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Literature summary for 3.4.23.16 extracted from

  • Ishima, R.; Ghirlando, R.; Tozser, J.; Gronenborn, A.M.; Torchia, D.A.; Louis, J.M.
    Folded monomer of HIV-1 protease (2001), J. Biol. Chem., 276, 49110-49116.
    View publication on PubMed
Search for more literature for 3.4.23.16

Cloned(Commentary)

Cloned (Comment) Organism
mutant enzymes Human immunodeficiency virus 1

Protein Variants

Protein Variants Comment Organism
additional information truncated enzyme PR-(5-95): displays severe aggregation. The catalytic activity is similar to that of wild-type enzyme. The lower kcat/Km observed for Pr-(5-99) using five different substrates suggests that only a small fraction of the protein contrubutes to the observed activity. PR-(1-95) does not exhibit detectable cleavage of any of the substrates tested Human immunodeficiency virus 1
Q7K/L33I/L63I/C67A/C95A mutant enzyme with restricted autoproteolysis, self-degradation Human immunodeficiency virus 1
R87K loss of specific interactions involving the side chain of Arg87 destabilizes the mutant enzyme by perturbing the inner C-terminal region that is sandwiched between the two beta-strands formed by the N-terminal residues in the mature protease Human immunodeficiency virus 1

Inhibitors

Inhibitors Comment Organism Structure
DMP323
-
 Human immunodeficiency virus 1

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.016
-
 IRKILFLDG pH 5.6, 37°C, autolysis resistant enzyme form PR with the mutations Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1
0.021
-
 KARVLAEAMS pH 5.6, 37°C, autolysis resistant enzyme form PR with the mutations Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1
0.032
-
 AETFYVDGAA pH 5.6, 37°C, autolysis resistant enzyme form PR with the mutations Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1
0.041
-
 AETFYVDGAA pH 5.6, 37°C, autolysis reistant and truncated enzyme form PR-(5-99) with mutation Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1
0.044
-
 CTLNFPISP pH 5.6, 37°C, autolysis resistant enzyme form PR with the mutations Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1
0.046
-
 IRKILFLDG pH 5.6, 37°C, autolysis reistant and truncated enzyme form PR-(5-99) with mutation Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1
0.087
-
 CTLNFPISP pH 5.6, 37°C, autolysis reistant and truncated enzyme form PR-(5-99) with mutation Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1
0.192
-
 KARVLAEAMS pH 5.6, 37°C, autolysis reistant and truncated enzyme form PR-(5-99) with mutation Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1 P03367
-
-

Purification (Commentary)

Purification (Comment) Organism
purification of wild-type enzyme, mutant enzyme R87K, and the truncated proteins PR-(1-95), PR-(5-99) and PR-(5-95) Human immunodeficiency virus 1

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
AETFYVDGAA + H2O
-
 Human immunodeficiency virus 1 AETF + YVDGAA
-
 ?
CTLNFPISP + H2O
-
 Human immunodeficiency virus 1 CTLNF + PISP
-
 ?
IRKILFLDG + H2O
-
 Human immunodeficiency virus 1 IRKIL + FLDG
-
 ?
KARV-Nle-Phe(NO2)-EA-Nle-NH2 + H2O
-
 Human immunodeficiency virus 1 KARV-Nle + Phe(NO2)-EA-Nle-NH2
-
 ?
KARVLAEAMS + H2O
-
 Human immunodeficiency virus 1 KARVL + AEAMS
-
 ?
VSFNFPQITL + H2O
-
 Human immunodeficiency virus 1 VSFNF + PQITL
-
 ?

Subunits

Subunits Comment Organism
dimer the mature enzyme folds into an enzymatically active stable dimer, both N-terminal and C-terminal beta-strands contribute to dimer stability Human immunodeficiency virus 1

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.0008
-
 AETFYVDGAA pH 5.6, 37°C, autolysis reistant and truncated enzyme form PR-(5-99) with mutation Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1
0.05
-
 CTLNFPISP pH 5.6, 37°C, autolysis reistant and truncated enzyme form PR-(5-99) with mutation Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1
0.08
-
 IRKILFLDG pH 5.6, 37°C, autolysis reistant and truncated enzyme form PR-(5-99) with mutation Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1
0.11
-
 KARVLAEAMS pH 5.6, 37°C, autolysis reistant and truncated enzyme form PR-(5-99) with mutation Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1
0.41
-
 AETFYVDGAA pH 5.6, 37°C, autolysis resistant enzyme form PR with the mutations Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1
0.89
-
 KARVLAEAMS pH 5.6, 37°C, autolysis resistant enzyme form PR with the mutations Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1
1.2
-
 IRKILFLDG pH 5.6, 37°C, autolysis resistant enzyme form PR with the mutations Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1
1.72
-
 CTLNFPISP pH 5.6, 37°C, autolysis resistant enzyme form PR with the mutations Q7K/L33I/L63I/C67A/C95A Human immunodeficiency virus 1