New Nucleotide-Competitive Non-Nucleoside Inhibitors of Terminal Deoxynucleotidyl Transferase: Discovery, Characterization, and Crystal Structure in Complex with …

R Costi, G Cuzzucoli Crucitti, L Pescatori…

文献索引：Costi, Roberta; Cuzzucoli Crucitti, Giuliana; Pescatori, Luca; Messore, Antonella; Scipione, Luigi; Tortorella, Silvano; Amoroso, Alessandra; Crespan, Emmanuele; Campiglia, Pietro; Maresca, Bruno; Porta, Amalia; Granata, Ilaria; Novellino, Ettore; Gouge, Jeroime; Delarue, Marc; Maga, Giovanni; Di Santo, Roberto Journal of Medicinal Chemistry, 2013 , vol. 56, # 18 p. 7431 - 7441

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被引用次数: 1

摘要

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 nucleotide-competitive inhibitors. These compounds show a selective toxicity toward ...