Synthesis of Structural ADP-Ribose Analogues as Inhibitors for SARS-CoV-2 Macrodomain 1.
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ABSTRACT:
SUBMITTER: Rijpkema KJ
PROVIDER: S-EPMC11249776 | biostudies-literature | 2024 Jul
REPOSITORIES: biostudies-literature
Publications
Synthesis of Structural ADP-Ribose Analogues as Inhibitors for SARS-CoV-2 Macrodomain 1.
Rijpkema Koen J KJ Schuller Marion M van der Veer Miriam S MS Rieken Sjoerd S Chang Diego L R DLR Balić Pascal P Todorov Alex A Minnee Hugo H Wijngaarden Sven S Matos Isaac A IA Hoch Nicolas C NC Codée Jeroen D C JDC Ahel Ivan I Filippov Dmitri V DV
Organic letters 20240627 27
Protein adenosine diphosphate (ADP)-ribosylation is crucial for a proper immune response. Accordingly, viruses have evolved ADP-ribosyl hydrolases to remove these modifications, a prominent example being the SARS-CoV-2 NSP3 macrodomain, "Mac1". Consequently, inhibitors are developed by testing large libraries of small molecule candidates, with considerable success. However, a relatively underexplored angle in design pertains to the synthesis of structural substrate mimics. Here, we present the s ...[more]
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