About: Antiviral Drug Discovery: Norovirus Proteases and Development of Inhibitors

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An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Antiviral Drug Discovery: Norovirus Proteases and Development of Inhibitors
Creator	Chang, Kyeong-Ok Kim, Yunjeong Lovell, Scott Groutas, William Rathnayake, Athri
Source	Medline; PMC
abstract	Proteases are a major enzyme group playing important roles in a wide variety of biological processes in life forms ranging from viruses to mammalians. The aberrant activity of proteases can lead to various diseases; consequently, host proteases have been the focus of intense investigation as potential therapeutic targets. A wide range of viruses encode proteases which play an essential role in viral replication and, therefore, constitute attractive targets for the development of antiviral therapeutics. There are numerous examples of successful drug development targeting cellular and viral proteases, including antivirals against human immunodeficiency virus and hepatitis C virus. Most FDA-approved antiviral agents are peptidomimetics and macrocyclic compounds that interact with the active site of a targeted protease. Norovirus proteases are cysteine proteases that contain a chymotrypsin-like fold in their 3D structures. This review focuses on our group’s efforts related to the development of norovirus protease inhibitors as potential anti-norovirus therapeutics. These protease inhibitors are rationally designed transition-state inhibitors encompassing dipeptidyl, tripeptidyl and macrocyclic compounds. Highly effective inhibitors validated in X-ray co-crystallization, enzyme and cell-based assays, as well as an animal model, were generated by launching an optimization campaign utilizing the initial hit compounds. A prodrug approach was also explored to improve the pharmacokinetics (PK) of the identified inhibitors.
has issue date	2019-02-25(xsd:dateTime)
bibo:doi	10.3390/v11020197
bibo:pmid	30823509
has license	cc-by
sha1sum (hex)	8bf3d561863300dbcb9ba92ad94807dfb8775f7a
schema:url	https://doi.org/10.3390/v11020197
resource representing a document's title	Antiviral Drug Discovery: Norovirus Proteases and Development of Inhibitors
has PubMed Central identifier	PMC6410195
has PubMed identifier	30823509
schema:publication	Viruses
resource representing a document's body	covid:8bf3d561863300dbcb9ba92ad94807dfb8775f7a#body_text
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