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Literature summary for 3.4.22.B80 extracted from

  • Arya, R.; Prashar, V.; Kumar, M.
    Evaluating stability and activity of SARS-CoV-2 PLpro for high-throughput screening of inhibitors (2022), Mol. Biotechnol., 64, 1-8 .
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
EDTA enhances activity, best activity at 0.5 mM EDTA Severe acute respiratory syndrome coronavirus 2

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli BL21 (DE3) Severe acute respiratory syndrome coronavirus 2

General Stability

General Stability Organism
for long-term storage, 5 mM DTT is useful to prevent protein aggregation Severe acute respiratory syndrome coronavirus 2

Inhibitors

Inhibitors Comment Organism Structure
DMSO activity gradually decreased above 1.0% DMSO Severe acute respiratory syndrome coronavirus 2

Organism

Organism UniProt Comment Textmining
Severe acute respiratory syndrome coronavirus 2 P0DTD1 SARS-CoV-2 PLpro corresponds to amino acids sequence 746-1064 of NSP3; SARS-CoV-2
-

Purification (Commentary)

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

Renatured (Commentary)

Renatured (Comment) Organism
the enzyme regains catalytic activity when incubated at pHs 8.0 and pH 8.5. Incubation at pH-values below 5.5 completely abolishes the catalytic activity, suggesting an irreversible inactivation of the enzyme. An irreversible loss of catalytic activity is observed at pH 9.0 and above Severe acute respiratory syndrome coronavirus 2

Storage Stability

Storage Stability Organism
best stability for long-term storage in a buffer containing 50 mM HEPES pH 7.5, 100 mM NaCl, and 5 mM DTT Severe acute respiratory syndrome coronavirus 2

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-LRGG-7-amido-4-methylcoumarin + H2O
-
Severe acute respiratory syndrome coronavirus 2 benzyloxycarbonyl-LRGG + 7-amino-4-methylcoumarin
-
?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
maximum Kcat/Km at 30°C Severe acute respiratory syndrome coronavirus 2

Temperature Range [°C]

Temperature Minimum [°C] Temperature Maximum [°C] Comment Organism
25 37 25°C: about 75% of maximal activity, 37°C: about 75% of maximal activity Severe acute respiratory syndrome coronavirus 2

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6.5
-
-
Severe acute respiratory syndrome coronavirus 2

pH Range

pH Minimum pH Maximum Comment Organism
5.5 8 pH 5.5: about 55% of maximal activity, pH 8.0: about 50% of maximal activity Severe acute respiratory syndrome coronavirus 2

General Information

General Information Comment Organism
drug target because of the essential roles of SARS-CoV-2 papain-like protease (PLpro) in the viral polyprotein processing and suppression of host immune responses, it is a crucial target for drug discovery against COVID-19 Severe acute respiratory syndrome coronavirus 2
physiological function essential roles of SARS-CoV-2 papain-like protease (PLpro) in the viral polyprotein processing and suppression of host immune responses Severe acute respiratory syndrome coronavirus 2