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Literature summary for 3.4.23.16 extracted from
- Room temperature neutron crystallography of drug resistant HIV-1 protease uncovers limitations of X-ray structural analysis at 100 K (2017), J. Med. Chem., 60, 2018-2025 .
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expressed in Escherichia coli BL21(DE3) cells | Human immunodeficiency virus 1 |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
| mutant enzyme V32I/I47V/V82I in complex with amprenavir, sitting drop vapor diffusion method, using 0.1M MES, 0.9 M NaCl, pH 6.0 in H2O | Human immunodeficiency virus 1 |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| V32I/I47V/V82I | the three mutations do not significantly alter the interaction between inhibitor amprenavir and the enzyme | Human immunodeficiency virus 1 |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| amprenavir | - |
Human immunodeficiency virus 1 |  |
| darunavir | - |
Human immunodeficiency virus 1 | |
| KNI-272 | - |
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 | - |
? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Human immunodeficiency virus 1 | Q7SSI0 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| high performance liquid chromatography and gel filtration | Human immunodeficiency virus 1 |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| Gag polyprotein + H2O | - |
Human immunodeficiency virus 1 | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| HIV-1 protease | - |
Human immunodeficiency virus 1 |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00000039 | - |
amprenavir | wild type enzyme, at pH 5.0 and 20°C | Human immunodeficiency virus 1 | |
| 0.000001 | - |
amprenavir | mutant enzyme V32I/I47V/V82I, at pH 4.0 and 28°C | Human immunodeficiency virus 1 | |
| 0.0000035 | - |
amprenavir | mutant enzyme V32I/I47V/V82I, at pH 5.8 and 28°C | Human immunodeficiency virus 1 | |
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Release 2023.1 (January 2023)
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