Epigenetic BET-inhibition to combat COVID-19
CALGARY, Alberta, March 24, 2020 (GLOBE NEWSWIRE) -- Resverlogix Corp. ("Resverlogix" or the "Company") (TSX:RVX) is pleased to announce a March 23, 2020 bioRxiv publication that has shown apabetalone to inhibit specialized proteins – called bromodomain and extraterminal domain (BET) proteins – from interacting with a SARS-CoV-2 viral protein, with potential for limiting viral reproduction in human cells.
The article titled: “A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing” by Gordon et al, identified BRD2/4 as a binding partner of viral protein E. Apabetalone was shown to disrupt this interaction. A paragraph in the publication states the following about Bromodomain proteins:
SARS-CoV-2 envelope interacts with bromodomain proteins
Surprisingly, we find that the transmembrane protein E binds to the bromodomain-containing proteins BRD2 and BRD4, potentially disrupting BRD-histone binding by mimicking histone structure. BRD2 is a member of the bromodomain and extra-terminal (BET) domain family whose members bind acetylated histones to regulate gene transcription. The N-terminus of histone 2A shares local sequence similarity over an alpha-helix of approximately 15 residues, some of which are in a transmembrane segment, of Protein E (Gordon et al., 2020, p.7).
“This novel research is certainly very encouraging and warrants additional testing of apabetalone, our investigational phase 3 clinical candidate with safety data in more than 4,000 subjects,” said Donald McCaffrey, President and CEO of Resverlogix. “Harnessing epigenetic modulation may be a potent tool in slowing down COVID-19 virus spread and disease severity, and as we announced yesterday, we would like to collaborate quickly with anyone who is testing drugs for COVID-19 in preclinical and clinical studies.”
Interested COVID-19 collaborators can contact:
Donald McCaffrey, President & CEO
Resverlogix is developing apabetalone (RVX-208), a first-in-class, small molecule that is a selective BET (bromodomain and extra-terminal) inhibitor. Apabetalone is the first therapy of its kind to have been granted US FDA Breakthrough Therapy Designation – for a major cardiovascular indication – to help facilitate a time-efficient drug development program including planned clinical trials and plans for expediting the manufacturing development strategy.
BET inhibition is an epigenetic mechanism that can regulate disease-causing genes. Apabetalone is a BET inhibitor selective for the second bromodomain (BD2) within the BET proteins. This selective inhibition of apabetalone on BD2 produces a specific set of biological effects with potentially important benefits for patients with high-risk cardiovascular disease, diabetes mellitus, chronic kidney disease, end-stage renal disease treated with hemodialysis, neurodegenerative disease, Fabry disease, peripheral artery disease and other orphan diseases, while maintaining a well described safety profile.
Resverlogix common shares trade on the Toronto Stock Exchange (TSX:RVX).
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This news release may contain certain forward-looking information as defined under applicable Canadian securities legislation, that are not based on historical fact, including without limitation statements containing the words "believes", "anticipates", "plans", "intends", "will", "should", "expects", "continue", "estimate", "forecasts" and other similar expressions. In particular, this news release includes forward looking information related to the potential benefit of apabetalone – through its known mechanism of action – in the treatment of patients with COVID-19 and the potential role of apabetalone in the treatment of patients with cognitive disorders, high-risk cardiovascular disease, diabetes mellitus, chronic kidney disease, end-stage renal disease treated with hemodialysis, Fabry disease, peripheral artery disease and other orphan diseases. Our actual results, events or developments could be materially different from those expressed or implied by these forward-looking statements. We can give no assurance that any of the events or expectations will occur or be realized. By their nature, forward-looking statements are subject to numerous assumptions and risk factors including those discussed in our Annual Information Form and most recent MD&A which are incorporated herein by reference and are available through SEDAR at www.sedar.com. The forward-looking statements contained in this news release are expressly qualified by this cautionary statement and are made as of the date hereof. The Company disclaims any intention and has no obligation or responsibility, except as required by law, to update or revise any forward-looking statements, whether as a result of new information, future events or otherwise.