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Literature summary for 3.4.23.16 extracted from
- Critical differences in HIV-1 and HIV-2 protease specificity for clinical inhibitors (2012), Protein Sci., 21, 339-350.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| mutant enzyme V32I/I47V/V82I is expressed in Escherichia coli BL21(DE3) cells | Human immunodeficiency virus 1 |
Crystallization (Commentary)
| Crystallization (Comment) | 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 |
Protein Variants
| Protein Variants | Comment | 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 | Comment | 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 | Comment | 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 | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| Gag polyprotein + H2O | Human immunodeficiency virus 1 | - |
? | - |
? | |
| Gag-Pol polyprotein + H2O | Human immunodeficiency virus 1 | - |
? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Human immunodeficiency virus 1 | Q7SSE3 | - |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| Gag polyprotein + H2O | - |
Human immunodeficiency virus 1 | ? | - |
? | |
| Gag-Pol polyprotein + H2O | - |
Human immunodeficiency virus 1 | ? | - |
? | |
| IPFAAAQQRK + H2O | the protein contains a HIV-2 cleavage site | Human immunodeficiency virus 1 | IPFAA + AQQRK | - |
? | |
| KARLMAEALK + H2O | the protein contains a HIV-2 cleavage site | Human immunodeficiency virus 1 | KARLM + AEALK | - |
? | |
| VLQNYPIVQ + H2O | the protein contains a HIV-1 cleavage site | Human immunodeficiency virus 1 | VLQNY + PIVQ | - |
? | |
| VSQLYPIVQ + H2O | the protein contains a HIV-1 cleavage site | Human immunodeficiency virus 1 | VSQLY + PIVQ | - |
? | |
| VSQVYPIVQ + H2O | the protein contains a HIV-1 cleavage site | Human immunodeficiency virus 1 | VSQVY + PIVQ | - |
? | |
| VVQNYPIVQ + H2O | the protein contains a HIV-1 cleavage site | Human immunodeficiency virus 1 | VVQNY + PIVQ | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| HIV-1 protease | - |
Human immunodeficiency virus 1 |
| PR1 | - |
Human immunodeficiency virus 1 |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | 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 | Comment | 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 | Human immunodeficiency virus 1 | |
| 0.00000004 | - |
darunavir | 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 | |
kcat/KM [mM/s]
| kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | 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 | Human immunodeficiency virus 1 | |
| 0.8 | - |
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 | |
| 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 | |
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