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Review
. 2021;27(3):254-256.
doi: 10.1007/s12268-021-1576-6. Epub 2021 May 11.

SARS-CoV-PLpro-Inhibitoren als mögliche Breitspektrum-Virostatika

[Article in German]
Affiliations
Review

SARS-CoV-PLpro-Inhibitoren als mögliche Breitspektrum-Virostatika

[Article in German]
Stefan Josef Hammerschmidt et al. Biospektrum (Heidelb). 2021.

Abstract

The SARS-CoV-encoded papain-like cysteine protease (PLpro) plays crucial roles in viral replication and maturation processes. It is required to cleave the precursor polyproteins into functional proteins. Thus, it is considered to be a promising target for developing specific drugs. For rational optimization of hit compounds, information about the structure-activity relationship (SAR) is fundamental. Herein, we characterize isoindolines as a new class of PLpro inhibitors.

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References

    1. Welker A, Kersten C, Müller C, et al. Structure-activity relationships of benzamides and isoindolines designed as SARS-CoV protease inhibitors effective against SARS-CoV-2. ChemMedChem. 2021;16:340–354. doi: 10.1002/cmdc.202000548. - DOI - PMC - PubMed
    1. Amendola G, Ettari R, Previti S et al. (2021) Lead discovery of SARS-CoV-2 main protease inhibitors through covalent docking-based virtual screening. J Chem Inf Model, 10.1021/acs.jcim.1c00184 - PubMed
    1. Shin D, Mukherjee R, Grewe D, et al. Papain-like protease regulates SARS-CoV-2 viral spread and innate immunity. Nature. 2020;587:657–662. doi: 10.1038/s41586-020-2601-5. - DOI - PMC - PubMed
    1. Ratia K, Pegan S, Takayama J, et al. A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replication. Proc Natl Acad Sci. 2008;105:16119–16124. doi: 10.1073/pnas.0805240105. - DOI - PMC - PubMed
    1. Ghosh A, Takayama J, Rao K, et al. Severe acute respiratory syndrome coronavirus papain-like novel protease inhibitors: design, synthesis, protein-ligand X-Ray structure and biological evaluation. J Med Chem. 2010;53:4968–4979. doi: 10.1021/jm1004489. - DOI - PMC - PubMed

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