BRENDA - Enzyme Database show
show all sequences of 3.4.23.16

Critical differences in HIV-1 and HIV-2 protease specificity for clinical inhibitors

Tie, Y.; Wang, Y.F.; Boross, P.I.; Chiu, T.Y.; Ghosh, A.K.; Tozser, J.; Louis, J.M.; Harrison, R.W.; Weber, I.T.; Protein Sci. 21, 339-350 (2012)

Data extracted from this reference:

Cloned(Commentary)
Commentary
Organism
mutant enzyme V32I/I47V/V82I is expressed in Escherichia coli BL21(DE3) cells
Human immunodeficiency virus 1
Crystallization (Commentary)
Crystallization
Organism
mutant enzyme V32I/I47V/V82I in complex with inhibitors darunavir, amprenavir or saquinavir, hanging drop vapor diffusion method, using 0.1 M sodium acetate buffer, pH 4.6 and 2 M NaCl as precipitant (darunavir), 1.5 M NaCl with 0.6 M imidazole/0.12 M zinc acetate buffer at pH 6 (amprenavir), or 0.1 M sodium acetate buffer, pH 5.0, 0.4 M potassium chloride as precipitant (saquinavir)
Human immunodeficiency virus 1
Engineering
Amino acid exchange
Commentary
Organism
Q7K/L33I/L63I/C67A/C95A
the mutations diminish the autoproteolysis and prevent cysteine-thiol oxidation of the HIV-1 protease
Human immunodeficiency virus 1
V32I/I47V/V82I
the mutations mimic the inhibitor binding site of HIV-2 protease and shows increased kcat values compared to the wild type enzyme
Human immunodeficiency virus 1
Inhibitors
Inhibitors
Commentary
Organism
Structure
amprenavir
less effective on HIV-2 protease than on HIV-1 protease
Human immunodeficiency virus 1
darunavir
-
Human immunodeficiency virus 1
saquinavir
-
Human immunodeficiency virus 1
KM Value [mM]
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
0.07
-
IPFAAAQQRK
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.09
-
KARLMAEALK
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.12
-
VSQLYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.13
-
KARLMAEALK
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.19
-
VVQNYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.23
-
VVQNYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.24
-
VSQVYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.28
-
IPFAAAQQRK
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.32
-
VLQNYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.35
-
VSQVYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.38
-
VSQLYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.4
-
VLQNYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
Natural Substrates/ Products (Substrates)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
Gag polyprotein + H2O
Human immunodeficiency virus 1
-
?
-
-
?
Gag-Pol polyprotein + H2O
Human immunodeficiency virus 1
-
?
-
-
?
Organism
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
Human immunodeficiency virus 1
Q7SSE3
-
-
Substrates and Products (Substrate)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
Gag polyprotein + H2O
-
718370
Human immunodeficiency virus 1
?
-
-
-
?
Gag-Pol polyprotein + H2O
-
718370
Human immunodeficiency virus 1
?
-
-
-
?
IPFAAAQQRK + H2O
the protein contains a HIV-2 cleavage site
718370
Human immunodeficiency virus 1
IPFAA + AQQRK
-
-
-
?
KARLMAEALK + H2O
the protein contains a HIV-2 cleavage site
718370
Human immunodeficiency virus 1
KARLM + AEALK
-
-
-
?
VLQNYPIVQ + H2O
the protein contains a HIV-1 cleavage site
718370
Human immunodeficiency virus 1
VLQNY + PIVQ
-
-
-
?
VSQLYPIVQ + H2O
the protein contains a HIV-1 cleavage site
718370
Human immunodeficiency virus 1
VSQLY + PIVQ
-
-
-
?
VSQVYPIVQ + H2O
the protein contains a HIV-1 cleavage site
718370
Human immunodeficiency virus 1
VSQVY + PIVQ
-
-
-
?
VVQNYPIVQ + H2O
the protein contains a HIV-1 cleavage site
718370
Human immunodeficiency virus 1
VVQNY + PIVQ
-
-
-
?
