Structural basis for the in vitro efficacy of nirmatrelvir against SARS-CoV-2 variants.


Journal

The Journal of biological chemistry
ISSN: 1083-351X
Titre abrégé: J Biol Chem
Pays: United States
ID NLM: 2985121R

Informations de publication

Date de publication:
06 2022
Historique:
received: 28 02 2022
revised: 18 04 2022
accepted: 19 04 2022
pubmed: 25 4 2022
medline: 30 6 2022
entrez: 24 4 2022
Statut: ppublish

Résumé

The COVID-19 pandemic continues to be a public health threat with emerging variants of SARS-CoV-2. Nirmatrelvir (PF-07321332) is a reversible, covalent inhibitor targeting the main protease (M

Identifiants

pubmed: 35461811
pii: S0021-9258(22)00412-4
doi: 10.1016/j.jbc.2022.101972
pmc: PMC9023115
pii:
doi:

Substances chimiques

Lactams 0
Nitriles 0
Viral Protease Inhibitors 0
Viral Proteins 0
nirmatrelvir 7R9A5P7H32
Proline 9DLQ4CIU6V
Cysteine Endopeptidases EC 3.4.22.-
Coronavirus 3C Proteases EC 3.4.22.28
Leucine GMW67QNF9C

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

101972

Informations de copyright

Copyright © 2022 The Authors. Published by Elsevier Inc. All rights reserved.

Déclaration de conflit d'intérêts

Conflict of interest All authors are employees of Pfizer, Inc and may hold or own shares of stock.

Références

Nature. 2020 Mar;579(7798):270-273
pubmed: 32015507
Science. 2012 May 25;336(6084):1030-3
pubmed: 22628654
Cell Res. 2022 May;32(5):498-500
pubmed: 35292745
J Med Chem. 2020 Nov 12;63(21):12725-12747
pubmed: 33054210
Acta Pharmacol Sin. 2020 Sep;41(9):1167-1177
pubmed: 32737471
Science. 2021 Dec 24;374(6575):1586-1593
pubmed: 34726479
AAPS J. 2021 Jan 5;23(1):14
pubmed: 33400058
Nat Commun. 2021 Oct 18;12(1):6055
pubmed: 34663813
Antiviral Res. 2022 Feb;198:105252
pubmed: 35085683
Cell Res. 2022 Mar;32(3):322-324
pubmed: 35058606
Bioorg Med Chem Lett. 2022 Apr 15;62:128629
pubmed: 35182772
J Virol. 2022 Apr 27;96(8):e0201321
pubmed: 35389231
Nat Microbiol. 2020 Apr;5(4):536-544
pubmed: 32123347

Auteurs

Samantha E Greasley (SE)

Medicine Design, Pfizer Worldwide Research, Development & Medical, La Jolla, California, USA.

Stephen Noell (S)

Medicine Design, Pfizer Worldwide Research, Development & Medical, Groton, Connecticut, USA.

Olga Plotnikova (O)

Medicine Design, Pfizer Worldwide Research, Development & Medical, Groton, Connecticut, USA.

RoseAnn Ferre (R)

Medicine Design, Pfizer Worldwide Research, Development & Medical, La Jolla, California, USA.

Wei Liu (W)

Medicine Design, Pfizer Worldwide Research, Development & Medical, La Jolla, California, USA.

Ben Bolanos (B)

Medicine Design, Pfizer Worldwide Research, Development & Medical, La Jolla, California, USA.

Kimberly Fennell (K)

Medicine Design, Pfizer Worldwide Research, Development & Medical, Groton, Connecticut, USA.

Jennifer Nicki (J)

Medicine Design, Pfizer Worldwide Research, Development & Medical, Groton, Connecticut, USA.

Tim Craig (T)

Medicine Design, Pfizer Worldwide Research, Development & Medical, Groton, Connecticut, USA.

Yuao Zhu (Y)

VRD Bacterial Vaccines, Pfizer Worldwide Research, Development & Medical, Pearl River, New York, USA.

Al E Stewart (AE)

Medicine Design, Pfizer Worldwide Research, Development & Medical, La Jolla, California, USA.

Claire M Steppan (CM)

Medicine Design, Pfizer Worldwide Research, Development & Medical, Groton, Connecticut, USA. Electronic address: claire.m.steppan@pfizer.com.

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Classifications MeSH