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About:
Structure-Based Design and Synthesis of Triazole-based Macrocyclic Inhibitors of Norovirus Protease: Structural, Biochemical, Spectroscopic, and Antiviral Studies
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schema:ScholarlyArticle
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wasabi.inria.fr
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Type:
Academic Article
research paper
schema:ScholarlyArticle
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type
Academic Article
research paper
schema:ScholarlyArticle
isDefinedBy
Covid-on-the-Web dataset
has title
Structure-Based Design and Synthesis of Triazole-based Macrocyclic Inhibitors of Norovirus Protease: Structural, Biochemical, Spectroscopic, and Antiviral Studies
Creator
Chang, Kyeong-Ok
Kim, Yunjeong
Lovell, Scott
Mehzabeen, Nurjahan
Alliston, Kevin
Battaile, Kevin
Damalanka, Vishnu
Kankanamalage, Anushka
Lushington, Gerald
Weerawarna, Pathum
Groutas, C
William, +
Source
Elsevier; Medline; PMC
abstract
Outbreaks of acute gastroenteritis caused by noroviruses constitute a public health concern worldwide. To date, there are no approved drugs or vaccines for the management and prophylaxis of norovirus infections. A potentially effective strategy for the development of norovirus therapeutics entails the discovery of inhibitors of norovirus 3CL protease, an enzyme essential for noroviral replication. We describe herein the structure-based design of the first class of permeable, triazole-based macrocyclic inhibitors of norovirus 3C-like protease, as well as pertinent X-ray crystallographic, biochemical, spectroscopic, and antiviral studies.
has issue date
2016-08-01
(
xsd:dateTime
)
bibo:doi
10.1016/j.ejmech.2016.04.013
bibo:pmid
27235842
has license
hybrid-oa
sha1sum (hex)
e4cd0379bd512b707c6c503dddb9f29c92b17625
schema:url
https://doi.org/10.1016/j.ejmech.2016.04.013
resource representing a document's title
Structure-Based Design and Synthesis of Triazole-based Macrocyclic Inhibitors of Norovirus Protease: Structural, Biochemical, Spectroscopic, and Antiviral Studies
has PubMed Central identifier
PMC4916972
has PubMed identifier
27235842
schema:publication
European Journal of Medicinal Chemistry
resource representing a document's body
covid:e4cd0379bd512b707c6c503dddb9f29c92b17625#body_text
is
schema:about
of
named entity 'DRUGS'
named entity 'DEVELOPMENT'
named entity 'VACCINES'
named entity 'LIKE'
named entity 'NOROVIRUSES'
named entity 'REPLICATION'
named entity 'ENZYME'
named entity 'NOROVIRUS'
named entity 'INHIBITORS'
named entity 'DESIGN'
named entity 'NOROVIRUS INFECTIONS'
named entity 'ACUTE GASTROENTERITIS'
named entity 'BIOCHEMICAL'
named entity 'STRUCTURAL'
named entity 'SYNTHESIS'
named entity 'BASED'
named entity 'INHIBITORS'
named entity 'TRIAZOLE'
named entity 'DESIGN'
named entity 'CONCERN'
named entity 'WORLDWIDE'
named entity 'PROTEASE'
named entity 'ANTIVIRAL'
named entity 'STUDIES'
named entity 'PERMEABLE'
named entity 'MANAGEMENT'
named entity 'ANTIVIRAL'
named entity 'DESCRIBE'
named entity 'PROPHYLAXIS OF'
named entity 'THERAPEUTICS'
named entity 'PROTEASE'
named entity 'STRATEGY'
named entity 'CLASS'
named entity 'BASED'
named entity 'STRUCTURE'
named entity 'OUTBREAKS'
named entity 'STRUCTURE'
named entity 'NOROVIRUS'
named entity 'DATE'
named entity 'X-RAY'
named entity 'DISCOVERY'
named entity 'EFFECTIVE'
named entity 'BIOCHEMICAL'
named entity 'TRIAZOLE'
named entity 'PUBLIC HEALTH'
named entity 'APPROVED'
named entity 'CAUSED BY'
named entity 'STUDIES'
named entity 'ESSENTIAL'
named entity 'macrocyclic'
named entity 'triazole'
named entity 'structure-based design'
named entity 'vaccines'
named entity 'Triazole'
named entity 'active site'
named entity 'norovirus'
named entity 'triazole'
named entity 'morbidity'
named entity '3CLpro'
named entity 'cyclization'
named entity 'X-ray crystal structure'
named entity 'HCl'
named entity 'proteases'
named entity 'esters'
named entity 'protons'
named entity 'amino acid residues'
named entity 'open reading frames'
named entity 'enzyme'
named entity '3CLpro'
named entity 'single stranded RNA'
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