Turnover Number [1/s]
Turnover Number Minimum [1/s]
Turnover Number Maximum [1/s]
Substrate
Commentary
Organism
Structure
0.06
-
VLQNYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.16
-
VVQNYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.18
-
VVQNYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.26
-
VLQNYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.3
-
IPFAAAQQRK
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.3
-
KARLMAEALK
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.4
-
VSQLYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.6
-
KARLMAEALK
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
1.2
-
IPFAAAQQRK
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
2.6
-
VSQVYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
3
-
VSQVYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
5.1
-
VSQLYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
Ki Value [mM]
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
0.00000004
-
darunavir
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C; wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.00000007
-
saquinavir
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.00000011
-
saquinavir
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.00000017
-
amprenavir
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.00000324
-
amprenavir
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
Cloned(Commentary) (protein specific)
Commentary
Organism
mutant enzyme V32I/I47V/V82I is expressed in Escherichia coli BL21(DE3) cells
Human immunodeficiency virus 1
Crystallization (Commentary) (protein specific)
Crystallization
Organism
mutant enzyme V32I/I47V/V82I in complex with inhibitors darunavir, amprenavir or saquinavir, hanging drop vapor diffusion method, using 0.1 M sodium acetate buffer, pH 4.6 and 2 M NaCl as precipitant (darunavir), 1.5 M NaCl with 0.6 M imidazole/0.12 M zinc acetate buffer at pH 6 (amprenavir), or 0.1 M sodium acetate buffer, pH 5.0, 0.4 M potassium chloride as precipitant (saquinavir)
Human immunodeficiency virus 1
Engineering (protein specific)
Amino acid exchange
Commentary
Organism
Q7K/L33I/L63I/C67A/C95A
the mutations diminish the autoproteolysis and prevent cysteine-thiol oxidation of the HIV-1 protease
Human immunodeficiency virus 1
V32I/I47V/V82I
the mutations mimic the inhibitor binding site of HIV-2 protease and shows increased kcat values compared to the wild type enzyme
Human immunodeficiency virus 1
Inhibitors (protein specific)
Inhibitors
Commentary
Organism
Structure
amprenavir
less effective on HIV-2 protease than on HIV-1 protease
Human immunodeficiency virus 1
darunavir
-
Human immunodeficiency virus 1
saquinavir
-
Human immunodeficiency virus 1
Ki Value [mM] (protein specific)
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
0.00000004
-
darunavir
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C; wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.00000007
-
saquinavir
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.00000011
-
saquinavir
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.00000017
-
amprenavir
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.00000324
-
amprenavir
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
KM Value [mM] (protein specific)
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
0.07
-
IPFAAAQQRK
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.09
-
KARLMAEALK
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.12
-
VSQLYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.13
-
KARLMAEALK
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.19
-
VVQNYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.23
-
VVQNYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.24
-
VSQVYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.28
-
IPFAAAQQRK
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.32
-
VLQNYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.35
-
VSQVYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.38
-
VSQLYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.4
-
VLQNYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
Natural Substrates/ Products (Substrates) (protein specific)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
Gag polyprotein + H2O
Human immunodeficiency virus 1
-
?
-
-
?
Gag-Pol polyprotein + H2O
Human immunodeficiency virus 1
-
?
-
-
?
Substrates and Products (Substrate) (protein specific)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
Gag polyprotein + H2O
-
718370
Human immunodeficiency virus 1
?
-
-
-
?
Gag-Pol polyprotein + H2O
-
718370
Human immunodeficiency virus 1
?
-
-
-
?
IPFAAAQQRK + H2O
the protein contains a HIV-2 cleavage site
718370
Human immunodeficiency virus 1
IPFAA + AQQRK
-
-
-
?
KARLMAEALK + H2O
the protein contains a HIV-2 cleavage site
718370
Human immunodeficiency virus 1
KARLM + AEALK
-
-
-
?
VLQNYPIVQ + H2O
the protein contains a HIV-1 cleavage site
718370
Human immunodeficiency virus 1
VLQNY + PIVQ
-
-
-
?
VSQLYPIVQ + H2O
the protein contains a HIV-1 cleavage site
718370
Human immunodeficiency virus 1
VSQLY + PIVQ
-
-
-
?
VSQVYPIVQ + H2O
the protein contains a HIV-1 cleavage site
718370
Human immunodeficiency virus 1
VSQVY + PIVQ
-
-
-
?
VVQNYPIVQ + H2O
the protein contains a HIV-1 cleavage site
718370
Human immunodeficiency virus 1
VVQNY + PIVQ
-
-
-
?
Turnover Number [1/s] (protein specific)
Turnover Number Minimum [1/s]
Turnover Number Maximum [1/s]
Substrate
Commentary
Organism
Structure
0.06
-
VLQNYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.16
-
VVQNYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.18
-
VVQNYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.26
-
VLQNYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.3
-
IPFAAAQQRK
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.3
-
KARLMAEALK
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.4
-
VSQLYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.6
-
KARLMAEALK
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
1.2
-
IPFAAAQQRK
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
2.6
-
VSQVYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
3
-
VSQVYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
5.1
-
VSQLYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
KCat/KM [mM/s]
kcat/KM Value [1/mMs-1]
kcat/KM Value Maximum [1/mMs-1]
Substrate
Commentary
Organism
Structure
0.2
-
VLQNYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.8
-
VLQNYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.8
-
VVQNYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C; wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
1.1
-
IPFAAAQQRK
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
2.3
-
KARLMAEALK
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
3.3
-
VSQLYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
6.6
-
KARLMAEALK
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
8.6
-
VSQLYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
8.6
-
VSQVYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
10.8
-
VSQVYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
16.3
-
IPFAAAQQRK
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
KCat/KM [mM/s] (protein specific)
KCat/KM Value [1/mMs-1]
KCat/KM Value Maximum [1/mMs-1]
Substrate
Commentary
Organism
Structure
0.2
-
VLQNYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.8
-
VLQNYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
0.8
-
VVQNYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C; wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
1.1
-
IPFAAAQQRK
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
2.3
-
KARLMAEALK
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
3.3
-
VSQLYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
6.6
-
KARLMAEALK
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
8.6
-
VSQLYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
8.6
-
VSQVYPIVQ
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
10.8
-
VSQVYPIVQ
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
16.3
-
IPFAAAQQRK
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
Human immunodeficiency virus 1
Other publictions for EC 3.4.23.16
No.
