2. Academic Validation
  3. Synthesis of Structural ADP-Ribose Analogues as Inhibitors for SARS-CoV-2 Macrodomain 1

Synthesis of Structural ADP-Ribose Analogues as Inhibitors for SARS-CoV-2 Macrodomain 1

  • Org Lett. 2024 Jul 12;26(27):5700-5704. doi: 10.1021/acs.orglett.4c01792.
Koen J Rijpkema 1,  Marion Schuller 2,  Miriam S van der Veer 1,  Sjoerd Rieken 1,  Diego L R Chang 1,  Pascal Balić 1,  Alex Todorov 1,  Hugo Minnee 1,  Sven Wijngaarden 1,  Isaac A Matos 2 3,  Nicolas C Hoch 3,  Jeroen D C Codée 1,  Ivan Ahel 2,  Dmitri V Filippov 1
Affiliations

Affiliations

  • 1 Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
  • 2 Sir William Dunn School of Pathology, University of Oxford, South Parks Road, Oxford OX1 3RE, United Kingdom.
  • 3 Departamento de Bioquímica, Instituto de Química, Universidade de Sao Paulo, Av. Prof. Lineu Prestes, 748, Cidade Universitária, Sao Paulo 055800-000, Brasil.
PMID: 38935522 DOI: 10.1021/acs.orglett.4c01792
Abstract

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 synthesis and biophysical activity of novel adenosine diphosphate ribose (ADPr) analogues as SARS-CoV-2 NSP3 Mac1 inhibitors.

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