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Literature summary for 3.4.23.16 extracted from

  • Liu, F.; Kovalevsky, A.Y.; Tie, Y.; Ghosh, A.K.; Harrison, R.W.; Weber, I.T.
    Effect of flap mutations on structure of HIV-1 protease and inhibition by saquinavir and darunavir (2008), J. Mol. Biol., 381, 102-115.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.23.16

Crystallization (Commentary)

Crystallization (Comment) Organism
mutants I50V, I54V, I54M in complex with saquinavir, and mutants G48V, I54V, and I54M in complex with darunavir, at resolutions of 1.05-1.40 A. The mutants show changes in conformation of the flap region, interactions with adjacent residues, inhibitor binding, and the conformation of the 80s loop relative to the wild-type protease Human immunodeficiency virus 1

Protein Variants

Protein Variants Comment Organism
G48V mutation in flap region. About 30% of wild-type activity, poor inhibition by saquinavir and darunavir Human immunodeficiency virus 1
I50V mutation in flap region. About 10% of wild-type activity Human immunodeficiency virus 1
I54M mutation in flap region. Activity comparable to wild-type Human immunodeficiency virus 1
I54V mutation in flap region. About 40% of wild-type activity Human immunodeficiency virus 1

Inhibitors

Inhibitors Comment Organism Structure
darunavir
-
 Human immunodeficiency virus 1
saquinavir
-
 Human immunodeficiency virus 1

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.03
-
 Abz-Thr-Ile-Nle-Phe(NO2)-Gln-Arg wild-type, pH 5.6, 26°C Human immunodeficiency virus 1
0.041
-
 Abz-Thr-Ile-Nle-Phe(NO2)-Gln-Arg mutant I54M, pH 5.6, 26°C Human immunodeficiency virus 1
0.043
-
 Abz-Thr-Ile-Nle-Phe(NO2)-Gln-Arg mutant I54V, pH 5.6, 26°C Human immunodeficiency virus 1
0.091
-
 Abz-Thr-Ile-Nle-Phe(NO2)-Gln-Arg mutant G48V, pH 5.6, 26°C Human immunodeficiency virus 1
0.109
-
 Abz-Thr-Ile-Nle-Phe(NO2)-Gln-Arg mutant I50V, pH 5.6, 26°C Human immunodeficiency virus 1

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Abz-Thr-Ile-Nle-(p-nitro)Phe-Gln-Arg-NH2 + H2O
-
 Human immunodeficiency virus 1 Abz-Thr-Ile-Nle + (p-nitro)Phe-Gln-Arg-NH2
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.1
-
 Abz-Thr-Ile-Nle-Phe(NO2)-Gln-Arg mutant I50V, pH 5.6, 26°C Human immunodeficiency virus 1
2.23
-
 Abz-Thr-Ile-Nle-Phe(NO2)-Gln-Arg mutant I54V, pH 5.6, 26°C Human immunodeficiency virus 1
3.2
-
 Abz-Thr-Ile-Nle-Phe(NO2)-Gln-Arg wild-type, pH 5.6, 26°C Human immunodeficiency virus 1
3.67
-
 Abz-Thr-Ile-Nle-Phe(NO2)-Gln-Arg mutant G48V, pH 5.6, 26°C Human immunodeficiency virus 1
5
-
 Abz-Thr-Ile-Nle-Phe(NO2)-Gln-Arg mutant I54M, pH 5.6, 26°C Human immunodeficiency virus 1

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000042
-
 darunavir wild-type, pH 5.6, 26°C Human immunodeficiency virus 1
0.00000058
-
 saquinavir wild-type, pH 5.6, 26°C Human immunodeficiency virus 1
0.0000016
-
 saquinavir mutant I54M, pH 5.6, 26°C Human immunodeficiency virus 1
0.0000022
-
 darunavir mutant I54M, pH 5.6, 26°C Human immunodeficiency virus 1
0.000005
-
 saquinavir mutant I54V, pH 5.6, 26°C Human immunodeficiency virus 1
0.000006
-
 darunavir mutant I54V, pH 5.6, 26°C Human immunodeficiency virus 1
0.00001
-
 darunavir mutant I50V, pH 5.6, 26°C Human immunodeficiency virus 1
0.000017
-
 saquinavir mutant G48V, pH 5.6, 26°C Human immunodeficiency virus 1
0.000018
-
 saquinavir mutant I50V, pH 5.6, 26°C Human immunodeficiency virus 1
0.000036
-
 darunavir mutant G48V, pH 5.6, 26°C Human immunodeficiency virus 1