1st author
Pub Med
title
organims
journal
volume
pages
year
Activating Compound
Application
Cloned(Commentary)
Crystallization (Commentary)
Engineering
General Stability
Inhibitors
KM Value [mM]
Localization
Metals/Ions
Molecular Weight [Da]
Natural Substrates/ Products (Substrates)
Organic Solvent Stability
Organism
Oxidation Stability
Posttranslational Modification
Purification (Commentary)
Reaction
Renatured (Commentary)
Source Tissue
Specific Activity [micromol/min/mg]
Storage Stability
Substrates and Products (Substrate)
Subunits
Temperature Optimum [°C]
Temperature Range [°C]
Temperature Stability [°C]
Turnover Number [1/s]
pH Optimum
pH Range
pH Stability
Cofactor
Ki Value [mM]
pI Value
IC50 Value
Activating Compound (protein specific)
Application (protein specific)
Cloned(Commentary) (protein specific)
Cofactor (protein specific)
Crystallization (Commentary) (protein specific)
Engineering (protein specific)
General Stability (protein specific)
IC50 Value (protein specific)
Inhibitors (protein specific)
Ki Value [mM] (protein specific)
KM Value [mM] (protein specific)
Localization (protein specific)
Metals/Ions (protein specific)
Molecular Weight [Da] (protein specific)
Natural Substrates/ Products (Substrates) (protein specific)
Organic Solvent Stability (protein specific)
Oxidation Stability (protein specific)
Posttranslational Modification (protein specific)
Purification (Commentary) (protein specific)
Renatured (Commentary) (protein specific)
Source Tissue (protein specific)
Specific Activity [micromol/min/mg] (protein specific)
Storage Stability (protein specific)
Substrates and Products (Substrate) (protein specific)
Subunits (protein specific)
Temperature Optimum [°C] (protein specific)
Temperature Range [°C] (protein specific)
Temperature Stability [°C] (protein specific)
Turnover Number [1/s] (protein specific)
pH Optimum (protein specific)
pH Range (protein specific)
pH Stability (protein specific)
pI Value (protein specific)
Expression
General Information
General Information (protein specific)
Expression (protein specific)
KCat/KM [mM/s]
KCat/KM [mM/s] (protein specific)
718370
Tie
Critical differences in HIV-1 ...
Human immunodeficiency virus 1
Protein Sci.
21
339-350
2012
-
-
1
1
2
-
3
12
-
-
-
2
-
3
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8
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12
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5
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2
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3
5
12
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8
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12
-
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11
11
717302
Newell
Cascade detection for the extr ...
Human immunodeficiency virus 1
Bioinformatics
27
3415-3422
2011
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-
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2
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2
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2
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717348
Gao
Design and synthesis of potent ...
Human immunodeficiency virus 1
Bioorg. Med. Chem. Lett.
21
3730-3733
2011
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-
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11
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2
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9
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717709
Deng
Insights into the dynamics of ...
Human immunodeficiency virus 1
J. Am. Chem. Soc.
133
9387-9394
2011
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717975
Ghosh
Design and synthesis of potent ...
Human immunodeficiency virus 1
J. Med. Chem.
54
622-634
2011
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16
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2
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9
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7
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717976
Ganguly
Design, synthesis, and X-ray c ...
Human immunodeficiency virus 1
J. Med. Chem.
54
7176-7183
2011
-
-
-
1
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9
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2
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1
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7
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1
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9
7
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1
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717998
Ozen
Dynamics of preferential subst ...
Human immunodeficiency virus 1
J. Mol. Biol.
410
726-744
2011
-
-
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1
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2
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2
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9
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9
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-
718075
He
-
Modification and biological ev ...
Human immunodeficiency virus 1
Med. Chem. Res.
20
200-209
2011
-
-
-
-
-
-
22
-
-
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2
-
1
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3
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21
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21
22
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3
-
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-
-
-
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-
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-
-
-
-
718440
Hallengaerd
Increased expression and immun ...
Human immunodeficiency virus 1
Vaccine
29
839-848
2011
-
-
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-
2
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3
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-
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1
1
1
1
-
-
707173
Tojo
Novel Protease Inhibitors (PIs ...
Human immunodeficiency virus 1
Antimicrob. Agents Chemother.
54
3460-3470
2010
-
-
1
-
2
-
4
-
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3
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707180
Lee
Lignan, sesquilignans and dili ...
Human immunodeficiency virus 1
Antiviral Res.
85
425-428
2010
-
-
-
-
-
-
3
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-
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4
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2
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1
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3
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3
3
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2
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1
-
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-
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-
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707444
Chang
Identification of broad-based ...
Human immunodeficiency virus 1
Biochem. J.
429
527-532
2010
-
-
1
-
1
-
2
1
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2
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1
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1
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2
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2
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1
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1
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2
2
2
1
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1
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1
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707528
Genoni
Computational study of the res ...
Human immunodeficiency virus 1
Biochemistry
49
4283-4295
2010
-
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4
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1
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3
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1
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4
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1
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1
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707692
Ghosh
Synthesis and biological evalu ...
Human immunodeficiency virus 1
Bioorg. Med. Chem. Lett.
20
1241-1246
2010
-
-
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9
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2
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10
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9
10
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707740
Lu
Design, asymmetric synthesis, ...
Human immunodeficiency virus 1
Bioorg. Med. Chem.
18
2037-2048
2010
-
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11
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2
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11
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11
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708083
Deeb
Exploring QSARs for inhibitory ...
Human immunodeficiency virus 1
Chem. Biol. Drug Des.
75
506-514
2010
-
-
-
-
-
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45
-
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2
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46
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45
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708386
Hu
Some insights into mechanism f ...
Human immunodeficiency virus 1
Eur. J. Med. Chem.
45
227-235
2010
-
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3
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1
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2
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3
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1
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709467
Bonini
Synthesis of new thienyl ring ...
