Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.21.98 extracted from

  • El-Sayed, S.M.; Ali, M.A.M.; El-Gendy, B.E.M.; Dandash, S.S.; Issac, Y.; Saad, R.; Azab, M.M.; Mohamed, M.R.
    Identification of novel small molecule inhibitors against the NS3/4A protease of hepatitis C virus genotype 4a (2018), Curr. Pharm. Des., 24, 4484-4491 .
    View publication on PubMed
Search for more literature for 3.4.21.98

Application

Application Comment Organism
drug development NS3/4A is a target for development of direct-acting antiviral agents (DAAs) targeting key viral enzymes essential for viral replication represents a significant milestone in the treatment of chronic HCV infection Hepatitis C virus genotype 4a

Cloned(Commentary)

Cloned (Comment) Organism
cloning from clinical isolate genotype 4a and recombinant expression of GST-tagged enzyme in Escherichia coli TOP cells Hepatitis C virus genotype 4a

Inhibitors

Inhibitors Comment Organism Structure
2-[[(2,3-dimethylphenoxy)acetyl]amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carboxamide an inhibitor identified due to its activity against genotype 4d Hepatitis C virus genotype 4a
6-(2-ethoxyphenyl)-3-(2-methylfuran-3-yl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole an inhibitor identified due to its activity against genotype 4d Hepatitis C virus genotype 4a
additional information N-(3-cyano-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)-2-phenoxyacetamide and N-(3-cyano-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)-2-(naphthalen-2-yloxy)acetamide are not inhibitory. The inhibitory efficacy of four computer-designed and chemically-synthesized small-molecule compounds is evaluated against in vitro-expressed NS3/4A protease from HCV genotype 4a, the most prevalent genotype in Egypt, using a fluorescence-based enzymatic assay, overview. Molecular modeling. No inhibition by N-(3-cyano-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)-2-phenoxyacetamide (BE115) and N-(3-cyano-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)-2-(naphthalen-2-yloxy)acetamide (BR116) Hepatitis C virus genotype 4a
N-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thien-2-yl)-2-(naphthalen-2-yloxy)acetamide i.e. BE114 Hepatitis C virus genotype 4a
N-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thien-2-yl)-2-phenoxyacetamide i.e. BE113 Hepatitis C virus genotype 4a

Organism

Organism UniProt Comment Textmining
Hepatitis C virus genotype 4a O39929 HCV, isolate ED43
-

Purification (Commentary)

Purification (Comment) Organism
recombinant GST-tagged enzyme from Escherichia coli TOP cells by glutathione affinity chromatography Hepatitis C virus genotype 4a

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ac-Asp-Glu-Asp(5-((2-aminoethyl)amino)naphthalene-1-sulfonic acid)-Glu-Glu-aminobutyryl-Psi-[COO]Ala-Ser-Lys-(4-(dimethylaminoazo)benzene-4-carboxylic acid)-NH2 + H2O
-
 Hepatitis C virus genotype 4a ?
-
 ?

Synonyms

Synonyms Comment Organism
NS3/4A protease
-
 Hepatitis C virus genotype 4a

General Information

General Information Comment Organism
evolution NS3/4A protease from HCV genotype 4a is the most prevalent genotype in Egypt Hepatitis C virus genotype 4a