High-Throughput Activity Assay for Screening Inhibitors of the SARS-CoV-2 Mac1 Macrodomain
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DOI: 10.1021/acschembio.1c00721
Abstract: Macrodomains are a class of conserved ADP-ribosylhydrolases expressed by viruses of pandemic concern, including coronaviruses and alphaviruses. Viral macrodomains are critical for replication and virus-induced pathogenesis; therefore, these enzymes are a promising target for antiviral… read more here.
Keywords: cov mac1; high throughput; macrodomain; sars cov ... See more keywords
Iterative computational design and crystallographic screening identifies potent inhibitors targeting the Nsp3 macrodomain of SARS-CoV-2
Sign Up to like & getrecommendations! Published in 2023 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2212931120
Abstract: Significance The nonstructural protein 3 (NSP3) of the severe acute respiratory syndrome-coronavirus-2 (SARS-CoV-2) contains a conserved macrodomain enzyme (Mac1) that is critical for pathogenesis and lethality. There are currently no well-validated inhibitors for this protein.… read more here.
Keywords: iterative computational; macrodomain; design crystallographic; crystallographic screening ... See more keywords
Crystal structure and biochemical activity of the macrodomain from rubella virus p150
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DOI: 10.1128/jvi.01777-23
Abstract: ABSTRACT Rubella virus encodes a nonstructural polyprotein with RNA polymerase, methyltransferase, and papain-like cysteine protease activities, along with a putative macrodomain of unknown function. Macrodomains bind ADP–ribose adducts, a post-translational modification that plays a key… read more here.
Keywords: macrodomain; pathology; virus; rubella virus ... See more keywords