A novel compound active against SARS-CoV-2 targeting uridylate-specific endoribonuclease (NendoU/NSP15):


Journal

RSC medicinal chemistry
ISSN: 2632-8682
Titre abrégé: RSC Med Chem
Pays: England
ID NLM: 101759460

Informations de publication

Date de publication:
20 Oct 2021
Historique:
received: 17 06 2021
accepted: 17 08 2021
entrez: 15 11 2021
pubmed: 16 11 2021
medline: 16 11 2021
Statut: epublish

Résumé

NendoU (NSP15) is an Mn(2+)-dependent, uridylate-specific enzyme, which leaves 2'-3'-cyclic phosphates 5' to the cleaved bond. Our in-house library was subjected to high throughput virtual screening (HTVS) to identify compounds with potential to inhibit NendoU enzyme, high-rank compounds (those that bound to multiple target structures) were further subjected to 100 nanoseconds MD simulations. Among these, one was found to be bound highly stable within the active site of the NendoU protein structure. Here, we are reporting a derivative of piperazine based '(2

Identifiants

pubmed: 34778776
doi: 10.1039/d1md00202c
pii: d1md00202c
pmc: PMC8528204
doi:

Types de publication

Journal Article

Langues

eng

Pagination

1757-1764

Informations de copyright

This journal is © The Royal Society of Chemistry.

Déclaration de conflit d'intérêts

The authors declare no conflict of interest.

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Auteurs

Sumit Kumar (S)

Department of Chemistry, Miranda House, University of Delhi Delhi India poonam.chemistry@mirandahouse.ac.in.

Yash Gupta (Y)

Division of Infectious Diseases Mayo Clinic, Jacksonville Florida USA Kempaiah.Prakasha@mayo.edu.

Samantha E Zak (SE)

United States Army Medical Research Institute of Infectious Diseases Fort Detrick MD USA.
The Geneva Foundation 917 Pacific Avenue Tacoma WA USA.

Charu Upadhyay (C)

Department of Chemistry, Miranda House, University of Delhi Delhi India poonam.chemistry@mirandahouse.ac.in.

Neha Sharma (N)

Laboratory for Translational Chemistry and Drug Discovery, Department of Chemistry, Hansraj College, University of Delhi India brijeshrathi@hrc.du.ac.in.

Andrew S Herbert (AS)

United States Army Medical Research Institute of Infectious Diseases Fort Detrick MD USA.

Ravi Durvasula (R)

Division of Infectious Diseases Mayo Clinic, Jacksonville Florida USA Kempaiah.Prakasha@mayo.edu.

Vladimir Potemkin (V)

South Ural State University, Laboratory of Computational Modelling of Drugs 454080 Russia.

John M Dye (JM)

United States Army Medical Research Institute of Infectious Diseases Fort Detrick MD USA.
The Geneva Foundation 917 Pacific Avenue Tacoma WA USA.
Department of Chemistry, Miranda House, University of Delhi Delhi India poonam.chemistry@mirandahouse.ac.in.

Prakasha Kempaiah (P)

Division of Infectious Diseases Mayo Clinic, Jacksonville Florida USA Kempaiah.Prakasha@mayo.edu.

Brijesh Rathi (B)

Laboratory for Translational Chemistry and Drug Discovery, Department of Chemistry, Hansraj College, University of Delhi India brijeshrathi@hrc.du.ac.in.
South Ural State University, Laboratory of Computational Modelling of Drugs 454080 Russia.

Classifications MeSH