Optimizing polar, small inhibitors of a viral cysteine protease to identify a lead for an oral COVID-19 treatment [Added supplements: COVID-19 Variant Supplement; COVID-19 Variant Network]

  • Funded by Canadian Institutes of Health Research (CIHR)
  • Total publications:0 publications

Grant number: 172655, 175551, 175573

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Key facts

  • Disease

    COVID-19
  • Start & end year

    2020
    2022
  • Known Financial Commitments (USD)

    $549,227.81
  • Funder

    Canadian Institutes of Health Research (CIHR)
  • Principal Investigator

    Pending
  • Research Location

    Canada
  • Lead Research Institution

    University of Alberta Biochemistry
  • Research Priority Alignment

    N/A
  • Research Category

    Therapeutics research, development and implementation

  • Research Subcategory

    Pre-clinical studies

  • Special Interest Tags

    N/A

  • Study Subject

    Non-Clinical

  • Clinical Trial Details

    N/A

  • Broad Policy Alignment

    Pending

  • Age Group

    Not Applicable

  • Vulnerable Population

    Not applicable

  • Occupations of Interest

    Not applicable

Abstract

The COVID-19 pandemic has caused incredible social, personal and economic upheaval and as of early May 2020 killed 275 000 people world-wide and, tragically, is projected to kill millions more. COVID-19 is caused by the SARS-CoV2 (SARS2) virus, which is a coronavirus closely related to SARS. These viruses infect cells and using the host's enzymes and virally encoded proteins create copies of themselves. These viral proteins are different than the host ones and are key targets to stop the viral replication. One such protein for SARS2, nicknamed 3CLP, is key to liberating the viral proteins in order to enable viral replication. Last month compounds we tested strongly inhibited the SARS2 3CLP and were able to inhibit SARS2 replication in a cell-based assay. This proposal is to design and make modifications of those compounds to better inhibit SARS2 and also optimize drug-like properties to discover a Lead compound for the ultimate development of an oral drug to treat COVID-19.