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Literature summary for 3.4.23.16 extracted from
- Interactions of different inhibitors with active-site aspartyl residues of HIV-1 protease and possible relevance to pepsin (2008), Proteins, 75, 556-568.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| acetyl pepstatin | study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry. Binding is most sensitive to mutantion D25N, with DeltaTm ratio for mutant/wild-type of 16.3. Binding is nearly abolished by the mutation D29N | Human immunodeficiency virus 1 |  |
| amprenavir | study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry. Binding is most sensitive to mutantion D25N, with DeltaTm ratio for mutant/wild-type of 35.8 | Human immunodeficiency virus 1 | |
| atazanavir | study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry | Human immunodeficiency virus 1 | |
| darunavir | study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry | Human immunodeficiency virus 1 | |
| indinavir | study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry | Human immunodeficiency virus 1 | |
| lopinavir | study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry | Human immunodeficiency virus 1 | |
| N-[(2S)-2-[(N-acetylthreonylisoleucyl)amino]hexyl]norleucyl-N-(3-carbamimidamido-1-carbamoylpropyl)-6-oxolysinamide | i.e. RPB, nonhydrolyzable substrate analogue. Study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry. Binding is nearly abolished by the mutation D29N, but hyrdly affected by mutation D25N | Human immunodeficiency virus 1 | |
| nelfinavir | study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry | Human immunodeficiency virus 1 | |
| ritonavir | study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry | Human immunodeficiency virus 1 | |
| saquinavir | study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry | Human immunodeficiency virus 1 | |
| tipranavir | study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry | Human immunodeficiency virus 1 | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Human immunodeficiency virus 1 | - |
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