Human immunodeficiency virus 1
J. Med. Chem.
53
1451-1457
2010
-
-
1
-
2
-
12
-
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2
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1
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1
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12
-
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1
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2
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12
12
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1
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1
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709481
Mahalingam
HIV-1 protease inhibitors with ...
Human immunodeficiency virus 1
J. Med. Chem.
53
607-615
2010
-
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1
1
1
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29
-
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2
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1
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1
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33
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1
1
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29
33
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1
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709579
Khedkar
Molecular docking and 3D-QSAR ...
Human immunodeficiency virus 1
J. Mol. Model.
16
1251-1268
2010
-
-
-
-
-
-
53
-
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2
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54
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53
54
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709580
Dirauf
Effects of the V82A and I54V m ...
Human immunodeficiency virus 1
J. Mol. Model.
16
1577-1583
2010
-
-
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2
-
2
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3
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709582
Chen
Insights into drug resistance ...
Human immunodeficiency virus 1
J. Mol. Model.
16
459-468
2010
-
-
-
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2
-
1
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2
-
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709660
Ramachary
A general approach to chiral b ...
Human immunodeficiency virus 1
J. Org. Chem.
75
74-85
2010
-
-
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4
-
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2
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709749
Nalam
Evaluating the substrate-envel ...
Human immunodeficiency virus 1
J. Virol.
84
5368-5378
2010
-
-
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1
4
-
25
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2
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112
-
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1
4
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25
112
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710216
Vathipadiekal
Molecular cloning, over expres ...
Human immunodeficiency virus 1
Peptides
31
16-21
2010
-
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1
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1
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4
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1
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1
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-
710346
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An Assay to Monitor HIV-1 Prot ...
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HIV-1 protease mutations and p ...
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Epsilon substituted lysinol de ...
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Ishima
Highly conserved glycine 86 an ...
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Analysis and characterization ...
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Assessment of QM/MM scoring fu ...
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2009
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Drug-resistant molecular mecha ...
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The folding free-energy surfac ...
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2009
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Insights into the functional r ...
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HLA-associated alterations in ...
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2009
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Clayton
Sustained and specific in vitr ...
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2009
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707378
Bihani
Resistance mechanism revealed ...
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2009
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1
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1
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1
2
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1
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1
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707512
Blackburn
Monitoring inhibitor-induced c ...
Human immunodeficiency virus 1
Biochemistry
48
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2009
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Jochim
Evaluation of triazolamers as ...
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19
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2009
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8
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707721
Waibel
On the inhibition of HIV-1 pro ...
Human immunodeficiency virus 1
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2009
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8
8
1
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1
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1
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708383
da Cunha
3D-QSAR CoMFA/CoMSIA models ba ...
Human immunodeficiency virus 1
Eur. J. Med. Chem.
44
4344-4352
2009
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31
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1
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708410
Chandra
HIV-1 protease inhibitor induc ...
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Exp. Biol. Med. (Maywood)
234
442-453
2009
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3
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Torbeev
Dynamics of 'flap' structures ...
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2009
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1
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1
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1
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1
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Li
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7
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709332
Muratori
Human immunodeficiency virus t ...
Human immunodeficiency virus 1
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3
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709443
Ghosh
Design of HIV-1 protease inhib ...
Human immunodeficiency virus 1
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52
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2009
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12
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1
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1
1
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14
12
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1
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709592
El Dine
Inhibition of the dimerization ...
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J. Nat. Prod.
72
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2009
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1
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1
-
4
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1
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4
5
1
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-
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-
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1
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710383
Castello
HIV- 1 protease inhibits Cap- ...
Human immunodeficiency virus 1
PLoS ONE
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2009
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1
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2
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1
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2
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1
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2
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710423
Adachi
Structure of HIV-1 protease in ...
Human immunodeficiency virus 1
Proc. Natl. Acad. Sci. USA
106
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2009
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1
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1
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1
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1
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1
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1
1
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1
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1
1
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1
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678341
Tyndall
Crystal structures of highly c ...
Human immunodeficiency virus 1
Biochemistry
47
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2008
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1
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1
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678346
Coman
The contribution of naturally ...
Human immunodeficiency virus 1
Biochemistry
47
731-743
2008
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6
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13
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1
6
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9
17
13
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Mimoto
Structure-activity relationshi ...
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2008
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1
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18
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18
18
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-
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-
1
-
-
-
-
-
-
-
-
-
-
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-
-
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678626
Narendra Babu
Design, synthesis and structur ...
Human immunodeficiency virus 1
Bioorg. Med. Chem.
16
874-880
2008
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-
-
-
-
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5
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3
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1
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5
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-
-
-
-
1
-
-
-
-
-
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680381
Altman
HIV-1 protease inhibitors from ...
Human immunodeficiency virus 1
J. Am. Chem. Soc.
130
6099-6113
2008
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1
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59
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59
59
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1
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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-
680900
Sayer
Effect of the active-site D25N ...
Human immunodeficiency virus 1
J. Biol. Chem.
283
13459-13470
2008
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-
-
1
1
-
1
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-
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3
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-
-
-
-
-
-
-
-
-
-
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1
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-
-
-
-
-
-
-
-
-
-
-
1
1
-
-
1
-
-
-
-
-
-
-
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-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
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681326
Clemente
Design, synthesis, evaluation, ...
