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ChemicalBook >> journal list >> Journal of Enzyme Inhibition and Medicinal Chemistry >>article
Journal of Enzyme Inhibition and Medicinal Chemistry

Journal of Enzyme Inhibition and Medicinal Chemistry

IF: 5.6
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In-cell bioluminescence resonance energy transfer (BRET)-based assay uncovers ceritinib and CA-074 as SARS-CoV-2 papain-like protease inhibitors

Published:1 December 2024 DOI: 10.1080/14756366.2024.2387417 PMID: 39163165
Mei Li,?Zhu-Chun Bei,?Yongtian Yuan,?Baogang Wang,?Dongna Zhang,?Likun Xu,?Liangliang Zhao,?Qin Xu,?Yabin Song

Abstract

Papain-like protease (PLpro) is an attractive anti-coronavirus target. The development of PLpro inhibitors, however, is hampered by the limitations of the existing PLpro assay and the scarcity of validated active compounds. We developed a novel in-cell PLpro assay based on BRET and used it to evaluate and discover SARS-CoV-2 PLpro inhibitors. The developed assay demonstrated remarkable sensitivity for detecting the reduction of intracellular PLpro activity while presenting high reliability and performance for inhibitor evaluation and high-throughput screening. Using this assay, three protease inhibitors were identified as novel PLpro inhibitors that are structurally disparate from those previously known. Subsequent enzymatic assays and ligand-protein interaction analysis based on molecular docking revealed that ceritinib directly inhibited PLpro, showing high geometric complementarity with the substrate-binding pocket in PLpro, whereas CA-074 methyl ester underwent intracellular hydrolysis, exposing a free carboxyhydroxyl group essential for hydrogen bonding with G266 in the BL2 groove, resulting in PLpro inhibition.

Substances (30)

Materials
Procduct Name CAS Molecular Formula Supplier Price
Disulfiram 97-77-8 C10H20N2S4 578 suppliers $13.44-$1504.50
Disulfiram 97-77-8 C10H20N2S4 578 suppliers $13.44-$1504.50
Disulfiram 97-77-8 C10H20N2S4 578 suppliers $13.44-$1504.50
Disulfiram 97-77-8 C10H20N2S4 578 suppliers $13.44-$1504.50
Ceritinib (LDK378) 1032900-25-6 C28H36ClN5O3S 448 suppliers $8.00-$3600.00
Ceritinib (LDK378) 1032900-25-6 C28H36ClN5O3S 448 suppliers $8.00-$3600.00
Ceritinib (LDK378) 1032900-25-6 C28H36ClN5O3S 448 suppliers $8.00-$3600.00
Ceritinib (LDK378) 1032900-25-6 C28H36ClN5O3S 448 suppliers $8.00-$3600.00
6-Thioguanine 154-42-7 C5H5N5S 406 suppliers $5.00-$4405.00
6-Thioguanine 154-42-7 C5H5N5S 406 suppliers $5.00-$4405.00

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