A first-in-class clinical G-quadruplex-targeting drug. The bench-to-bedside translation of the fluoroquinolone QQ58 to CX-5461 (Pidnarulex)

Results of the phase I CCTG IND.231 trial of CX-5461 in patients with advanced solid tumors enriched for DNA-repair deficiencies

(2022) John Hilton et al.   Nature Communications

The i-Motif as a Molecular Target: More than a Complementary DNA Secondary Structure

(2021) Susie L. Brown et al.   Pharmaceuticals

Transcription-associated topoisomerase 2α (TOP2A) activity is a major effector of cytotoxicity induced by G-quadruplex ligands

(2021) Madeleine Bossaert et al.   eLife

The chemotherapeutic CX-5461 primarily targets TOP2B and exhibits selective activity in high-risk neuroblastoma

(2021) Min Pan et al.   Nature Communications

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

A Genetic Map of the Response to DNA Damage in Human Cells

(2020) Michele Olivieri et al.   CELL

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

DNA damage and genome instability by G-quadruplex ligands are mediated by R loops in human cancer cells

(2018) Alessio De Magis et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2017) Hong Xu et al.   Nature Communications

The Interplay between G-quadruplex and Transcription

(2017) Nayun Kim   CURRENT MEDICINAL CHEMISTRY

Targeting BRCA1 and BRCA2 Deficiencies with G-Quadruplex-Interacting Compounds

(2016) Jutta Zimmer et al.   MOLECULAR CELL

G-Quadruplex DNA as a Molecular Target for Induced Synthetic Lethality in Cancer Cells

(2013) Keith I. E. McLuckie et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

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

(2009) D. Drygin et al.   CANCER RESEARCH

Identification and Characterization of Nucleolin as a c-mycG-quadruplex-binding Protein

(2009) Verónica González et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Importance of Negative Superhelicity in Inducing the Formation of G-Quadruplex and i-Motif Structures in the c-Myc Promoter: Implications for Drug Targeting and Control of Gene Expression

(2009) Daekyu Sun et al.   JOURNAL OF MEDICINAL CHEMISTRY