Crystallization (Comment) | Organism |
---|---|
crystallization of a protein-inhibitor complex | Human immunodeficiency virus 1 |
Protein Variants | Comment | Organism |
---|---|---|
D30N | mutant of HIV-1 protease subtype B, kcat/Km is 4.2fold lower than wild-type value | Human immunodeficiency virus 1 |
D30N | mutant of HIV-1 protease subtype C, kcat/Km is 1.8fold lower than wild-type value | Human immunodeficiency virus 1 |
D30N/L90M | mutant of HIV-1 protease subtype B, kcat/Km is 9.2fold lower than wild-type value | Human immunodeficiency virus 1 |
D30N/L90M | mutant of HIV-1 protease subtype C, kcat/Km is 1.9fold lower than wild-type value | Human immunodeficiency virus 1 |
D30N/N88D | mutant of HIV-1 protease subtype B, kcat/Km is 1.4fold lower than wild-type value | Human immunodeficiency virus 1 |
D30N/N88D | mutant of HIV-1 protease subtype C, kcat/Km is 1.9fold lower than wild-type value | Human immunodeficiency virus 1 |
L90M | mutant of HIV-1 protease subtype B, kcat/Km is nearly identical to wild-type value | Human immunodeficiency virus 1 |
L90M | mutant of HIV-1 protease subtype C, kcat/Km is 1.6fold lower than wild-type value | Human immunodeficiency virus 1 |
N88D | mutant of HIV-1 protease subtype B, kcat/Km is 1.4fold higher than wild-type value | Human immunodeficiency virus 1 |
N88D | mutant of HIV-1 protease subtype C, kcat/Km is 1.7fold lower than wild-type value | Human immunodeficiency virus 1 |
N88D/L90M | mutant of HIV-1 protease subtype B, kcat/Km is 1.6fold lower than wild-type value | Human immunodeficiency virus 1 |
N88D/L90M | mutant of HIV-1 protease subtype C, kcat/Km is 1.1fold higher than wild-type value | Human immunodeficiency virus 1 |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
amprenavir | - |
Human immunodeficiency virus 1 | |
atazanavir | - |
Human immunodeficiency virus 1 | |
indinavir | structural analyses of the subtype C protease bound to nelfinavir and indinavir showed that these inhibitors form similar interactions with the residues in the active site of subtype B and C proteases | Human immunodeficiency virus 1 | |
lopinavir | - |
Human immunodeficiency virus 1 | |
additional information | inhibition analysis with eight clinically used protease inhibitors reveales that the natural polymorphisms found in subtype C protease, in combination with drug resistance mutations, can influence enzymatic catalytic efficiency and inhibitor resistance | Human immunodeficiency virus 1 | |
nelfinavir | structural analyses of the subtype C protease bound to nelfinavir and indinavir showed that these inhibitors form similar interactions with the residues in the active site of subtype B and C proteases | Human immunodeficiency virus 1 | |
ritonavir | - |
Human immunodeficiency virus 1 | |
saquinavir | - |
Human immunodeficiency virus 1 | |
tipranavir | - |
Human immunodeficiency virus 1 |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.01 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease mutant L90M | Human immunodeficiency virus 1 | |
0.016 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease mutant N88D | Human immunodeficiency virus 1 | |
0.017 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype C protease | Human immunodeficiency virus 1 | |
0.019 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease D30N/N88D | Human immunodeficiency virus 1 | |
0.0195 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease | Human immunodeficiency virus 1 | |
0.022 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease mutant N88D | Human immunodeficiency virus 1 | |
0.023 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease D30N/L90M | Human immunodeficiency virus 1 | |
0.023 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease mutant L90M | Human immunodeficiency virus 1 | |
0.024 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease N88D/L90M | Human immunodeficiency virus 1 | |
0.03 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease N88D/L90M | Human immunodeficiency virus 1 | |
0.035 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease mutant 0.061 D30N/N88D | Human immunodeficiency virus 1 | |
0.0386 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease mutant D30N | Human immunodeficiency virus 1 | |
0.061 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease mutant 0.03 D30M/L90M | Human immunodeficiency virus 1 | |
0.064 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype C protease mutant D30N | Human immunodeficiency virus 1 |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Human immunodeficiency virus 1 | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly + H2O | - |
Human immunodeficiency virus 1 | Lys-Ala-Arg-Val-Nle + Phe(4-NO2)-Glu-Ala-Nle-Gly | - |
? |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
3.2 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease D30N/N88D | Human immunodeficiency virus 1 | |
3.5 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease mutant D30M/L90M | Human immunodeficiency virus 1 | |
4 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease D30N/L90M | Human immunodeficiency virus 1 | |
4.3 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease mutant N88D | Human immunodeficiency virus 1 | |
4.8 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease mutant L90M | Human immunodeficiency virus 1 | |
5 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease mutant D30N | Human immunodeficiency virus 1 | |
5.6 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype C protease | Human immunodeficiency virus 1 | |
5.8 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease mutant L90M | Human immunodeficiency virus 1 | |
10 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease | Human immunodeficiency virus 1 | |
10.2 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease N88D/L90M | Human immunodeficiency virus 1 | |
12 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease mutant N88D | Human immunodeficiency virus 1 | |
12 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype C protease mutant D30N | Human immunodeficiency virus 1 | |
12.4 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease mutant D30N/N88D | Human immunodeficiency virus 1 | |
13 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-Gly | 37°C, pH 4.7, HIV-1 subtype B protease N88D/L90M | Human immunodeficiency virus 1 |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | influence of mutations (D30N, N88D, L90M, D30N/L90M, D30N/N88D, N88D/L90M) on Ki-values for ritonavir, indinavir, nelfinavir, saquinavir, amprenavir, lopinavir, atazanavir, tipranavir | Human immunodeficiency virus 1 | |
0.00000007 | - |
ritonavir | HIV-1 subtype B protease | Human immunodeficiency virus 1 | |
0.00000007 | - |
atazanavir | HIV-1 subtype B protease | Human immunodeficiency virus 1 | |
0.00000011 | - |
lopinavir | HIV-1 subtype B protease | Human immunodeficiency virus 1 | |
0.00000011 | - |
tipranavir | HIV-1 subtype C protease | Human immunodeficiency virus 1 | |
0.00000013 | - |
atazanavir | HIV-1 subtype C protease | Human immunodeficiency virus 1 | |
0.00000019 | - |
lopinavir | HIV-1 subtype C protease | Human immunodeficiency virus 1 | |
0.00000027 | - |
ritonavir | HIV-1 subtype C protease | Human immunodeficiency virus 1 | |
0.00000029 | - |
amprenavir | HIV-1 subtype C protease | Human immunodeficiency virus 1 | |
0.0000004 | - |
amprenavir | HIV-1 subtype B protease | Human immunodeficiency virus 1 | |
0.0000004 | - |
tipranavir | HIV-1 subtype B protease | Human immunodeficiency virus 1 | |
0.0000017 | - |
nelfinavir | HIV-1 subtype B protease | Human immunodeficiency virus 1 | |
0.0000018 | - |
indinavir | HIV-1 subtype B protease | Human immunodeficiency virus 1 | |
0.0000022 | - |
saquinavir | HIV-1 subtype B protease | Human immunodeficiency virus 1 | |
0.0000026 | - |
saquinavir | HIV-1 subtype C protease | Human immunodeficiency virus 1 | |
0.0000027 | - |
nelfinavir | HIV-1 subtype C protease | Human immunodeficiency virus 1 | |
0.0000033 | - |
indinavir | HIV-1 subtype C protease | Human immunodeficiency virus 1 |