Literature summary for 3.4.23.47 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.

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Application

Application	Comment	Organism
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)

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

Inhibitors

Inhibitors	Comment	Organism	Structure
(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
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
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
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
Ro31-8959	-	Human immunodeficiency virus 2
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
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]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.025	-	Lys-Ala-Arg-Ile-Nle-Nph-Glu-Ala-Nle-NH2	pH 4.7, 37°C	Human immunodeficiency virus 2
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]

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism	UniProt	Comment	Textmining
Human immunodeficiency virus 2	-	human immunodeficiency virus type 2	-

Purification (Commentary)

Purification (Comment)	Organism
recombinant enzyme	Human immunodeficiency virus 2

Storage Stability

Storage Stability	Organism
-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)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
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	-	?
GAG precursor protein of HIV-2 + H2O	-	Human immunodeficiency virus 2	?	-	?
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

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

Turnover Number [1/s]

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

pH Optimum

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

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
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
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
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
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

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Release 2023.1 (January 2023)