Synthesis of Structural ADP-Ribose Analogues as Inhibitors for SARS-CoV-2 Macrodomain 1 Article Swipe
Koen J. Rijpkema
,
M. Schuller
,
Miriam S. van der Veer
,
Sjoerd Rieken
,
Diego L. R. Chang
,
Pascal Balić
,
Alex G. Todorov
,
Hugo Minnee
,
Sven Wijngaarden
,
Isaac de Araújo Matos
,
Nícolas C. Hoch
,
Jeroen D. C. Codée
,
Ivan Ahel
,
Dmitri V. Filippov
·
YOU?
·
· 2024
· Open Access
·
· DOI: https://doi.org/10.1021/acs.orglett.4c01792
YOU?
·
· 2024
· Open Access
·
· DOI: https://doi.org/10.1021/acs.orglett.4c01792
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.
Related Topics
Concepts
Chemistry
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)
Ribose
Coronavirus disease 2019 (COVID-19)
Enzyme
Biochemistry
Stereochemistry
Computational biology
Combinatorial chemistry
Biology
Medicine
Disease
Infectious disease (medical specialty)
Pathology
Metadata
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.1021/acs.orglett.4c01792
- https://pubs.acs.org/doi/pdf/10.1021/acs.orglett.4c01792
- OA Status
- hybrid
- Cited By
- 4
- References
- 34
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W4400077378
All OpenAlex metadata
Raw OpenAlex JSON
- OpenAlex ID
-
https://openalex.org/W4400077378Canonical identifier for this work in OpenAlex
- DOI
-
https://doi.org/10.1021/acs.orglett.4c01792Digital Object Identifier
- Title
-
Synthesis of Structural ADP-Ribose Analogues as Inhibitors for SARS-CoV-2 Macrodomain 1Work title
- Type
-
articleOpenAlex work type
- Language
-
enPrimary language
- Publication year
-
2024Year of publication
- Publication date
-
2024-06-27Full publication date if available
- Authors
-
Koen J. Rijpkema, M. Schuller, Miriam S. van der Veer, Sjoerd Rieken, Diego L. R. Chang, Pascal Balić, Alex G. Todorov, Hugo Minnee, Sven Wijngaarden, Isaac de Araújo Matos, Nícolas C. Hoch, Jeroen D. C. Codée, Ivan Ahel, Dmitri V. FilippovList of authors in order
- Landing page
-
https://doi.org/10.1021/acs.orglett.4c01792Publisher landing page
- PDF URL
-
https://pubs.acs.org/doi/pdf/10.1021/acs.orglett.4c01792Direct link to full text PDF
- Open access
-
YesWhether a free full text is available
- OA status
-
hybridOpen access status per OpenAlex
- OA URL
-
https://pubs.acs.org/doi/pdf/10.1021/acs.orglett.4c01792Direct OA link when available
- Concepts
-
Chemistry, Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), Ribose, Coronavirus disease 2019 (COVID-19), Enzyme, Biochemistry, Stereochemistry, Computational biology, Combinatorial chemistry, Biology, Medicine, Disease, Infectious disease (medical specialty), PathologyTop concepts (fields/topics) attached by OpenAlex
- Cited by
-
4Total citation count in OpenAlex
- Citations by year (recent)
-
2025: 4Per-year citation counts (last 5 years)
- References (count)
-
34Number of works referenced by this work
- Related works (count)
-
10Other works algorithmically related by OpenAlex
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