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Synthesis of Structural ADP-Ribose Analogues as Inhibitors for SARS-CoV-2 Macrodomain 1.
Rijpkema, Koen J; Schuller, Marion; van der Veer, Miriam S; Rieken, Sjoerd; Chang, Diego L R; Balic, Pascal; Todorov, Alex; Minnee, Hugo; Wijngaarden, Sven; Matos, Isaac A; Hoch, Nicolas C; Codée, Jeroen D C; Ahel, Ivan; Filippov, Dmitri V.
Afiliação
  • Rijpkema KJ; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
  • Schuller M; Sir William Dunn School of Pathology, University of Oxford, South Parks Road, Oxford OX1 3RE, United Kingdom.
  • van der Veer MS; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
  • Rieken S; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
  • Chang DLR; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
  • Balic P; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
  • Todorov A; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
  • Minnee H; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
  • Wijngaarden S; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
  • Matos IA; Sir William Dunn School of Pathology, University of Oxford, South Parks Road, Oxford OX1 3RE, United Kingdom.
  • Hoch NC; Departamento de Bioquímica, Instituto de Química, Universidade de Sao Paulo, Av. Prof. Lineu Prestes, 748, Cidade Universitária, Sao Paulo 055800-000, Brasil.
  • Codée JDC; Departamento de Bioquímica, Instituto de Química, Universidade de Sao Paulo, Av. Prof. Lineu Prestes, 748, Cidade Universitária, Sao Paulo 055800-000, Brasil.
  • Ahel I; Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
  • Filippov DV; Sir William Dunn School of Pathology, University of Oxford, South Parks Road, Oxford OX1 3RE, United Kingdom.
Org Lett ; 26(27): 5700-5704, 2024 Jul 12.
Article em En | MEDLINE | ID: mdl-38935522
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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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Antivirais / Adenosina Difosfato Ribose / SARS-CoV-2 Idioma: En Ano de publicação: 2024 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Antivirais / Adenosina Difosfato Ribose / SARS-CoV-2 Idioma: En Ano de publicação: 2024 Tipo de documento: Article