The development of novel agents to combat COVID-19 is of high importance. SARS-CoV-2 main protease (M) is a highly attractive target for the development of novel antivirals and a variety of inhibitors have already been developed. Accumulating evidence on the pathobiology of COVID-19 has shown that lipids and lipid metabolizing enzymes are critically involved in the severity of the infection. The purpose of the present study was to identify an inhibitor able to simultaneously inhibit both SARS-CoV-2 M and phospholipase A (PLA), an enzyme which plays a significant role in inflammatory diseases. Evaluating several PLA inhibitors, we demonstrate that the previously known potent inhibitor of Group IIA secretory PLA, GK241, may also weakly inhibit SARS-CoV-2 M. Molecular mechanics docking and molecular dynamics calculations shed light on the interactions between GK241 and SARS-CoV-2 M. 2-Oxoamide GK241 may represent a lead molecular structure for the development of dual PLA and SARS-CoV-2 M inhibitors.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9414318 | PMC |
| http://dx.doi.org/10.3390/ph15080961 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Knowledge and behavior towards COVID-19 in the northern region of the state of Rio de Janeiro - Brazil.
J Infect Dev Ctries
December 2024
Faculdade de Medicina de Campos, Campos dos Goytacazes, Brazil.
Introduction: Despite efforts by health organizations to share evidence-based information, fake news hindered the promotion of social distancing and vaccination during the coronavirus disease 2019 (COVID-19) pandemic. This study analyzed COVID-19 knowledge and practices in a vulnerable area in northern Rio de Janeiro, acknowledging the influence of the complex social and economic landscape on public health perceptions.
Methodology: This cross-sectional study was conducted in Novo Eldorado - a low-income, conflict-affected neighborhood in Campos dos Goytacazes - using a structured questionnaire, following the peak of COVID-19 deaths in Brazil (July-December 2021).
Hospital attendance, malaria prevalence and self-medication with an antimalarial drug before and after the start of COVID-19 pandemic in a sentinel site for malaria surveillance in Gabon.
Malar J
January 2025
Department of Parasitology-Mycology and Tropical Medicine, Université Des Sciences de La Santé de Libreville, BP 4009, Libreville, Gabon.
Background: The negative impact of COVID-19 pandemic on healthcare service utilization has been reported in several countries. In Gabon, data on the preparedness for future pandemic are lacking. The aim of the present study was to assess the trends of hospital attendance, malaria and self-medication prevalences as well as ITN use before and during Covid-19 first epidemic waves in a paediatric wards of a sentinel site for malaria surveillance, in Libreville, Gabon.
View Article and Find Full Text PDFIntroducing and establishing birth companionship in labour ward of a tertiary care centre in North India: a quality improvement journey through and beyond COVID-19 pandemic.
BMJ Open Qual
January 2025
Professor Department of Obstetrics and Gynaecology, Lady Hardinge Medical College, New Delhi, India.
Background: Allowing a birth companion is the basic right of a mother and is identified as an important component of respectful maternity care. The implementation of this intervention has been a challenge in heavy-load public health facilities in India.
Local Problem: Despite the proven benefits of the presence of birth companions on maternal-fetal outcomes, there was no policy of allowing birth companions in our hospital.
The Ability of Combined Flavonol and Trihydroxyorganic Acid to Suppress SARS-CoV-2 Reproduction.
Viruses
December 2024
Scientific Research Institute for Biological Safety Problems, Ministry of Health of Kazakhstan, Almaty 080409, Kazakhstan.
The global burden of COVID-19 continues to rise, and despite significant progress in vaccine development, there remains a critical need for effective treatments for the severe inflammation and acute lung injury associated with SARS-CoV-2 infection. In this study, we explored the antiviral properties of a plant-derived complex consisting of flavonol and hydroxyorganic acid compounds. Our research focused on the ability of the flavonol and hydroxyorganic acid complex to suppress the activity of several key proteins involved in the replication and maturation of SARS-CoV-2.
View Article and Find Full Text PDFPatterns of Isoform Variation for N Gene Subgenomic mRNAs in Betacoronavirus Transcriptomes.
Viruses
December 2024
Department of Biology, Center for Computational and Integrative Biology, Rutgers University, Camden, NJ 08102, USA.
The nucleocapsid (N) protein is the most expressed protein in later stages of SARS-CoV-2 infection with several important functions. It is translated from a subgenomic mRNA (sgmRNA) formed by template switching during transcription. A recently described translation initiation site (TIS) with a CTG codon in the leader sequence (TIS-L) is out of frame with most structural and accessory genes including the N gene and may act as a translation suppressor.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!