Electron paramagnetic resonance (EPR) study of spin-labeled camptothecin derivatives: A different look of the ternary complex

…, E Pedroso, Y Pommier, G Capranico…

Index: Ricci, Antonio; Marinello, Jessica; Bortolus, Marco; Sanchez, Albert; Grandas, Anna; Pedroso, Enrique; Pommier, Yves; Capranico, Giovanni; Maniero, Anna Lisa; Zagotto, Giuseppe Journal of Medicinal Chemistry, 2011 , vol. 54, # 4 p. 1003 - 1009

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Citation Number: 6

Abstract

Camptothecin (CPT) derivatives are clinically effective poisons of DNA topoisomerase I (Top1) able to form a ternary complex with the Top1− DNA complex. The aim of this investigation was to examine the dynamic aspects of the ternary complex formation by means of site-directed spin labeling electron paramagnetic resonance (SDSL-EPR). Two semisynthetic CPT derivatives bearing the paramagnetic moiety were synthesized, and ...