PERK Inhibition by HC-5404 Sensitizes Renal Cell Carcinoma Tumor Models to Antiangiogenic Tyrosine Kinase Inhibitors

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Authors: Michael E Stokes, Veronica Calvo, Sho Fujisawa, Crissy Dudgeon, Sharon Huang, Nupur Ballal, Leyi Shen, Jennifer Gasparek, Matthew Betzenhauser, Simon J. Taylor, Kirk A. Staschke, Alan C. Rigby, Mark J. Mulvihill, Nandita Bose, Eric S. Lightcap, David Surguladze
This study highlights the discovery and preliminary evaluation of XRD-0394, an orally administered compound that not only radiosensitizes cancer cells but also increases the activity of topoisomerase I inhibitors under laboratory conditions. Furthermore, XRD-0394 demonstrates single-agent efficacy in BRCA1/2-deficient cells and exhibits synergistic effects when combined with PARP inhibitors.
Clin Cancer Res. 2023 Dec 1;29(23):4870-4882
DOI: 10.1158/1078-0432.CCR-23-1182
Access the publication at:https://pubmed.ncbi.nlm.nih.gov/37733811/