Human immunodeficiency virus 1
J. Med. Chem.
51
852-860
2008
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-
-
1
-
-
3
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-
-
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-
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2
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-
-
-
-
-
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-
-
-
-
-
-
-
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-
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6
-
-
-
-
-
-
1
-
-
-
3
6
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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-
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681698
Kozisek
Ninety-nine is not enough: mol ...
Human immunodeficiency virus 1
J. Virol.
82
5869-5878
2008
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1
-
1
-
-
-
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5
-
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-
-
-
-
-
-
-
-
-
-
-
-
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-
-
-
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1
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-
1
-
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-
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-
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-
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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682227
Kona
Theoretical study on the mecha ...
Human immunodeficiency virus 1
Org. Biomol. Chem.
6
359-365
2008
-
-
-
-
-
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1
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-
2
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-
-
-
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1
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-
-
-
-
-
-
-
-
-
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682770
Altman
Computational design and exper ...
Human immunodeficiency virus 1
Proteins
70
678-694
2008
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1
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4
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2
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-
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-
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-
-
-
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-
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1
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4
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-
-
-
-
-
-
-
-
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-
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693905
Eizert
Amino acid preferences of retr ...
Human immunodeficiency virus 1
J. Virol.
82
10111-10117
2008
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1
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-
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1
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-
-
-
-
-
-
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-
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1
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-
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694787
Lee
Inhibition of HIV-1 protease a ...
Human immunodeficiency virus 1
Planta Med.
74
532-534
2008
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-
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10
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3
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7
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7
10
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-
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-
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-
-
-
-
-
-
-
-
-
-
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695291
Mahmoud
Picomolar detection of proteas ...
Human immunodeficiency virus 1
ACS Nano
2
1051-1057
2008
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1
-
-
-
-
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-
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4
-
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1
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-
-
-
-
-
-
-
-
-
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695631
Dekhtyar
Characterization of a novel hu ...
Human immunodeficiency virus 1
Antimicrob. Agents Chemother.
52
1337-1344
2008
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-
-
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2
-
2
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3
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2
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2
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-
-
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-
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-
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-
-
-
-
-
-
-
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697298
Zhou
Synthesis and biological evalu ...
Human immunodeficiency virus 1
Chem. Pharm. Bull.
56
1147-1152
2008
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1
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4
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4
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1
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4
4
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697300
Lee
Two new triterpenes from the r ...
Human immunodeficiency virus 1
Chem. Pharm. Bull.
56
711-714
2008
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6
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6
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6
6
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698514
Gonzalez
Impact of HIV-1 protease mutat ...
Human immunodeficiency virus 1
J. Antimicrob. Chemother.
61
1201-1204
2008
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1
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1
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698516
Lambert-Niclot
Impact of gag mutations on sel ...
Human immunodeficiency virus 1
J. Antimicrob. Chemother.
62
905-908
2008
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1
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1
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1
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1
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699546
Liu
Effect of flap mutations on st ...
Human immunodeficiency virus 1
J. Mol. Biol.
381
102-115
2008
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4
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2
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1
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10
-
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1
4
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2
10
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1
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699555
Boettcher
Structural and kinetic analysi ...
Human immunodeficiency virus 1
J. Mol. Biol.
383
347-357
2008
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2
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4
12
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4
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12
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1
2
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4
12
12
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4
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699896
Mosebi
Active-site mutations in the S ...
Human immunodeficiency virus 1
J. Virol.
82
11476-11479
2008
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2
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4
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-
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12
-
12
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2
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12
4
12
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-
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-
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699902
Bandaranayake
Structural analysis of human i ...
Human immunodeficiency virus 1
J. Virol.
82
6762-6766
2008
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1
1
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1
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-
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-
-
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1
-
1
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-
-
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-
-
-
-
-
-
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1
-
-
-
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701086
Emmons
Large-scale purification of hu ...
Human immunodeficiency virus 1
Protein Pept. Lett.
15
119-130
2008
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2
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-
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2
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701133
Sayer
Interactions of different inhi ...
Human immunodeficiency virus 1
Proteins
75
556-568
2008
-
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11
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4
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11
-
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701392
Moore
Suboptimal inhibition of prote ...
Human immunodeficiency virus 1
Virology
379
152-160
2008
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2
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1
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1
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2
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-
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-
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678249
Kovalevsky
Caught in the act: the 1.5 A r ...
Human immunodeficiency virus 1
Biochemistry
46
14854-14864
2007
-
-
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1
-
-
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2
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1
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-
-
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-
-
-
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-
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-
-
-
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-
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-
-
1
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-
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1
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-
-
-
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-
-
-
-
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678731
Trylska
HIV-1 protease substrate bindi ...
Human immunodeficiency virus 1
Biophys. J.
92
4179-4187
2007
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-
-
-
-
-
-
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2
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1
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-
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-
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-
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-
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-
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-
-
-
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-
-
1
-
-
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680778
Ishima
Mutational and structural stud ...
Human immunodeficiency virus 1
J. Biol. Chem.
282
17190-17199
2007
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2
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3
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1
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2
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1
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1
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681460
Kozisek
Molecular analysis of the HIV- ...
Human immunodeficiency virus 1
J. Mol. Biol.
374
1005-1016
2007
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1
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8
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1
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8
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6
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1
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1
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5
6
8
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1
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1
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8
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682765
Chellappan
Evaluation of the substrate en ...
Human immunodeficiency virus 1
Proteins
68
561-567
2007
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1
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1
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1
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664137
Toth
Closing of the flaps of HIV-1 ...
