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Literature summary for 3.4.23.16 extracted from

  • Ermolieff, J.; Lin, X.; Tang, J.
    Kinetic properties of saquinavir-resistant mutants of human immunodeficiency virus type 1 protease and their implications in drug resistance in vivo (1997), Biochemistry, 36, 12364-12370.
    View publication on PubMed
Search for more literature for 3.4.23.16

Protein Variants

Protein Variants Comment Organism
G48V the kcat/Km ratio for the substrate KARVLAEAMS is 55% of that for the autoproteolysis resistant variant Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1
G48V less loss of activity with saquinavir as inhibitor, Ki is 13.5fold higher Human immunodeficiency virus 1
G48V mutant enzyme with 9.3% of the activity of the wild-type enzyme with VSQNYPIVQ as substrate Human immunodeficiency virus 1
G48V/L90M mutant enzyme with 1.7% of the activity of the wild-type enzyme with VSQNYPIVQ as substrate, less loss of activity with saquinavir as inhibitor, Ki is 419fold higher than that of the wild-type enzyme Human immunodeficiency virus 1
L90M mutant enzyme with 7.9% of the activity of the wild-type enzyme with VSQNYPIVQ as substrate, less loss of activity with saquinavir as inhibitor, Ki is 3fold higher Human immunodeficiency virus 1

Inhibitors

Inhibitors Comment Organism Structure
saquinavir
-
 Human immunodeficiency virus 1

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.1
-
 GAETFYVDGAA pH 5.0, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.34
-
 RQGTVSFNFPQITL pH 5.0, 37°C, mutant enzyme A28S Human immunodeficiency virus 1
0.5
-
 TATIMMQRGN pH 5.0, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.54
-
 RQGTVSFNFPQITL pH 5.0, 37°C, wild-type enzyme Human immunodeficiency virus 1
1.15
-
 VSQNYPIVQ pH 5.0, 37°C, mutant enzyme L90M Human immunodeficiency virus 1
1.5
-
 VSQNYPIVQ pH 5.0, 37°C, wild-type enzyme Human immunodeficiency virus 1
3.8
-
 VSQNYPIVQ pH 5.0, 37°C, mutant enzyme G48V/L90M Human immunodeficiency virus 1
6.4
-
 KLRPGNFLQSRP pH 5.0, 37°C, wild-type enzyme Human immunodeficiency virus 1
9.8
-
 VSQNYPIVQ pH 5.0, 37°C, mutant enzyme G48V 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.
GAETFYVDGAA + H2O
-
 Human immunodeficiency virus 1 GAETF + YVDGAA
-
 ?
HKARVLAEAMS + H2O
-
 Human immunodeficiency virus 1 HKARVL + AEAMS
-
 ?
KARVL-Phe(NO2)-EAM + H2O
-
 Human immunodeficiency virus 1 KARVL + Phe(NO2)-EAM
-
 ?
KLRPGNFLQSRP + H2O
-
 Human immunodeficiency virus 1 KLRPGNF + LQSRP
-
 ?
RQGTVSFNFPQITL + H2O
-
 Human immunodeficiency virus 1 RQGTVSFNF + PQITL
-
 ?
TATIMMQRGN + H2O
-
 Human immunodeficiency virus 1 TATIM + MQRGN
-
 ?
VSQNYPIVQ + H2O
-
 Human immunodeficiency virus 1 VSQNY + PIVQ
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.018
-
 TATIMMQRGN pH 5.0, 37°C, mutant enzyme A28S Human immunodeficiency virus 1
2.2
-
 VSQNYPIVQ pH 5.0, 37°C, mutant enzyme G48V/L90M Human immunodeficiency virus 1
3.14
-
 VSQNYPIVQ pH 5.0, 37°C, mutant enzyme L90M Human immunodeficiency virus 1
5.05
-
 GAETFYVDGAA pH 5.0, 37°C, wild-type enzyme Human immunodeficiency virus 1
12.7
-
 KLRPGNFLQSRP pH 5.0, 37°C, wild-type enzyme Human immunodeficiency virus 1
31.3
-
 VSQNYPIVQ pH 5.0, 37°C, mutant enzyme G48V Human immunodeficiency virus 1
51.8
-
 VSQNYPIVQ pH 5.0, 37°C, wild-type enzyme Human immunodeficiency virus 1
58.8
-
 TATIMMQRGN pH 5.0, 37°C, wild-type enzyme Human immunodeficiency virus 1
62.7
-
 RQGTVSFNFPQITL pH 5.0, 37°C, wild-type enzyme Human immunodeficiency virus 1

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000002
-
 saquinavir pH 5.0, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.0000006
-
 saquinavir pH 5.0, 37°C, mutant enzyme G48V Human immunodeficiency virus 1
0.0000027
-
 saquinavir pH 5.0, 37°C, mutant enzyme G48V Human immunodeficiency virus 1
0.0000837
-
 saquinavir pH 5.0, 37°C, mutant enzyme G48V/L90M Human immunodeficiency virus 1