[HTML][HTML] Inhibitors of sars-cov-2 plpro

DJ Calleja, G Lessene, D Komander - Frontiers in chemistry, 2022 - frontiersin.org
… structures with small molecule inhibitors bound in a surprising … SARS-CoV PLpro inhibitor
GRL-0617, and recapitulate how new GRL-0617 derivatives exploit different features of PLpro, …

High-throughput screening identifies established drugs as SARS-CoV-2 PLpro inhibitors

Y Zhao, X Du, Y Duan, X Pan, Y Sun, T You… - Protein & …, 2021 - academic.oup.com
SARS-CoV-2 PLpro inhibition activity as the primary screening tool for the discovery of the
small molecule inhibitors, … four compounds that strongly inhibit SARS-CoV-2 PLpro. These are …

[HTML][HTML] Identification of SARS-CoV-2 inhibitors targeting Mpro and PLpro using in-cell-protease assay

A Narayanan, M Narwal, SA Majowicz… - Communications …, 2022 - nature.com
… -CoV-2 antivirals. Additionally, we show that the combined inhibition of Mpro and PLpro
is more effective in inhibiting SARS-CoV-2 and the delta variant. …

Mechanism and inhibition of the papain‐like protease, PLpro, of SARSCoV‐2

T Klemm, G Ebert, DJ Calleja, CC Allison… - The EMBO …, 2020 - embopress.org
… SARS2 PLpro identified no compounds that inhibited PLpro … molecule SARS PLpro inhibitors
also target SARS2 PLpro, … excellent antiviral activity in a SARS-CoV-2 infection model. …

Design of SARS-CoV-2 PLpro inhibitors for COVID-19 antiviral therapy leveraging binding cooperativity

Z Shen, K Ratia, L Cooper, D Kong, H Lee… - Journal of medicinal …, 2021 - ACS Publications
… again the challenge in developing potent PLpro inhibitors. … potent PLpro inhibitors would
require exploiting binding cooperativity to leverage multiple shallow binding sites on the PLpro

Discovery of PLpro and Mpro Inhibitors for SARS-CoV-2

AC Puhl, AS Godoy, GD Noske, AM Nakamura… - ACS …, 2023 - ACS Publications
… We additionally tested several kinase inhibitors and … 50 3.33 ± 0.06 μM) as PL pro inhibitors
for the first time. In some … this virus, or we have used Calu-3 cells infected with SARS-CoV-2…

Identification of SARSCoV‐2 Papain‐like Protease (PLpro) Inhibitors Using Combined Computational Approach

M Sencanski, V Perovic, J Milicevic… - …, 2022 - Wiley Online Library
… as potential SARS-CoV-2 PLpro inhibitors that we … PLpro inhibitor, showed antiviral action
against SARS-CoV-2. Quinine, proposed as PLpro inhibitor in this work, inhibited SARS-CoV-…

[HTML][HTML] The complex structure of GRL0617 and SARS-CoV-2 PLpro reveals a hot spot for antiviral drug discovery

Z Fu, B Huang, J Tang, S Liu, M Liu, Y Ye, Z Liu… - Nature …, 2021 - nature.com
… 6 from promising SARS-CoV PLpro inhibitors 26,29 based … data of SARS-CoV-2 PLpro
support the claim that PLpro is a … structure of PLpro C111S in complex with the potent inhibitor

[HTML][HTML] SARS-CoV-2: the many pros of targeting PLpro

CB McClain, N Vabret - Signal Transduction and Targeted Therapy, 2020 - nature.com
… sheds light on SARS-CoV2 PLpro and its role in the pathogenesis of COVID-19 by characterizing
its deISGylation activity. It suggests that inhibition of PLpro would not only inhibits viral …

Activity profiling and structures of inhibitor-bound SARS-CoV-2-PLpro protease provides a framework for anti-COVID-19 drug design

W Rut, Z Lv, M Zmudzinski, S Patchett, D Nayak… - biorxiv, 2020 - biorxiv.org
… and irreversible inhibitors with a high degree of selectivity for SARS PLpro variants versus
… of these inhibitors (VIR250 and VIR251) in complex with SARS-CoV-2-PLpro which reveals …