Human immunodeficiency virus 1
Biochemistry
45
6606-6614
2006
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1
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1
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1
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1
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664605
Specker
Unexpected novel binding mode ...
Human immunodeficiency virus 1
ChemMedChem
1
106-117
2006
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1
1
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8
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2
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1
1
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1
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1
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6
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1
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1
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6
8
1
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1
1
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1
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665991
Skalova
HIV-1 protease mutations and i ...
Human immunodeficiency virus 1
J. Med. Chem.
49
5777-5784
2006
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1
1
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8
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1
1
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4
8
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666078
Liu
Mechanism of drug resistance r ...
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J. Mol. Biol.
358
1191-1199
2006
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1
1
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-
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1
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-
1
1
-
-
1
-
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-
-
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-
-
1
-
-
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-
666884
Ozer
Substrate specificity in HIV-1 ...
Human immunodeficiency virus 1
Proteins
64
444-456
2006
-
-
-
-
-
-
-
-
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2
-
2
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3
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-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
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-
-
680351
Layten
The open structure of a multi- ...
Human immunodeficiency virus 1
J. Am. Chem. Soc.
128
13360-13361
2006
-
-
-
1
-
1
-
-
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2
-
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1
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1
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-
-
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-
-
-
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681109
Gohda
A quantitative structure-activ ...
Human immunodeficiency virus 1
J. Enzyme Inhib. Med. Chem.
21
609-615
2006
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-
-
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16
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16
-
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16
16
-
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
682522
Das
Crystal structure of HIV-1 pro ...
Human immunodeficiency virus 1
Proc. Natl. Acad. Sci. USA
103
18464-18469
2006
-
-
-
1
-
-
-
-
-
-
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2
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1
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-
1
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-
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-
-
1
-
-
-
-
-
-
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-
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-
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-
-
682973
Thomas
Characterization of human immu ...
Human immunodeficiency virus 1
Virology
354
261-270
2006
-
-
-
-
-
-
-
-
-
-
-
1
-
3
-
-
-
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2
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1
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2
-
-
-
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-
-
-
-
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662382
Guo
Inhibition of cellular HIV-1 p ...
Human immunodeficiency virus 1
J. Biol. Chem.
280
26018-26023
2005
-
-
1
-
-
-
1
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-
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3
-
2
-
-
-
-
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-
1
-
5
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
3
-
-
-
-
-
-
1
-
5
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
664895
Tie
Molecular basis for substrate ...
Human immunodeficiency virus 1
FEBS J.
272
5265-5277
2005
-
-
1
1
2
-
6
-
-
-
-
-
-
2
-
1
1
-
1
-
-
-
3
1
-
-
-
-
1
-
-
-
13
-
-
-
-
1
-
1
2
-
-
6
13
-
-
-
-
-
-
-
1
1
1
-
-
-
3
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
665976
Surleraux
Design of HIV-1 protease inhib ...
Human immunodeficiency virus 1
J. Med. Chem.
48
1965-1973
2005
-
2
-
-
-
-
9
-
-
-
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4
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
9
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
666063
Liu
Kinetic, stability, and struct ...
Human immunodeficiency virus 1
J. Mol. Biol.
354
789-800
2005
-
-
1
1
3
-
3
4
-
-
-
2
-
2
-
-
1
-
1
-
-
-
6
1
1
-
-
3
1
-
-
-
12
-
-
-
-
1
-
1
3
-
-
3
12
4
-
-
-
2
-
-
-
1
1
-
-
-
6
1
1
-
-
3
1
-
-
-
-
-
-
-
-
-
666190
Bagossi
Amino acid preferences for a c ...
Human immunodeficiency virus 1
J. Virol.
79
4213-4218
2005
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
10
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
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-
-
-
-
-
10
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
666873
Kovalskyy
A molecular dynamics study of ...
Human immunodeficiency virus 1
Proteins
58
450-458
2005
-
-
-
-
-
-
-
1
-
1
-
-
-
2
-
-
-
1
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
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-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
664013
Clemente
Comparing the accumulation of ...
Human immunodeficiency virus 1
Biochemistry
43
12141-12151
2004
-
-
1
1
14
-
5
1
-
-
-
-
-
2
-
-
1
-
1
-
-
-
1
-
1
-
-
-
1
-
-
-
32
-
-
-
-
1
-
1
14
-
-
5
32
1
-
-
-
-
-
-
-
1
1
-
-
-
1
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
664299
Hamada
Water-soluble prodrugs of dipe ...
Human immunodeficiency virus 1
Bioorg. Med. Chem.
12
159-170
2004
-
-
-
-
-
-
4
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
665102
Dunn
-
Human immunodeficiency virus 2 ...
Human immunodeficiency virus 1
Handbook of Proteolytic Enzymes (Barrett, A. J. ; Rowlings, N. D. ; Woessner, J. F. , eds. )
1
154-157
2004
-
-
1
1
1
-
3
2
-
-
-
-
-
1
-
1
-
-
-
-
-
-
3
1
-
-
-
-
1
-
-
-
3
-
-
-
-
1
-
1
1
-
-
3
3
2
-
-
-
-
-
-
1
-
-
-
-
-
3
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
666016
Tie
High resolution crystal struct ...
