Protease Inhibitor Assay of SARS-CoV-2

Proteases play an important role in protein activation, cell regulation and signal transduction, and amino acid production. The proteolytic processing of coronavirus major proteases through replication enzyme polyprotein plays a key role in viral gene expression and replication and is an attractive target for anti-CoV drug design. The viral proteases necessary to inhibit the proteolytic processing of polyproteins have been successful strategies for the treatment of human immunodeficiency virus (HIV) and hepatitis C, respectively, proving that protease inhibitors can be used to treat viral infections. Similarly, the main protease of SARS-CoV-2 is considered to be essential for viral replication, and therefore is considered a promising target for COVID-19 antiviral therapy. To find and validate potent inhibitors for SARS-CoV-2 protease, Creative Biolabs provides protease assay service to help speed up the development of therapeutics to conquer COVID-19.

Protease Inhibitor Assay of SARS-CoV-2

Inhibitors of TMPRSS2 Serine Protease

TMPRSS2 is a type II transmembrane serine protease (TTSP) and is essential for proteolytic activation and spread of SARS-CoV-2 in epithelial cells of the respiratory, which provide promising drug targets for the treatment of respiratory virus infections. SARS-CoV-2 uses TMPRSS2 for spike protein priming and S protein-driven cell entry. Inhibitors of TMPRSS2 may block the entry of SARS-CoV-2 virus into cells and therefore represent potential drug targets.

  • TMPRSS2 Enhanced Cell Lines
CAT Product Name Product Overview
VCeL-Wyb047 TMPRSS2 enhanced Caco-2 Cell Line TMPRSS2 enhanced human epithelial colorectal adenocarcinoma cell
VCeL-Wyb048 TMPRSS2 enhanced MCF-7 Cell Line TMPRSS2 enhanced human breast cancer cell
VCeL-Wyb049 TMPRSS2 enhanced SK-BR-3 Cell Line TMPRSS2 enhanced human breast cancer cell
VCeL-Wyb050 TMPRSS2 enhanced T-47D Cell Line TMPRSS2 enhanced human breast cancer cell
  • ACE2 and TMPRSS2 Co-Enhanced Cell Line
CAT Product Name Product Overview
VCeL-Wyb051 ACE2-TMPRSS2 co-enhanced RT4 Cell Line ACE2-TMPRSS2 co-enhanced human bladder carcinoma cell
VCeL-Lsx001 TMPRSS2 enhanced VeroE6 Cell Line VeroE6 cells stably express transmembrane serine protease TMPRSS2.

Inhibitors of Furin

The proprotein convertase (PC) furin is a type I transmembrane protein that is widely expressed in eukaryotic cells and tissues. Furin cleaves the precursors of a broad range of proteins and has been identified as an activating protease for the fusion proteins of various viruses. It is also essential for SARS-CoV-2 activation in human airway cells. Inhibitors of furin may block the entry of SARS-CoV-2 virus into cells and are promising drug targets for the treatment of COVID-19.

Evaluation of Inhibitors for SARS-CoV-2 Protease

To help accelerate the development of anti-SARS-CoV-2 therapeutics, Creative Biolabs can provide protease assays to evaluate inhibitors of SARS-CoV-2 proteases:

  • Spike-pseudovirus Based Neutralization Assay
  • FRET-based assay
  • Dose-response titration
  • Thermal shift binding assay
  • Counter screening assays
  • Cellular cytotoxicity test
  • Viral yield reduction (VYR) assay
  • SARS-CoV-2 CPE assay
  • Differential scanning fluorimetry

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