(2019) Murugan Kalimutho et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Blockade of PDGFRβ circumvents resistance to MEK-JAK inhibition via intratumoral CD8+ T-cells infiltration in triple-negative breast cancer

(2019) Murugan Kalimutho et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

First-in-Human RNA Polymerase I Transcription Inhibitor CX-5461 in Patients with Advanced Hematological Cancers: Results of a Phase I Dose Escalation Study

(2019) Amit Khot et al.   Cancer Discovery

The Targeting of RNA Polymerase I Transcription Using CX-5461 in Combination with Radiation Enhances Tumour Cell Killing Effects in Human Solid Cancers

(2019) Mohammed Ismael et al.   Cancers

CEP55 is a determinant of cell fate during perturbed mitosis in breast cancer

(2018) Murugan Kalimutho et al.   EMBO Molecular Medicine

High speed of fork progression induces DNA replication stress and genomic instability

(2018) Apolinar Maya-Mendoza et al.   NATURE

The Mutant p53-Targeting Compound APR-246 Induces ROS-Modulating Genes in Breast Cancer Cells

(2018) Naoise C. Synnott et al.   Translational Oncology

Enhanced dependency of KRAS-mutant colorectal cancer cells on RAD51-dependent homologous recombination repair identified from genetic interactions in Saccharomyces cerevisiae

(2017) Murugan Kalimutho et al.   Molecular Oncology

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

(2017) Xiaoxiao Peng et al.   Cell Death & Disease

CX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours

(2017) Hong Xu 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

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

Multiple functions of p21 in cell cycle, apoptosis and transcriptional regulation after DNA damage

(2016) Ansar Karimian et al.   DNA REPAIR

CX-5461 induces autophagy and inhibits tumor growth via mammalian target of rapamycin-related signaling pathways in osteosarcoma

(2016) Xu Li et al.   OncoTargets and Therapy

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

Inhibition of RNA polymerase I transcription initiation by CX-5461 activates non-canonical ATM/ATR signaling

(2016) Jaclyn Quin et al.   Oncotarget

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

(2015) Thomas Grellety et al.   BMC CANCER

Targeted Therapies for Triple-Negative Breast Cancer: Combating a Stubborn Disease

(2015) Murugan Kalimutho et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

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

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

rRNA synthesis inhibitor, CX-5461, activates ATM/ATR pathway in acute lymphoblastic leukemia, arrests cells in G2 phase and induces apoptosis

(2015) Sandeep S. Negi et al.   Oncotarget

Mutant p53 in Cancer: New Functions and Therapeutic Opportunities

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

p53 as a target for the treatment of cancer

(2014) Michael J. Duffy et al.   CANCER TREATMENT REVIEWS

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

Mutational landscape and significance across 12 major cancer types

(2013) Cyriac Kandoth et al.   NATURE

Inhibition of RNA Polymerase I as a Therapeutic Strategy to Promote Cancer-Specific Activation of p53

(2012) Megan J. Bywater et al.   CANCER CELL

Mutant p53: one name, many proteins

(2012) W. A. Freed-Pastor et al.   GENES & DEVELOPMENT

TBCRC 001: Randomized Phase II Study of Cetuximab in Combination With Carboplatin in Stage IV Triple-Negative Breast Cancer

(2012) Lisa A. Carey et al.   JOURNAL OF CLINICAL ONCOLOGY

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 TP53 website: an integrative resource centre for the TP53 mutation database and TP53 mutant analysis

(2012) Bernard Leroy et al.   NUCLEIC ACIDS RESEARCH

Discovery of CX-5461, the First Direct and Selective Inhibitor of RNA Polymerase I, for Cancer Therapeutics

(2012) Mustapha Haddach et al.   ACS Medicinal Chemistry Letters

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

Analysis of protein dynamics at active, stalled, and collapsed replication forks

(2011) B. M. Sirbu et al.   GENES & DEVELOPMENT

Olaparib in patients with recurrent high-grade serous or poorly differentiated ovarian carcinoma or triple-negative breast cancer: a phase 2, multicentre, open-label, non-randomised study

(2011) Karen A Gelmon et al.   LANCET ONCOLOGY

Iniparib plus Chemotherapy in Metastatic Triple-Negative Breast Cancer

(2011) Joyce O'Shaughnessy et al.   NEW ENGLAND JOURNAL OF MEDICINE

Essential Gene Profiles in Breast, Pancreatic, and Ovarian Cancer Cells

(2011) Richard Marcotte et al.   Cancer Discovery

Visualization of DNA Replication in the Vertebrate Model System DT40 using the DNA Fiber Technique

(2011) Rebekka A.V. Schwab et al.   Jove-Journal of Visualized Experiments

The RNA Polymerase I Transcription Machinery: An Emerging Target for the Treatment of Cancer

(2010) Denis Drygin et al.   Annual Review of Pharmacology and Toxicology

Targeting RNA Polymerase I with an Oral Small Molecule CX-5461 Inhibits Ribosomal RNA Synthesis and Solid Tumor Growth

(2010) Denis Drygin et al.   CANCER RESEARCH

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

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

Anticancer Activity of CX-3543: A Direct Inhibitor of rRNA Biogenesis

(2009) D. Drygin et al.   CANCER RESEARCH

Basal-Like Breast Cancer: A Critical Review

(2008) Emad A. Rakha et al.   JOURNAL OF CLINICAL ONCOLOGY