An Update on the Current State of SARS-CoV-2 Mac1 Inhibitors
Pathogens, 2023 Non-structural protein 3 (nsp3) from all coronaviruses (CoVs) contains a conserved macrodomain, known as Mac1, that has been proposed as a potential therapeutic target for CoVs due to its critical role in viral pathogenesis. Mac1 is an ADP-ribose binding
Dana Ferraris +2 more
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Identification of a series of pyrrolo-pyrimidine-based SARS-CoV-2 Mac1 inhibitors that repress coronavirus replication [PDF]
mBioCoronaviruses (CoVs) can emerge from zoonotic sources and cause severe diseases in humans and animals. CoVs encode for a macrodomain (Mac1) that binds to and removes ADP-ribose from target proteins.
Jessica J. Pfannenstiel +18 more
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Microglial MAC1 receptor and PI3K are essential in mediating β-amyloid peptide-induced microglial activation and subsequent neurotoxicity [PDF]
Journal of Neuroinflammation, 2011 Background β-Amyloid peptide (Aβ) is a major protein in the brain associated with Alzheimer's and Parkinson's diseases. The purpose of this study was to investigate the role of macrophage antigen-1 (MAC1) receptor, an integrin scavenger receptor in ...
Jau-Shyong Hong, Shih-Heng Chen
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Mutations differentially affecting the coronavirus Mac1 ADP-ribose binding and hydrolysis activities indicate that it promotes multiple stages of the viral replication cycle [PDF]
Journal of VirologyAll coronaviruses (CoVs) encode a conserved macrodomain, termed Mac1, in non-structural protein 3 (nsp3) that binds and hydrolyzes ADP-ribose covalently attached to proteins.
Anuradha Roy +2 more
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Viruses, 2023 Since the emergence of SARS-CoV-2, many genetic variations within its genome have been identified, but only a few mutations have been found in nonstructural proteins (NSPs).
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Cellular engagement of the SARS-CoV-2 macrodomain by GS-441524 and enhanced in vitro inhibition by its diphosphorylated metabolite [PDF]
RSC Chemical BiologyCoronavirus macrodomains (Mac1) counter host immunity by removing ADP-ribose. GS-441524, the parent nucleoside of remdesivir, inhibits SARS-CoV-2 Mac1, but its active metabolite and cellular engagement were undefined.
Banhi Biswas +15 more
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Interactomics of SARS-CoV-2 Macrodomain 1 Reveals Putative Clients of ADP-Ribosyl Hydrolase Activity [PDF]
VirusesSevere acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has greatly impacted public health due to high rates of transmissibility and mutation during the COVID-19 pandemic.
Crissey D. Cameron +3 more
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MBio, 2022 Intracellular pathogens residing within macrophage phagosomes are challenged with recognizing the phagosomal environment and appropriately responding to changing host defense strategies imposed in this organelle.
Chad Rappleye, Stephanie C Ray
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Antioxidants, 2022 Recent studies suggest that improper resolution of acute neuroinflammation may lead to long-lasting low-grade chronic neuroinflammation and drive progressive neurodegeneration.
Jau-Shyong Hong +2 more
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The Mac1 ADP-ribosylhydrolase is a therapeutic target for SARS-CoV-2 [PDF]
eLifeSevere acute respiratory syndrome coronavirus 2 (SARS-CoV-2) continues to pose a threat to public health. Current therapeutics remain limited to direct-acting antivirals that lack distinct mechanisms of action and are already showing signs of viral ...
Rahul K Suryawanshi +30 more
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