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Cell-free assays reveal that the HIV-1 capsid protects reverse transcripts from cGAS immune sensing.
PLoS Pathog
January 2025
Division of Microbiology and Immunology, Department of Pathology, University of Utah School of Medicine, Salt Lake City, Utah, United States of America.
Retroviruses can be detected by the innate immune sensor cyclic GMP-AMP synthase (cGAS), which recognizes reverse-transcribed DNA and activates an antiviral response. However, the extent to which HIV-1 shields its genome from cGAS recognition remains unclear. To study this process in mechanistic detail, we reconstituted reverse transcription, genome release, and innate immune sensing of HIV-1 in a cell-free system.
View Article and Find Full Text PDFA Review of Bavachinin and Its Derivatives as Multi-therapeutic Agents.
Chem Biodivers
January 2025
Gannan Medical University, Depatment of Medicinal Chemistry, Gannan Medical University, 341000, Ganzhou, CHINA.
Extracting natural active ingredients from plants is an effective way to develop and screen modern drugs. Psoralea corylifolia is a leguminous plant whose seeds have long been used as a Traditional Chinese Medicine to treat psoriasis, rheumatism, dermatitis, and other diseases. To date, several main compounds, including coumarins, flavonoids, monoterpene phenols, and benzofurans, have been identified from the seeds of Psoralea corylifolia.
View Article and Find Full Text PDFConformational flexibility is a critical factor in designing broad-spectrum human norovirus protease inhibitors.
J Virol
January 2025
Verna and Marrs McLean Department of Biochemistry and Molecular Pharmacology, Baylor College of Medicine, Houston, Texas, USA.
Unlabelled: Human norovirus (HuNoV) is a leading cause of gastroenteritis worldwide and is associated with significant morbidity, mortality, and economic impact. There are currently no licensed antiviral drugs for the treatment of HuNoV-associated gastroenteritis. The HuNoV protease plays a critical role in the initiation of virus replication by cleaving the polyprotein.
View Article and Find Full Text PDFInvestigation of Pyrrole Analogues Inhibition on Mpro by Spectroscopic Analysis, Molecular Docking and Enzyme Activity.
Chem Biodivers
January 2025
Zhengzhou University, College of Chemistry, Kexue Road 100, 450001, Zhengzhou, CHINA.
The main protease (Mpro) is a cysteine enzyme and represents a vital target for antiviral drug screening. In this work, Twenty-five pyrrole derivatives were synthesized and screened by enzyme activity experiments. Results indicate that six pyrrole derivatives can bind to Mpro and have inhibitory effect on Mpro.
View Article and Find Full Text PDFSynthesis and biological investigation of peptidomimetic SARS-CoV-2 main protease inhibitors bearing quinoline-based heterocycles at P.
Arch Pharm (Weinheim)
January 2025
Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Siena, Italy.
In the last few years, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has been the cause of a worldwide pandemic, highlighting the need for novel antiviral agents. The main protease (M) of SARS-CoV-2 was immediately identified as a crucial enzyme for viral replication and has been validated as a drug target. Here, we present the design and synthesis of peptidomimetic M covalent inhibitors characterized by quinoline-based P moieties.
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