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Literature summary for 3.4.22.B80 extracted from

  • Freitas, B.T.; Durie, I.A.; Murray, J.; Longo, J.E.; Miller, H.C.; Crich, D.; Hogan, R.J.; Tripp, R.A.; Pegan, S.D.
    Characterization and noncovalent inhibition of the deubiquitinase and deISGylase activity of SARS-CoV-2 papain-like protease (2020), ACS Infect. Dis., 6, 2099-2109 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.22.B80

Application

Application Comment Organism
drug development naphthalene PLpro inhibitors designed for SARS-CoV can inhibit SARSCoV-2 PLpro as well as impede SARS-CoV-2 replication Severe acute respiratory syndrome coronavirus 2

Cloned(Commentary)

Cloned (Comment) Organism
transformed into T7 and expressed in Escherrichia coli Severe acute respiratory syndrome coronavirus 2

Inhibitors

Inhibitors Comment Organism Structure
2-methyl-N-[1-(2-naphthyl)ethyl]-benzamide
-
 Severe acute respiratory syndrome coronavirus 2
5-(acetylamino)-2-methyl-N-[(1R)-1-(1-naphthanlenyl)ethyl]-benzamide
-
 Severe acute respiratory syndrome coronavirus 2
5-amino-2-methyl-N-[(R)-1-(1-naphthyl)ethyl]benzamide
-
 Severe acute respiratory syndrome coronavirus 2
additional information naphthalene PLpro inhibitors designed for SARS-CoV can inhibit SARSCoV-2 PLpro as well as impede SARS-CoV-2 replication Severe acute respiratory syndrome coronavirus 2
N-(4-methoxybenzyl)-1-(1-naphthylmethyl)-4-piperidinecarboxamide
-
 Severe acute respiratory syndrome coronavirus 2

Organism

Organism UniProt Comment Textmining
Severe acute respiratory syndrome coronavirus 2 MN908947.3 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.
additional information the papain-like protease is likely responsible for cleavage of the coronavirus viral polypeptide. The protease from SARS-CoV-2 has a marked reduction in its ability to process K48 linked ubiquitin substrates compared to its counterpart in SARS-CoV. Its substrate activity more closely mirrors that of the PLpro from the Middle East respiratory syndrome coronavirus and prefers interferon-stimulated gene products (ISG15s) from certain species including humans Severe acute respiratory syndrome coronavirus 2 ?
-
-
RLRGG 7-amido-4-methylcoumarin + H2O
-
 Severe acute respiratory syndrome coronavirus 2 RLRGG + 7-amino-4-methylcoumarin
-
 ?
[interferon-stimulated gene product 15] 7-amido-4-methylcoumarin + H2O
-
 Severe acute respiratory syndrome coronavirus 2 ?
-
 ?
[ubiquitin] 7-amido-4-methylcoumarin + H2O
-
 Severe acute respiratory syndrome coronavirus 2 ?
-
 ?

Synonyms

Synonyms Comment Organism
SARS-CoV-2 papain-like protease
-
 Severe acute respiratory syndrome coronavirus 2
SARS-CoV-2 PLpro orf1ab 1564-1876 Severe acute respiratory syndrome coronavirus 2

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0024
-
 pH 7.4, 37°C Severe acute respiratory syndrome coronavirus 2 5-amino-2-methyl-N-[(R)-1-(1-naphthyl)ethyl]benzamide
0.005
-
 pH 7.4, 37°C Severe acute respiratory syndrome coronavirus 2 5-(acetylamino)-2-methyl-N-[(1R)-1-(1-naphthanlenyl)ethyl]-benzamide
0.0235
-
 pH 7.4, 37°C Severe acute respiratory syndrome coronavirus 2 2-methyl-N-[1-(2-naphthyl)ethyl]-benzamide
0.1007
-
 pH 7.4, 37°C Severe acute respiratory syndrome coronavirus 2 N-(4-methoxybenzyl)-1-(1-naphthylmethyl)-4-piperidinecarboxamide

General Information

General Information Comment Organism
metabolism the papain-like protease is likely responsible for cleavage of the coronavirus viral polypeptide. It is also responsible for suppression of host innate immune responses by virtue of its ability to reverse host ubiquitination and ISGylation events Severe acute respiratory syndrome coronavirus 2