Ontology highlight
ABSTRACT:
SUBMITTER: Sirivolu VR
PROVIDER: S-EPMC7479925 | biostudies-literature | 2012 Oct
REPOSITORIES: biostudies-literature
Sirivolu Venkata Ramana VR Vernekar Sanjeev Kumar V SK Marchand Christophe C Naumova Alena A Chergui Adel A Renaud Amelie A Stephen Andrew G AG Chen Feng F Sham Yuk Y YY Pommier Yves Y Wang Zhengqiang Z
Journal of medicinal chemistry 20121008 20
Tyrosyl-DNA phosphodiesterase I (Tdp1) is a cellular enzyme that repairs the irreversible topoisomerase I (Top1)-DNA complexes and confers chemotherapeutic resistance to Top1 inhibitors. Inhibiting Tdp1 provides an attractive approach to potentiating clinically used Top1 inhibitors. However, despite recent efforts in studying Tdp1 as a therapeutic target, its inhibition remains poorly understood and largely underexplored. We describe herein the discovery of arylidene thioxothiazolidinone as a sc ...[more]