Ontology highlight
ABSTRACT:
SUBMITTER: Marchand C
PROVIDER: S-EPMC7857643 | biostudies-literature | 2016 Jul
REPOSITORIES: biostudies-literature
Marchand Christophe C Abdelmalak Monica M Kankanala Jayakanth J Huang Shar-Yin SY Kiselev Evgeny E Fesen Katherine K Kurahashi Kayo K Sasanuma Hiroyuki H Takeda Shunichi S Aihara Hideki H Wang Zhengqiang Z Pommier Yves Y
ACS chemical biology 20160511 7
Tyrosyl-DNA phosphodiesterase 2 repairs irreversible topoisomerase II-mediated cleavage complexes generated by anticancer topoisomerase-targeted drugs and processes replication intermediates for picornaviruses (VPg unlinkase) and hepatitis B virus. There is currently no TDP2 inhibitor in clinical development. Here, we report a series of deazaflavin derivatives that selectively inhibit the human TDP2 enzyme in a competitive manner both with recombinant and native TDP2. We show that mouse, fish, a ...[more]