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Literature summary for 3.4.22.B80 extracted from

  • Xu, Y.; Chen, K.; Pan, J.; Lei, Y.; Zhang, D.; Fang, L.; Tang, J.; Chen, X.; Ma, Y.; Zheng, Y.; Zhang, B.; Zhou, Y.; Zhan, J.; Xu, W.
    Repurposing clinically approved drugs for COVID-19 treatment targeting SARS-CoV-2 papain-like protease (2021), Int. J. Biol. Macromol., 188, 137-146 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.22.B80

Cloned(Commentary)

Cloned (Comment) Organism
PLpro and PLpro-C111S are expressede as His-tagged enzymes in Escherichia coli BL21(DE3) Severe acute respiratory syndrome coronavirus 2

Protein Variants

Protein Variants Comment Organism
C111S Tm-value of PLpro-C111S (47°C) is 2°C higher than that of PLpro (45°C) Severe acute respiratory syndrome coronavirus 2

Inhibitors

Inhibitors Comment Organism Structure
chloroxine directly interact with the enzyme Severe acute respiratory syndrome coronavirus 2
tanshinone IIA sulfonate sodium directly interact with the enzyme Severe acute respiratory syndrome coronavirus 2

Organism

Organism UniProt Comment Textmining
Severe acute respiratory syndrome coronavirus 2 P0DTD1 SARS-CoV-2
-

Purification (Commentary)

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ALKGG-7-amido-4-methylcoumarin +
-
 Severe acute respiratory syndrome coronavirus 2 ALKGG + 7-amino-4-methylcoumarin
-
 ?

Synonyms

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

Temperature Stability [°C]

Temperature Stability Minimum [°C] Temperature Stability Maximum [°C] Comment Organism
45
-
 Tm-value of PLpro, mixing PLpro with chloroxine increases Tm-value by 2.5°C Severe acute respiratory syndrome coronavirus 2
47
-
 Tm-value of PLpro-C111S Severe acute respiratory syndrome coronavirus 2

pH Stability

pH Stability pH Stability Maximum Comment Organism
7
-
 PLpro-C111S and PLpro-C111S/chloroxine exhibit the highest stability at pH 7.0 Severe acute respiratory syndrome coronavirus 2

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00165
-
 pH 7.5, 25°C, directly interact with the enzyme Severe acute respiratory syndrome coronavirus 2 tanshinone IIA sulfonate sodium
0.00724
-
 pH 7.5, 25°C, directly interact with the enzyme Severe acute respiratory syndrome coronavirus 2 chloroxine

General Information

General Information Comment Organism
drug target the enzyme is an attractive drug target because it has multiple essential functions involved in processing viral proteins, including viral genome replication and removal of post-translational ubiquitination modifications Severe acute respiratory syndrome coronavirus 2
physiological function the enzyme has multiple essential functions involved in processing viral proteins, including viral genome replication and removal of post-translational ubiquitination modifications Severe acute respiratory syndrome coronavirus 2