In Silico Binding of 2-Aminocyclobutanones to SARS-CoV-2 Nsp13 Helicase and Demonstration of Antiviral Activity.

HTS SAR antiviral carbonyl hydrate computer-aided drug design coronavirus variants cyclobutanone enzyme inhibitor high-throughput in silico screen nonstructural protein 13, Nsp13 helicase peptidomimetics transition state mimetic

Journal

International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791

Informations de publication

Date de publication:
07 Mar 2023
Historique:
received: 23 01 2023
revised: 22 02 2023
accepted: 02 03 2023
medline: 30 3 2023
entrez: 29 3 2023
pubmed: 30 3 2023
Statut: epublish

Résumé

The landscape of viral strains and lineages of SARS-CoV-2 keeps changing and is currently dominated by Delta and Omicron variants. Members of the latest Omicron variants, including BA.1, are showing a high level of immune evasion, and Omicron has become a prominent variant circulating globally. In our search for versatile medicinal chemistry scaffolds, we prepared a library of substituted ɑ-aminocyclobutanones from an ɑ-aminocyclobutanone synthon (

Identifiants

pubmed: 36982188
pii: ijms24065120
doi: 10.3390/ijms24065120
pmc: PMC10049026
pii:
doi:

Substances chimiques

Antiviral Agents 0
RNA Helicases EC 3.6.4.13
Viral Nonstructural Proteins 0
DNA Helicases EC 3.6.4.-

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Subventions

Organisme : Loyola University Chicago
ID : IPRS #1083

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Auteurs

Thahani S Habeeb Mohammad (TSH)

Department of Chemistry and Biochemistry, Loyola University Chicago, Chicago, IL 60660, USA.

Yash Gupta (Y)

Department of Medicine, Division of Infectious Diseases, Mayo Clinic, Jacksonville, FL 32224, USA.

Cory T Reidl (CT)

Department of Chemistry and Biochemistry, Loyola University Chicago, Chicago, IL 60660, USA.

Vlad Nicolaescu (V)

Howard T. Ricketts Laboratory, Department of Microbiology, The University of Chicago, Chicago, IL 60637, USA.

Haley Gula (H)

Howard T. Ricketts Laboratory, Department of Microbiology, The University of Chicago, Chicago, IL 60637, USA.

Ravi Durvasula (R)

Department of Medicine, Division of Infectious Diseases, Mayo Clinic, Jacksonville, FL 32224, USA.

Prakasha Kempaiah (P)

Department of Medicine, Division of Infectious Diseases, Mayo Clinic, Jacksonville, FL 32224, USA.

Daniel P Becker (DP)

Department of Chemistry and Biochemistry, Loyola University Chicago, Chicago, IL 60660, USA.

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Classifications MeSH