New nucleotide-competitive non-nucleoside inhibitors of terminal deoxynucleotidyl transferase: discovery, characterization, and crystal structure in complex with the target.

Abstract

Terminal deoxynucletidyl transferase (TdT) is overexpressed in some cancer types, where it might compete with pol μ during the mutagenic repair of double strand breaks (DSBs) through the nonhomologous end joining (NHEJ) pathway. Here we report the discovery and characterization of pyrrolyl and indolyl diketo acids that specifically target TdT and behave as… (More)
DOI: 10.1021/jm4010187

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Cite this paper

@article{Costi2013NewNN, title={New nucleotide-competitive non-nucleoside inhibitors of terminal deoxynucleotidyl transferase: discovery, characterization, and crystal structure in complex with the target.}, author={Roberta Costi and Giuliana Cuzzucoli Crucitti and Luca Pescatori and Antonella Messore and Luigi Scipione and Silvano Tortorella and Alessandra Amoroso and Emmanuele Crespan and Pietro Campiglia and Bruno Maresca and Amalia Porta and Ilaria Granata and Ettore Novellino and J{\'e}r{\^o}me Gouge and Marc Delarue and Giovanni Maga and Roberto Di Santo}, journal={Journal of medicinal chemistry}, year={2013}, volume={56 18}, pages={7431-41} }