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Literature summary for 3.4.22.69 extracted from

  • Jo, S.; Kim, S.; Shin, D.H.; Kim, M.S.
    Inhibition of SARS-CoV 3CL protease by flavonoids (2020), J. Enzyme Inhib. Med. Chem., 35, 145-151 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.22.69

Cloned(Commentary)

Cloned (Comment) Organism
the catalytic domain of 3CLpro is synthesised chemically and cloned into a bacteriophage T7-based expression vector, pBT7. The plasmid DNA is transformed into Escherichia coli BL21 (DE3) for protein expression Severe acute respiratory syndrome-related coronavirus

Inhibitors

Inhibitors Comment Organism Structure
3,4',5,7,8-pentahydroxyflavone i.e. herbacetin, efficiently blocks the enzymatic activity, suggested to be a template to design functionally improved inhibitors Severe acute respiratory syndrome-related coronavirus
5,7-dihydroxy 4',6-dimethoxyflavone 7-rutinoside i.e. pectolinarin, efficiently blocks the enzymatic activity, suggested to be a template to design functionally improved inhibitors Severe acute respiratory syndrome-related coronavirus
apigenin-7-O-rhamnoglucoside i.e. rhoifolin, efficiently blocks the enzymatic activity, suggested to be a template to design functionally improved inhibitors Severe acute respiratory syndrome-related coronavirus

Organism

Organism UniProt Comment Textmining
Severe acute respiratory syndrome-related coronavirus P0C6X7 human, i.e. SARS-CoV
-

Purification (Commentary)

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Dabcyl-KTSAVLQSGFRKME-EDANS + H2O
-
 Severe acute respiratory syndrome-related coronavirus Dabcyl-KTSAVLQ + SGFRKME-EDANS
-
 ?

Synonyms

Synonyms Comment Organism
SARS-CoV 3CL protease
-
 Severe acute respiratory syndrome-related coronavirus
SARS-CoV nsp5-pp1a/pp1ab 3CL protease
-
 Severe acute respiratory syndrome-related coronavirus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.03317
-
 pH 6.5, 37°C Severe acute respiratory syndrome-related coronavirus 3,4',5,7,8-pentahydroxyflavone
0.03745
-
 pH 6.5, 37°C Severe acute respiratory syndrome-related coronavirus apigenin-7-O-rhamnoglucoside
0.03778
-
 pH 6.5, 37°C Severe acute respiratory syndrome-related coronavirus 5,7-dihydroxy 4',6-dimethoxyflavone 7-rutinoside