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Literature summary extracted from

  • Griffiths, J.T.; Tomchak, L.A.; Mills, J.S.; Graves, M.C.; Cook, N.D.; Dunn, B.M.; Kay, J.
    Interactions of substrates and inhibitors with a family of tethered HIV-1 and HIV-2 homo- and heterodimeric proteinases (1994), J. Biol. Chem., 269, 4787-4793.
    View publication on PubMed

Application

EC Number Application Comment Organism
3.4.23.47 medicine potential target for chemotherapy of virus infection and associated diseases, essential for maturation of infectious virions, development of drugs against the protease should be effective against HIV-2 Human immunodeficiency virus 2

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.23.47 genes constructed encode HIV-2 homodimeric and heterodimeric proteinases, expression in Escherichia coli K-12 strain MC1061 Human immunodeficiency virus 2

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.23.47 (2R,4S,5S)-6-cyclohexyl-5-(3,3-dimethylbutanamido)-4-hydroxy-2-isopropyl-N-((2S,3R)-3-methyl-1-oxo-1-(phenethylamino)pentan-2-yl)hexanamide synthetic inhibitor 4 Human immunodeficiency virus 2
3.4.23.47 benzyl (S)-1-((2S,3R)-4-((R)-4-(tert-butylcarbamoyl)thiazolidin-3-yl)-3-hydroxy-1-phenylbutan-2-ylamino)-4-amino-1,4-dioxobutan-2-ylcarbamate synthetic inhibitor 1 Human immunodeficiency virus 2
3.4.23.47 benzyl (S)-1-((2S,3R)-4-((S) -2-(tert-butylcarbamoyl)indolin-1-yl)-3-hydroxy-1-phenylbutan-2-ylamino)-4-amino-1,4-dioxobutan-2-ylcarbamate synthetic inhibitor 2 Human immunodeficiency virus 2
3.4.23.47 N-((S)-1-((2S,3R)-4-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)-octahydroisoquinolin-2(1H)-yl)-3-hydroxy-1-phenylbutan-2-ylamino)-4-amino-1,4-dioxobutan-2-yl)quinoline-3-carboxamide synthetic inhibitor 3 Human immunodeficiency virus 2
3.4.23.47 Ro31-8959
-
 Human immunodeficiency virus 2
3.4.23.47 tert-butyl (2S,3S)-5-(((2S,3R)-3-methyl-1-oxo-1-(phenethylamino)pentan-2-yl)carbamoyl)-1-cyclohexyl-3-hydroxy-6-methylheptan-2-ylcarbamate synthetic inhibitor 6 Human immunodeficiency virus 2
3.4.23.47 tert-butyl (2S,3S,5R)-5-(((2S,3R)-3-methyl-1-oxo-1-(phenethylamino)pentan-2-yl)carbamoyl)-1-cyclohexyl-3-hydroxy-6-methylheptan-2-ylcarbamate synthetic inhibitor 5 Human immunodeficiency virus 2

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.23.47 0.025
-
 Lys-Ala-Arg-Ile-Nle-Nph-Glu-Ala-Nle-NH2 pH 4.7, 37°C Human immunodeficiency virus 2
3.4.23.47 0.36
-
 Ac-Tyr-Arg-Ala-Arg-Val-Phe Nph-Val-Arg-Ala-Ala-Lys pH 4.7, 37°C Human immunodeficiency virus 2

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
3.4.23.47 22000
-
 2 * 22000, Western blotting Human immunodeficiency virus 2

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.4.23.47 GAG precursor protein of HIV-2 + H2O Human immunodeficiency virus 2
-
 ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.4.23.47 Human immunodeficiency virus 2
-
 human immunodeficiency virus type 2
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.23.47 recombinant enzyme Human immunodeficiency virus 2

Storage Stability

EC Number Storage Stability Organism
3.4.23.47 -80°C, stored in 10 mM potassium phosphate, pH 7.5, containing 125 mM KCl and 0.0125% Tween 20 Human immunodeficiency virus 2

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.23.47 Ac-Tyr-Arg-Ala-Arg-Val-Phe Nph-Val-Arg-Ala-Ala-Lys + H2O chromogenic substrate Human immunodeficiency virus 2 Ac-Tyr-Arg-Ala-Arg-Val-Phe + Nph-Va-Arg-Ala-Ala-Lys
-
 ?
3.4.23.47 GAG precursor protein of HIV-2 + H2O
-
 Human immunodeficiency virus 2 ?
-
 ?
3.4.23.47 Lys-Ala-Arg-Ile-Nle-Nph-Glu-Ala-Nle-NH2 + H2O chromogenic substrate Human immunodeficiency virus 2 Lys-Ala-Arg-Ile-Nle + Nph-Glu-Ala-Nle-NH2
-
 ?

Subunits

EC Number Subunits Comment Organism
3.4.23.47 dimer 2 * 22000, Western blotting Human immunodeficiency virus 2

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.4.23.47 0.00167
-
 Ac-Tyr-Arg-Ala-Arg-Val-Phe Nph-Val-Arg-Ala-Ala-Lys pH 4.7, 37°C Human immunodeficiency virus 2
3.4.23.47 0.00722
-
 Lys-Ala-Arg-Ile-Nle-Nph-Glu-Ala-Nle-NH2 pH 4.7, 37°C Human immunodeficiency virus 2

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.23.47 4.7
-
-
 Human immunodeficiency virus 2

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.23.47 0.0002
-
 N-((S)-1-((2S,3R)-4-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)-octahydroisoquinolin-2(1H)-yl)-3-hydroxy-1-phenylbutan-2-ylamino)-4-amino-1,4-dioxobutan-2-yl)quinoline-3-carboxamide pH 4.7, 37°C, synthetic inhibitor 3 Human immunodeficiency virus 2
3.4.23.47 0.0002
-
 benzyl (S)-1-((2S,3R)-4-((R)-4-(tert-butylcarbamoyl)thiazolidin-3-yl)-3-hydroxy-1-phenylbutan-2-ylamino)-4-amino-1,4-dioxobutan-2-ylcarbamate pH 4.7, 37°C, synthetic inhibitor 1 Human immunodeficiency virus 2
3.4.23.47 0.0004
-
 tert-butyl (2S,3S,5R)-5-(((2S,3R)-3-methyl-1-oxo-1-(phenethylamino)pentan-2-yl)carbamoyl)-1-cyclohexyl-3-hydroxy-6-methylheptan-2-ylcarbamate pH 4.7, 37°C, synthetic inhibitor 5 Human immunodeficiency virus 2
3.4.23.47 0.0007
-
 (2R,4S,5S)-6-cyclohexyl-5-(3,3-dimethylbutanamido)-4-hydroxy-2-isopropyl-N-((2S,3R)-3-methyl-1-oxo-1-(phenethylamino)pentan-2-yl)hexanamide pH 4.7, 37°C, synthetic inhibitor 4 Human immunodeficiency virus 2