Ananya Anmangandla, Sadhan Jana, Kewen Peng, Shamar D Wallace, Saket R Bagde, Bryon S Drown, Jiashu Xu, Paul J Hergenrother, J Christopher Fromme, Hening Lin
Viral macrodomains, which can bind to and/or hydrolyze adenine diphosphate ribose (ADP-ribose or ADPr) from proteins, have been suggested to counteract host immune response and be viable targets for the development of antiviral drugs. Therefore, developing high-throughput screening (HTS) techniques for macrodomain inhibitors is of great interest. Herein, using a novel tracer TAMRA-ADPr , an ADP-ribose compound conjugated with tetramethylrhodamine, we developed a robust fluorescence polarization assay for various viral and human macrodomains including SARS-CoV-2 Macro1, VEEV Macro, CHIKV Macro, human MacroD1, MacroD2, and PARP9 Macro2...
May 1, 2023: ACS Chemical Biology