A5050699455- interferon and immune responses
- SARS-CoV-2 and COVID-19 Research
- COVID-19 Clinical Research Studies
- Aquaculture disease management and microbiota
- Neutrophil, Myeloperoxidase and Oxidative Mechanisms
- Protease and Inhibitor Mechanisms
- Antimicrobial Peptides and Activities
- Eosinophilic Disorders and Syndromes
- Viral Infections and Outbreaks Research
University of California, San Diego
2021-2024
University of Montana
2021
The host cell serine protease TMPRSS2 is an attractive therapeutic target for COVID-19 drug discovery. This activates the Spike protein of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and other coronaviruses essential viral spread in lung. Utilizing rational structure-based design (SBDD) coupled to substrate specificity screening TMPRSS2, we have discovered covalent small-molecule ketobenzothiazole (kbt) inhibitors which are structurally distinct from significantly improved...
Cathepsin L is a key host cysteine protease utilized by coronaviruses for cell entry and promising drug target novel antivirals against SARS-CoV-2. The marine natural product gallinamide A several synthetic analogues were identified as potent inhibitors of cathepsin with IC50 values in the picomolar range. Lead molecules possessed selectivity over other cathepsins alternative proteases involved viral entry. Gallinamide directly interacted cells and, together two lead analogues, potently...
Abstract The host cell serine protease TMPRSS2 is an attractive therapeutic target for COVID-19 drug discovery. This activates the Spike protein of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) and other coronaviruses essential viral spread in lung. Utilizing rational structure-based design (SBDD) coupled to substrate specificity screening TMPRSS2, we have discovered a novel class small molecule ketobenzothiazole inhibitors with significantly improved activity over existing...