Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.23.16 extracted from

  • Kozisek, M.; Bray, J.; Rezacova, P.; Saskova, K.; Brynda, J.; Pokorna, J.; Mammano, F.; Rulisek, L.; Konvalinka, J.
    Molecular analysis of the HIV-1 resistance development: enzymatic activities, crystal structures, and thermodynamics of nelfinavir-resistant HIV protease mutants (2007), J. Mol. Biol., 374, 1005-1016.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
overexpressed in Escherichia coli BL21 Human immunodeficiency virus 1

Crystallization (Commentary)

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

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 [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

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Human immunodeficiency virus 1

Substrates and Products (Substrate)

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 [1/s]

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 [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