Human immunodeficiency virus 1
J. Mol. Biol.
338
341-352
2004
-
-
-
1
3
-
1
3
-
-
-
-
-
3
-
-
-
-
-
-
-
-
1
-
-
-
-
3
1
-
-
-
3
-
-
-
-
-
-
1
3
-
-
1
3
3
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
3
1
-
-
-
-
-
-
-
-
-
666106
Shuman
Kinetic and thermodynamic char ...
Human immunodeficiency virus 1
J. Mol. Recognit.
17
106-119
2004
-
1
-
-
-
-
4
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
1
-
-
-
-
-
-
4
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
648152
Tossi
Small hydroxyethylene-based pe ...
Human immunodeficiency virus 1
Bioorg. Med. Chem.
11
4719-4727
2003
-
-
-
-
-
-
18
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
18
-
-
-
-
-
-
-
18
18
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
648154
Kumar
Adaptability and flexibility o ...
Human immunodeficiency virus 1
Eur. J. Biochem.
270
1231-1239
2003
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
648165
Louis
Revisiting monomeric HIV-1 pro ...
Human immunodeficiency virus 1
J. Biol. Chem.
278
6085-6092
2003
-
-
-
-
4
-
-
-
-
-
-
-
-
2
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
648137
Beck
Defining HIV-1 protease substr ...
Human immunodeficiency virus 1
Curr. Drug Targets Infect. Disord.
2
37-50
2002
-
1
-
-
9
-
-
-
-
1
-
-
-
2
-
-
-
-
-
-
-
-
117
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
9
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
117
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
648151
Porter
HIV-1 protease: characterizati ...
Human immunodeficiency virus 1
Biochemistry
41
1302-1307
2002
-
-
-
-
-
-
-
1
-
-
-
-
-
3
-
-
-
-
-
-
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
648157
Prabu-Jeyabalan
Substrate shape determines spe ...
Human immunodeficiency virus 1
Structure
10
369-381
2002
-
1
-
1
1
-
-
-
-
-
-
1
-
2
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
1
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
648168
Pettit
Replacement of the P1 amino ac ...
Human immunodeficiency virus 1
J. Virol.
76
10226-10233
2002
-
-
-
-
-
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
648163
Pillai
1.9.ANG. X-ray study shows clo ...
Human immunodeficiency virus 1
Proteins Struct. Funct. Genet.
43
57-64
2001
-
-
1
1
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
648164
Ishima
Folded monomer of HIV-1 protea ...
Human immunodeficiency virus 1
J. Biol. Chem.
276
49110-49116
2001
-
-
1
-
3
-
1
8
-
-
-
-
-
2
-
-
1
-
-
-
-
-
6
1
-
-
-
8
-
-
-
-
-
-
-
-
-
1
-
-
3
-
-
1
-
8
-
-
-
-
-
-
-
1
-
-
-
-
6
1
-
-
-
8
-
-
-
-
-
-
-
-
-
-
648167
Mahalingam
Structural implications of dru ...
Human immunodeficiency virus 1
Proteins
43
455-464
2001
-
-
-
1
4
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
4
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
648170
Ventoso
HIV-1 protease cleaves eukaryo ...
Human immunodeficiency virus 1
Proc. Natl. Acad. Sci. USA
98
12966-12971
2001
-
-
-
-
-
-
-
-
-
-
-
1
-
7
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
648144
Haneda
Biochemical characterization o ...
Human immunodeficiency virus 1
Biochem. Biophys. Res. Commun.
275
434-439
2000
1
-
-
-
-
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
648150
Short
Probing the S1/S1' substrate b ...
Human immunodeficiency virus 1
Biochemistry
39
8768-8781
2000
-
-
-
-
1
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
648162
Hong
Crystal structure of an in viv ...
Human immunodeficiency virus 1
Protein Sci.
9
1898-1904
2000
-
-
-
1
-
-
1
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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Prabu-Jeyabalan
How does a symmetric dimer rec ...
Human immunodeficiency virus 1
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2000
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1
1
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1
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648153
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Structural and kinetic analysi ...
Human immunodeficiency virus 1
Eur. J. Biochem.
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1999
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1
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2
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648161
Louis
Proteolytic processing of HIV- ...
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1
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648169
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Autoprocessing of HIV-1 protea ...
Human immunodeficiency virus 1
Nat. Struct. Biol.
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1999
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4
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1
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3
1
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648173
Xie
Drug resistance mutations can ...
Human immunodeficiency virus 1
Protein Sci.
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1999
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648138
Ridky
Drug-resistant HIV-1 proteases ...
Human immunodeficiency virus 1
Biochemistry
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1998
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8
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49
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648139
Swairjo
Structural role of the 30's lo ...
Human immunodeficiency virus 1
Biochemistry
37
10928-10936
1998
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1
1
-
1
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1
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1
1
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1
1
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648141
Louis
Hydrophilic peptides derived f ...
Human immunodeficiency virus 1
Biochemistry
37
2105-2110
1998
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1
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24
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1
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15
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1
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24
15
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-
1
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648145
Todd
The structural stability of th ...
Human immunodeficiency virus 1
J. Mol. Biol.
283
475-488
1998
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3
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2
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1
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3
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2
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648147
Hong
X-ray crystallographic studies ...
Human immunodeficiency virus 1
Adv. Exp. Med. Biol.
436
59-63
1998
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1
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1
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1
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1
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1
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1
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1
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1
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1
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648148
Ermolieff
The effect of substrates on th ...
Human immunodeficiency virus 1
Adv. Exp. Med. Biol.
436
47-51
1998
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7
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13
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7
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8
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4
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13
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648155
Cai
Artificial neural network meth ...
