Development of Small Molecules that Specifically Inhibit the D-loop Activity of RAD51

…, M Pawlowski, PP Connell, AP Kozikowski

Index: Budke, Brian; Kalin, Jay H.; Pawlowski, Michal; Zelivianskaia, Anna S.; Wu, Megan; Kozikowski, Alan P.; Connell, Philip P. Journal of Medicinal Chemistry, 2013 , vol. 56, # 1 p. 254 - 263

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Citation Number: 2

Abstract

RAD51 is the central protein in homologous recombination (HR) DNA repair and represents a therapeutic target in oncology. Herein we report a novel class of RAD51 inhibitors that were identified by high throughput screening. In contrast to many previously reported RAD51 inhibitors, our lead compound 1 is capable of blocking RAD51-mediated D-loop formation (IC50 21.3±7.8 μM) at concentrations that do not influence RAD51 binding to ...