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Identification of RAD51–BRCA2 Inhibitors Using <i>N</i>-Acylhydrazone-Based Dynamic Combinatorial Chemistry

Greta Bagnolini, Beatrice Balboni, Fabrizio Schipani, Dario Gioia, Marina Veronesi, Francesca Franco, Cansu Kaya, Ravindra P. Jumde, José Antonio Ortega, Stefania Girotto, Anna K. H. Hirsch, Marinella Roberti, Andrea Cavalli

2022ACS Medicinal Chemistry Letters24 citationsDOIOpen Access PDF

Abstract

could bind RAD51 and be displaced by BRC4, suggesting an interaction in the same binding pocket of BRCA2. These results proved not only that ptDCC could be successfully applied on full-length oligomeric RAD51, but also that it could address the need of alternative strategies toward the identification of small-molecule PPI inhibitors.

Topics & Concepts

RAD51RecombinaseComputational biologyCombinatorial chemistryChemistryHomologous recombinationIdentification (biology)DNA Damage RepairBiochemistryDNABiologyDNA damageRecombinationGeneBotanyAdvanced biosensing and bioanalysis techniquesDNA and Nucleic Acid ChemistryCancer therapeutics and mechanisms
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