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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
Joseph J O'Connor, Dana Ferraris, Anthony R Fehr   +2 more
exaly   +8 more sources

Identification of a series of pyrrolo-pyrimidine-based SARS-CoV-2 Mac1 inhibitors that repress coronavirus replication. [PDF]

mBio
Coronaviruses (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.
Pfannenstiel JJ, Duong MTH, Cluff D, Sherrill LM, Colquhoun I, Cadoux G, Thorne D, Pääkkönen J, Schemmel NF, O'Connor J, Saenjamsai P, Feng M, Parthasarathy S, Hageman MJ, Johnson DK, Roy A, Lehtiö L, Ferraris DV, Fehr AR.   +18 more
europepmc   +7 more sources

The Mac1 ADP-ribosylhydrolase is a therapeutic target for SARS-CoV-2. [PDF]

Elife
Severe 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 ...
Suryawanshi RK, Jaishankar P, Correy GJ, Rachman MM, O'Leary PC, Taha TY, Matsui Y, Zapatero-Belinchón FJ, McCavitt-Malvido M, Doruk YU, Stevens MGV, Diolaiti ME, Jogalekar MP, Chen H, Richards AL, Kongpracha P, Bali S, Montano M, Rosecrans J, Matthay M, Togo T, Gonciarz RL, Gopalkrishnan S, Neitz RJ, Krogan NJ, Swaney DL, Shoichet BK, Ott M, Renslo AR, Ashworth A, Fraser JS.   +30 more
europepmc   +7 more sources

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 ...
Dong-Ming Zhang, Shun-Hua Chen, Hui Zhou   +2 more
exaly   +4 more sources

Structure-Based High-Throughput Virtual Screening and Molecular Dynamics Simulation for the Discovery of Novel SARS-CoV-2 NSP3 Mac1 Domain Inhibitors

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).
Behnaz Yazdani, Hajar Sirous, Simone Brogi   +2 more
exaly   +5 more sources

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 Virology
All coronaviruses (CoVs) encode a conserved macrodomain, termed Mac1, in non-structural protein 3 (nsp3) that binds and hydrolyzes ADP-ribose covalently attached to proteins.
Joseph J O'Connor, Anuradha Roy, Nancy Schwarting   +2 more
exaly   +4 more sources

Activation of the MAC1-ERK1/2-NOX2 Pathway Is Required for LPS-Induced Sustaining Reactive Microgliosis, Chronic Neuroinflammation and Neurodegeneration

Antioxidants, 2022
Recent studies suggest that improper resolution of acute neuroinflammation may lead to long-lasting low-grade chronic neuroinflammation and drive progressive neurodegeneration.
Shuangyu Han, Dezhen Tu, Huiming Gao
exaly   +4 more sources

Examining the Effects of the RUNX1 p.Leu43Ser Variant on FPD/AML Phenotypes Using a CRISPR/Cas9-Generated Knock-In Murine Model. [PDF]

Biomolecules
Germline heterozygous variants in RUNX1 lead to Familial Platelet Disorder with Myeloid Leukemia Predisposition (FPD/AML). Cellular and/or animal models are helpful to uncovering the role of a variant in disease progression. Twenty-five mice per genotype
Marin-Quilez A, García-Tuñón I, Benito R, Ordoñez JL, Díaz-Ajenjo L, Lama-Villanueva A, Guerrero C, Pérez-Losada J, González-Porras JR, Hernández-Rivas JM, Del Rey M, Bastida JM.   +11 more
europepmc   +2 more sources

Molecular basis for loss of virulence in Magnaporthe oryzae strain AM16. [PDF]

Front Plant Sci
The rapid virulence variation of Magnaporthe oryzae (M. oryzae) to rice is a big challenge for rice blast control. Even though many studies have been done by scientists all over the world, the mechanism of virulence variation in M. oryzae remains elusive.
Deng J, Zhang Z, Wang X, Cao Y, Huang H, Wang M, Luo Q.   +6 more
europepmc   +2 more sources

Neuroprotective Potential of New Monoterpene-Adamatane Conjugates-A Pilot Study. [PDF]

Curr Issues Mol Biol
Neurodegenerative diseases, including Alzheimer’s disease, are marked by cholinergic dysfunction, oxidative stress, and reduced neurotrophic support, which drives the quest for multifunctional therapeutic agents.
Dragomanova S, Petkova-Kirova P, Volcho K, Reynisson J, Grigorova V, Uzunova D, Tsvetanova E, Georgieva A, Alexandrova A, Stefanova M, Minchev B, Popoola J, Chouha N, Munkuev A, Ponomarev K, Suslov E, Salakhutdinov N, Kalfin R, Tancheva L.   +18 more
europepmc   +2 more sources