Cloned (Comment) | Organism |
---|---|
overexpressed in Escherichia coli BL21 | Human immunodeficiency virus 1 |
Crystallization (Comment) | Organism |
---|---|
hanging drop vapor diffusion technique, crystal structures of nelfinavir-resistant HIV protease mutants (D30N, D30N/A71V, D30N/N88D, and D30N/L90M) with nelfinavir | Human immunodeficiency virus 1 |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
indinavir | - |
Human immunodeficiency virus 1 | |
lopinavir | - |
Human immunodeficiency virus 1 | |
nelfinavir | in the HIV-1 protease sequence of viral variants resistant to the inhibitor nelfinavir, the mutations D30N and L90M appear frequently | Human immunodeficiency virus 1 | |
ritonavir | - |
Human immunodeficiency virus 1 | |
saquinavir | - |
Human immunodeficiency virus 1 |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.006 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme N88D | Human immunodeficiency virus 1 | |
0.011 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme L90M | Human immunodeficiency virus 1 | |
0.014 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme A71V | Human immunodeficiency virus 1 | |
0.015 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, wild-type enzyme | Human immunodeficiency virus 1 | |
0.018 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme D30N | Human immunodeficiency virus 1 | |
0.018 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme D30N/N88D | Human immunodeficiency virus 1 | |
0.024 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme D30N/A71V | Human immunodeficiency virus 1 | |
0.027 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme D30N/L63PA71V/L90M | Human immunodeficiency virus 1 | |
0.029 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme D30N/L90M | Human immunodeficiency virus 1 |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Human immunodeficiency virus 1 | - |
- |
- |
Purification (Comment) | Organism |
---|---|
- |
Human immunodeficiency virus 1 |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 + H2O | - |
Human immunodeficiency virus 1 | Lys-Ala-Arg-Val-Nle + Phe(4-NO2)-Glu-Ala-Nle-NH2 | - |
? |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
8 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme N88D | Human immunodeficiency virus 1 | |
12 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme A71V | Human immunodeficiency virus 1 | |
14 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme D30N/A71V | Human immunodeficiency virus 1 | |
16 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme D30N/L63PA71V/L90M | Human immunodeficiency virus 1 | |
16 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme L90M | Human immunodeficiency virus 1 | |
17 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme D30N | Human immunodeficiency virus 1 | |
22 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme D30N/L90M | Human immunodeficiency virus 1 | |
24 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, mutant enzyme D30N/N88D | Human immunodeficiency virus 1 | |
30 | - |
Lys-Ala-Arg-Val-Nle-Phe(4-NO2)-Glu-Ala-Nle-NH2 | 37°C, pH 4.7, wild-type enzyme | 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, A71V, D30N/A71V, D30N/N88D, D30N/L90M, D30N/L63P/A71V/L90M) on the Ki-values for saquinavir, ritonavir, indinavir, nelfinavir, and lopinavir | Human immunodeficiency virus 1 | |
0.000000015 | - |
ritonavir | pH 4.7, wild-type enzyme | Human immunodeficiency virus 1 | |
0.000000018 | - |
lopinavir | pH 4.7, wild-type enzyme | Human immunodeficiency virus 1 | |
0.00000004 | - |
saquinavir | pH 4.7, wild-type enzyme | Human immunodeficiency virus 1 | |
0.00000007 | - |
nelfinavir | pH 4.7, wild-type enzyme | Human immunodeficiency virus 1 | |
0.00000012 | - |
indinavir | pH 4.7, wild-type enzyme | Human immunodeficiency virus 1 |