Human immunodeficiency virus 1
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607-615
1998
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-
1
-
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-
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648171
Hong
Active-site mobility in human ...
Human immunodeficiency virus 1
Protein Sci.
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300-305
1998
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1
1
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1
3
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2
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4
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1
1
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-
1
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3
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1
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2
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4
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648172
Wallqvist
A cooperative folding unit in ...
Human immunodeficiency virus 1
Protein Eng.
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999-1005
1998
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1
1
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1
1
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-
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-
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-
-
-
-
-
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-
-
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648140
Komai
Inhibition of HIV-1 protease b ...
Human immunodeficiency virus 1
Biochem. Biophys. Res. Commun.
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557-561
1997
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7
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7
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1
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648142
Ermolieff
Kinetic properties of saquinav ...
Human immunodeficiency virus 1
Biochemistry
36
12364-12370
1997
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3
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1
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7
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9
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3
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1
4
9
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7
-
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-
-
9
-
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-
-
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-
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648149
Grobelny
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Antiviral activity of DG-35-VI ...
Human immunodeficiency virus 1
Antiviral Chem. Chemother.
8
99-106
1997
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-
-
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-
1
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-
-
-
-
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-
-
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-
-
-
1
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-
-
-
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-
-
-
-
-
-
-
-
-
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-
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-
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648159
Vance
Conformational selectivity of ...
Human immunodeficiency virus 1
J. Biol. Chem.
272
15603-15606
1997
1
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2
1
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4
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1
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-
3
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3
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-
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-
1
-
-
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-
2
1
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4
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-
-
-
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1
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-
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-
3
-
-
-
-
3
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-
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647817
Rose
Three-dimensional structures o ...
Human immunodeficiency virus 1
Biochemistry
35
12933-12944
1996
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1
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1
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648143
Davis
Regulation of HIV-1 protease a ...
Human immunodeficiency virus 1, Human immunodeficiency virus 1 HXB2
Biochemistry
35
2482-2488
1996
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1
1
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1
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1
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1
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1
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648146
Silva
Inhibition and catalytic mecha ...
Human immunodeficiency virus 1
J. Mol. Biol.
255
321-346
1996
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1
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1
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1
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-
-
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-
-
-
-
-
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-
1
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-
1
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-
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648156
Szeltner
Rate-determining steps in HIV- ...
Human immunodeficiency virus 1
J. Biol. Chem.
271
32180-32184
1996
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2
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5
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5
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2
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5
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648158
Szeltner
Conformational stability and c ...
Human immunodeficiency virus 1
J. Biol. Chem.
271
5458-5463
1996
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1
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2
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1
1
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2
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648176
March
-
Substrate-based cyclic peptido ...
Human immunodeficiency virus 1
J. Am. Chem. Soc.
118
3375-3379
1996
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1
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1
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648175
Abbenante
-
Regioselective structural and ...
Human immunodeficiency virus 1
J. Am. Chem. Soc.
117
10220-10226
1995
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1
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648121
Stebbins
Expression systems for retrovi ...
Human immunodeficiency virus 1
Methods Enzymol.
241
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1
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1
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1
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1
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648122
Hellen
Assay methods for retroviral p ...
Human immunodeficiency virus 1
Methods Enzymol.
241
46-58
1994
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7
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1
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7
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648123
von der Helm
Identification, purification, ...
Human immunodeficiency virus 1
Methods Enzymol.
241
89-104
1994
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1
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1
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1
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1
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1
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648124
Meek
Use of steady state kinetic me ...
Human immunodeficiency virus 1
Methods Enzymol.
241
127-156
1994
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6
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1
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6
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648125
Ringe
X-ray structures of retroviral ...
Human immunodeficiency virus 1
Methods Enzymol.
241
157-177
1994
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15
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11
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1
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15
11
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648126
Lin
Relationships of human immunod ...
Human immunodeficiency virus 1
Methods Enzymol.
241
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1994
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1
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Specificity of retroviral prot ...
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9
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9
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648128
Vacca
Design of tight-binding inhibi ...
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29
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2
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1
1
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5
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22
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22
29
5
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-
-
-
-
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-
-
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-
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1
1
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648134
Yamazaki
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NMR and X-Ray evidence that th ...
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1
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1
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3
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-
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-
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-
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-
-
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-
1
1
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-
-
-
-
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1
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-
1
-
-
-
1
-
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3
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-
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648135
Kim
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Expression and purification of ...
Human immunodeficiency virus 1
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1994
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1
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1
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1
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1
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1
-
1
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1
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1
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648136
Mildner
The HIV-1 protease as enzyme a ...
Human immunodeficiency virus 1
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10
1
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16
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4
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1
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2
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5
4
14
1
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10
1
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16
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16
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16
22
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Athauda
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2
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1
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2
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Friedman
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Inhibition of the HIV-1 protea ...
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1
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1
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648133
Hui
Large scale purification and r ...
Human immunodeficiency virus 1
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1
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2
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2
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648132
Blundell
The 3-D structure of HIV-1 pro ...
Human immunodeficiency virus 1
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425-430
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1
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1
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1
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2
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1
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1
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648120
Miller
Structure of complex of synthe ...
Human immunodeficiency virus 1
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1
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1
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1
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1
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648174
Wlodawer
Weber, I.T.; Selk, L.M.; Claws ...
Human immunodeficiency virus 1
Science
245
616-621
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1
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