ArticlebioRxiv : the preprint server for biology2023
Discovery of 2-amide-3-methylester thiophenes that target SARS-CoV-2 Mac1 and repress coronavirus replication, validating Mac1 as an anti-viral target.
Sarah Wazir, Tomi A O Parviainen, Jessica J Pfannenstiel, Men Thi Hoai Duong, Daniel Cluff, Sven T Sowa, Albert Galera-Prat, Dana Ferraris, Mirko M Maksimainen, Anthony R Fehr and 2 more
Open access · greenAbstract readPreprint
In one paragraphArticle in bioRxiv : the preprint server for biology, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from itWhat it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
2 · The registryThe trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
3 · Its place in the literatureWho cites it
0 citing papers in PubMed, 5 citations in OpenAlex.
No citing paper in PubMed yet.
4 · The recordCorrections and comments
5 · Who and what moneyAuthors and funding
12 authors at 3 institutions in 2 countries.
Sarah WazirFaculty of Biochemistry and Molecular Medicine & Biocenter Oulu, University of Oulu, Finland.ORCID 0000-0003-0133-2923 Tomi A O ParviainenResearch Unit of Sustainable Chemistry, University of Oulu, P.O. Box 4300, FI-90014 Oulu, Finland.ORCID 0000-0002-3402-6378 Jessica J PfannenstielDepartment of Molecular Biosciences, University of Kansas, Lawrence, Kansas, United States of America.ORCID 0009-0003-0783-3208 Men Thi Hoai DuongFaculty of Biochemistry and Molecular Medicine & Biocenter Oulu, University of Oulu, Finland.ORCID 0000-0002-1845-7186 Daniel CluffDepartment of Molecular Biosciences, University of Kansas, Lawrence, Kansas, United States of America.
Sven T SowaFaculty of Biochemistry and Molecular Medicine & Biocenter Oulu, University of Oulu, Finland.ORCID 0000-0001-7411-5925 Albert Galera-PratFaculty of Biochemistry and Molecular Medicine & Biocenter Oulu, University of Oulu, Finland.ORCID 0000-0002-6334-3428 Mirko M MaksimainenFaculty of Biochemistry and Molecular Medicine & Biocenter Oulu, University of Oulu, Finland.ORCID 0000-0001-8586-9538 Anthony R FehrDepartment of Molecular Biosciences, University of Kansas, Lawrence, Kansas, United States of America.ORCID 0000-0003-1560-1573 Juha P HeiskanenResearch Unit of Sustainable Chemistry, University of Oulu, P.O. Box 4300, FI-90014 Oulu, Finland.ORCID 0000-0002-1884-1583 Lari LehtiöFaculty of Biochemistry and Molecular Medicine & Biocenter Oulu, University of Oulu, Finland.ORCID 0000-0001-7250-832X University of Oulu · FIUniversity of Kansas · USMcDaniel College · US
Funding
RADx-UP: Improving the Response of Local Urban and Rural Communities to Disparities in Covid-19 TestingUL1TR002366 · NCATS · UNIVERSITY OF KANSAS MEDICAL CENTER · PI Mario Castro, JAMES STEVEN LEEDER · 2017 to 2026
$44.3MSynthetic Chemical Biology CoreP20GM113117 · NIGMS · UNIVERSITY OF KANSAS LAWRENCE · PI OROZCO, ROBIN C. · 2016 to 2025
$23.9MProtein Structure Laboratory P30GM110761 · NIGMS · UNIVERSITY OF KANSAS LAWRENCE · PI LOVELL, SCOTT W. · 2014 to 2018
$5.6MDetermining mechanisms of innate immune modulation by ADP-ribosylationR35GM138029 · NIGMS · UNIVERSITY OF KANSAS LAWRENCE · PI Anthony R. Fehr · 2020 to 2026
$2.7MNCATS NIH HHS UL1 TR002366NIGMS NIH HHS P20 GM113117NIGMS NIH HHS P30 GM110761NIGMS NIH HHS R35 GM138029
6 · The paper itselfAbstract
The COVID-19 pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virus has made it clear that further development of antiviral therapies will be needed to combat additional SARS-CoV-2 variants or novel CoVs. Here, we describe small molecule inhibitors for SARS-CoV-2 Mac1, which counters ADP-ribosylation mediated innate immune responses. The compounds inhibiting Mac1 were discovered through high-throughput screening (HTS) using a protein FRET-based competition assay and the best hit compound had an IC
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PMID38234730
PMCPMC10793406
OpenAlexW4386293964
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