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Literature summary for 3.4.22.B80 extracted from

  • Ratia, K.; Pegan, S.; Takayama, J.; Sleeman, K.; Coughlin, M.; Baliji, S.; Chaudhuri, R.; Fu, W.; Prabhakar, B.S.; Johnson, M.E.; Baker, S.C.; Ghosh, A.K.; Mesecar, A.D.
    A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replication (2008), Proc. Natl. Acad. Sci. USA, 105, 16119-16124.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.22.B80

Cloned(Commentary)

Cloned (Comment) Organism
expression of polyprotein residues 1541-1855 severe acute respiratory syndrome coronavirus

Crystallization (Commentary)

Crystallization (Comment) Organism
structure of PLpro in complex with GRL0617, the inhibitor binds within the S4-S3 subsites of the enzyme and induces a loop closure that shuts down catalysis at the active site severe acute respiratory syndrome coronavirus

Inhibitors

Inhibitors Comment Organism Structure
2-chloro-N-[(1R)-1-(naphthalen-2-yl)ethyl]benzamide
-
 severe acute respiratory syndrome coronavirus
2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]-5-nitrobenzamide
-
 severe acute respiratory syndrome coronavirus
2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide
-
 severe acute respiratory syndrome coronavirus
2-methyl-N-[(1R)-1-(naphthalen-2-yl)ethyl]benzamide
-
 severe acute respiratory syndrome coronavirus
5-acetamido-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide
-
 severe acute respiratory syndrome coronavirus
GRL0617 inhibits SARS-CoV viral replication in Vero E6 cells with an EC50 of 15 micoM and has no associated cytotoxicity severe acute respiratory syndrome coronavirus

Organism

Organism UniProt Comment Textmining
severe acute respiratory syndrome coronavirus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Arg-Leu-Arg-Gly-Gly-AMC +
-
 severe acute respiratory syndrome coronavirus Arg-Leu-Arg-Gly-Gly + 7-amino-4-methylcoumarin
-
 H2O

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0006
-
 pH not specified in the publication, temperature not specified in the publication severe acute respiratory syndrome coronavirus GRL0617
0.0023
-
 pH not specified in the publication, temperature not specified in the publication severe acute respiratory syndrome coronavirus 2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide
0.0026
-
 pH not specified in the publication, temperature not specified in the publication severe acute respiratory syndrome coronavirus 5-acetamido-2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]benzamide
0.0073
-
 pH not specified in the publication, temperature not specified in the publication severe acute respiratory syndrome coronavirus 2-methyl-N-[(1R)-1-(naphthalen-1-yl)ethyl]-5-nitrobenzamide
0.0087
-
 pH not specified in the publication, temperature not specified in the publication severe acute respiratory syndrome coronavirus 2-methyl-N-[(1R)-1-(naphthalen-2-yl)ethyl]benzamide
0.0145
-
 pH not specified in the publication, temperature not specified in the publication severe acute respiratory syndrome coronavirus 2-chloro-N-[(1R)-1-(naphthalen-2-yl)ethyl]benzamide