Signal Transduction and Targeted Therapy has recently published a review article that reported the current expertise in the molecular communication of SARS-CoV-2.

There is one session in the article specifically talking about small-molecule compound-based antiviral properties, including small molecules targeting S protein of SARS-CoV-2, TMPRSS2 inhibitors, and cathepsin B/L inhibitors.

Below are some highlights from the article:

Small molecules targeting S protein

  • S protein of SARS-CoV-2 plays an important role in receptor recognition and virus-cell membrane fusion
  • Hydrophilic compound, Salvianolic acid isolated from traditional Chinese medicine, inhibited SAR-CoV-2 infection by blocking the formation of 6-helix bundle core in authentic SARS-CoV-2 inhibition assays
  • 2 drug-like compounds, DRI-C23041 and DRI-C91005, showed antiviral activity in obstructing the interaction between human angiotensin-converting enzyme 2 (hACE2) and SARS-CoV-2 S protein
  • DRI-C23041 inhibited the entry of SARS-CoV-2-S pseudo viral into ACE2-expressing cells

TMPRSS2 inhibitors

  • TMPRSS2 could be used as a potential target to avoid virus entry
  • Camostat mesylate, a TMPRSS2 inhibitor, significantly inhibited SARS-CoV-2 pseudo viral entry into Calu-3 cells
  • MI-432 and MI-1900, two prospective peptide mimetic inhibitors of TMPRSS2, demonstrated antiviral activity against SARS-CoV-2 infection in vitro

Cathepsin B/L inhibitors

  • Cellular cathepsins can prime viral S protein cleavage and benefit viral fusion, including cathepsin B and cathepsin L
  • P9, derived from mouse β-defensin-4, has broad-spectrum antiviral activity against multiple respiratory viruses by interfering with cathepsin L
  • E64-d, a broad cathepsin B/L inhibitor, showed inhibitory activity in a SARS-CoV-2 pseudovirus infection assay


Zhang Q, Xiang R, Huo S, Zhou Y, Jiang S, Wang Q, Yu F. Molecular mechanism of interaction between SARS-CoV-2 and host cells and interventional therapy. Signal Transduct Target Ther. 2021 Jun 11;6(1):233. doi: 10.1038/s41392-021-00653-w. PMID: 34117216; PMCID: PMC8193598.

Related products

Membrane transporter and protease

    Related brands

    Abmole BioScience is a rapidly growing, professional inhibitors supplier. Abmole provides high purity life science reagents such as kinase inhibitors for laboratory research. Abmole has a unique collection of over 5,000 inhibitors on HDAC, PI3K, Apoptosis and more signalling pathways in stock.

    Read more

    APExBIO Technology LLC is a premier provider of Small Molecule Inhibitors/Activators, Compound Libraries, Peptides, Assay Kits, Fluorescent Labels, Enzymes, Modified Nucleotides, mRNA synthesis and various tools for Molecular Biology. APExBIO carries a broad product line in over 20 different research areas such as cancer, immunology, neurosciences, apoptosis and epigenetics etc. 

    Read more

    Molnova Chemicals is a biotech enterprise, specializing in chemical and biological research products and services to meet the research needs of global customers. Molnova has evolved into one of the biggest global compounds and peptides supplier with over 11000 products from over 20 signaling pathways and 400 targets. They carry a broad product line over different research areas such as cancer, infection, immunology, neurosciences, apoptosis and metabolic disorder, etc.

    Read more

    LC Laboratories has been in business for 40 years, manufacturing and selling the products directly to researchers and through many distributors and other reagent-vendor customers worldwide. Almost all PMA (Phorbol 12-Myristate 13-Acetate; TPA), PDBu (Phorbol 12, 13-Dibutyrate) or Prostratin (12-Deoxyphorbol 13-Acetate) used in laboratory research is made by LC Laboratories. LC Laboratories is committed to providing products of the highest purity at the lowest prices.

    Read more

    Contact us for more COVID-related research products.

    Share This