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Literature summary for 3.4.22.B80 extracted from

  • Zhao, Y.; Du, X.; Duan, Y.; Pan, X.; Sun, Y.; You, T.; Han, L.; Jin, Z.; Shang, W.; Yu, J.; Guo, H.; Liu, Q.; Wu, Y.; Peng, C.; Wang, J.; Zhu, C.; Yang, X.; Yang, K.; Lei, Y.; Guddat, L.W.; Xu, W.; Xiao, G.; Sun, L.; Zhang, L.; Rao, Z.; Yang, H.
    High-throughput screening identifies established drugs as SARS-CoV-2 PLpro inhibitors (2021), Protein Cell, 12, 877-888 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.22.B80

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Rosetta (DE3) Severe acute respiratory syndrome coronavirus 2

Crystallization (Commentary)

Crystallization (Comment) Organism
sitting-drop vapor-diffusion method at 18°C, crystal structures of the enzyme and its complex with YM155 at 2.1 A resolution Severe acute respiratory syndrome coronavirus 2

Inhibitors

Inhibitors Comment Organism Structure
cryptotanshinone exhibits strong antiviral activities in cell-based assays Severe acute respiratory syndrome coronavirus 2
GRL0617 exhibits strong antiviral activities in cell-based assays Severe acute respiratory syndrome coronavirus 2
additional information over 6000 compounds are screened that included approved drugs, drug candidates in clinical trials, and pharmacologically active compounds to identify leads that target the SARS-CoV-2 papain-like protease (PLpro) Severe acute respiratory syndrome coronavirus 2
tanshinone exhibits strong antiviral activities in cell-based assays Severe acute respiratory syndrome coronavirus 2
YM155 exhibits strong antiviral activities in cell-based assays. YM155 simultaneously targets three hotspots on PLpro, including the substrate-binding pocket, the interferon stimulating gene product 15 (ISG15) binding site and zinc finger motif Severe acute respiratory syndrome coronavirus 2

Organism

Organism UniProt Comment Textmining
Severe acute respiratory syndrome coronavirus 2 P0DTD1 full-length gene encoding SARS-CoV-2 PLpro (residues 1564-1878 of the SARS-CoV-2 polyprotein); SARS-CoV-2
-

Purification (Commentary)

Purification (Comment) Organism
-
 Severe acute respiratory syndrome coronavirus 2

Synonyms

Synonyms Comment Organism
PLpro
-
 Severe acute respiratory syndrome coronavirus 2
SARS-CoV-2 papain-like protease
-
 Severe acute respiratory syndrome coronavirus 2

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00139
-
 pH 7.5, temperature not specified in the publication, without Triton X-100 Severe acute respiratory syndrome coronavirus 2 GRL0617
0.00153
-
 pH 7.5, temperature not specified in the publication, 0.01% (v/v) Triton X-100 Severe acute respiratory syndrome coronavirus 2 tanshinone
0.00166
-
 pH 7.5, temperature not specified in the publication, 0.01% (v/v) Triton X-100 Severe acute respiratory syndrome coronavirus 2 GRL0617
0.00183
-
 pH 7.5, temperature not specified in the publication, 0.01% (v/v) Triton X-100 Severe acute respiratory syndrome coronavirus 2 YM155
0.00221
-
 pH 7.5, temperature not specified in the publication, without Triton X-100 Severe acute respiratory syndrome coronavirus 2 tanshinone
0.00247
-
 pH 7.5, temperature not specified in the publication, without Triton X-100 Severe acute respiratory syndrome coronavirus 2 YM155
0.00563
-
 pH 7.5, temperature not specified in the publication, without Triton X-100 Severe acute respiratory syndrome coronavirus 2 cryptotanshinone
0.00599
-
 pH 7.5, temperature not specified in the publication, 0.01% (v/v) Triton X-100 Severe acute respiratory syndrome coronavirus 2 cryptotanshinone