Identification and characterization of topoisomerase III beta poisons

• Published in: Proceedings of the National Academy of Sciences - PNAS Vol. 120; no. 34; p. e2218483120
• Main Authors: Wang, Wenjie, Saha, Sourav, Yang, Xi, Pommier, Yves, Huang, Shar-Yin N
• Format: Journal Article
• Language: English
• Published: United States National Academy of Sciences 22.08.2023
• Subjects: Biological Sciences; Cell Line; Cell lines; Cytotoxicity; DNA topoisomerase III; DNA Topoisomerases, Type I - metabolism; Lead compounds; Poisons; R-loops; RNA; Topoisomerase I Inhibitors - chemistry; TOP3B; anti-cancer; inhibitor screen

We designed and carried out a high-throughput screen for compounds that trap topoisomerase III beta (TOP3B poisons) by developing a Comparative Cellular Cytotoxicity Screen. We found a bisacridine compound NSC690634 and a thiacyanine compound NSC96932 that preferentially sensitize cell lines express...