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Literature summary for 3.4.23.16 extracted from

  • Mildner, A.M.; Rothrock, D.J.; Leone, J.W.; Bannow, C.A.; Lull, J.M.; Reardon, I.M.; Sarcich, J.L.; Howe, W.J.; Tomich, C.S.C.; Smith, C.W.; Heinrikson, R.L.; Tomasselli, A.G.
    The HIV-1 protease as enzyme and substrate: mutagenesis of autolysis sites and generation of a stable mutant with retained kinetic properties (1994), Biochemistry, 33, 9405-9413.
    View publication on PubMed
Search for more literature for 3.4.23.16

Cloned(Commentary)

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

Protein Variants

Protein Variants Comment Organism
Q7 mutant enzyme has markedly enhanced stability over the wild-type enzyme Human immunodeficiency virus 1
Q7K/L331I/L631I mutant enzyme is highly resistant to autolysis, while retaining the physical properties, specificity, and susceptibility to inhibition of the wild-type enzyme Human immunodeficiency virus 1

Inhibitors

Inhibitors Comment Organism Structure
U-71017 i.e. Poa-His-Cha-PSI[CH(OH)CH2]Val-Ile-Amp Human immunodeficiency virus 1
U-71038 i.e. Boc-Pro-Phe-Nalpha-MeHis-Leu-PSI[CH(OH)CH2]Val-Ile-Amp Human immunodeficiency virus 1
U-75875 i.e. Noa-His-Cha-PSI[CH(OH)CH2]Val-Ile-Amp Human immunodeficiency virus 1
U-79213 i.e. Poa-His-Cha-PSI[CH(OH)CH2]Val-Ile-Amp Human immunodeficiency virus 1
U-81749E i.e. Tba-Cha-PSI[CH(OH)CH2]Val-Ile-Amp Human immunodeficiency virus 1

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.125
-
 REYDQILIKVS pH 5.5, 30°C, mutant enzyme Q7K/L33I/L63I Human immunodeficiency virus 1
0.135
-
 REYDQILIKVS pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
0.143
-
 REYDQIIIEVS pH 5.5, 30°C, mutant enzyme Q7K/L33I/L63I Human immunodeficiency virus 1
0.152
-
 REYDQIIIEVS pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
0.202
-
 REYDQILIEVS pH 5.5, 30°C, mutant enzyme Q7K/L33I/L63I Human immunodeficiency virus 1
0.215
-
 REYDQILIEVS pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
0.71
-
 DTVIEEMS pH 5.5, 30°C, mutant enzyme Q7K/L33I/L63I Human immunodeficiency virus 1
0.81
-
 DTVIEEMS pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
0.87
-
 DTVVEEMS pH 5.5, 30°C, mutant enzyme Q7K/L33I/L63I Human immunodeficiency virus 1
0.95
-
 DTVVEEMS pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
1.02
-
 DTVLEEMS pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
1.11
-
 DTVLEEMS pH 5.5, 30°C, mutant enzyme Q7K/L33I/L63I Human immunodeficiency virus 1
2
-
 VSQNYPIV pH 5.5, 30°C, wild-type enzyme and mutant enzyme Q7K/L33I/L63I Human immunodeficiency virus 1
2.2
-
 PQITLWQRP pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1

Localization

Localization Comment Organism GeneOntology No. Textmining
inclusion body inclusion bodies from Escherichia coli harboring recombinant HIV-1 Human immunodeficiency virus 1 16234
-

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
DTVIEEMS + H2O
-
 Human immunodeficiency virus 1 DTVI + EEMS
-
 ?
DTVLEEMS + H2O
-
 Human immunodeficiency virus 1 DTVL + EEMS
-
 ?
DTVVEEMS + H2O
-
 Human immunodeficiency virus 1 DTVV + EEMS
-
 ?
DTVVEKMS + H2O
-
 Human immunodeficiency virus 1 DTVV + EKMS
-
 ?
PQITLWKRP + H2O
-
 Human immunodeficiency virus 1 PQITL + WKRP
-
 ?
PQITLWQRP + H2O
-
 Human immunodeficiency virus 1 PQITL + WQRP
-
 ?
REYDQIIIEVS + H2O
-
 Human immunodeficiency virus 1 REYDQII + IEVS
-
 ?
REYDQILIEVS + H2O
-
 Human immunodeficiency virus 1 REYDQIL + IEVS
-
 ?
REYDQILIKVS + H2O
-
 Human immunodeficiency virus 1 REYDQIL + IKVS
-
 ?
VSQNYPIV + H2O
-
 Human immunodeficiency virus 1 VSQNY + PIV
-
 ?

Subunits

Subunits Comment Organism
More the HIV-1 protease dimer is in equilibrium with monomeric, disordered species which serves as the substrate for autolysis Human immunodeficiency virus 1

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.000833
-
 REYDQILIKVS pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
0.001
-
 REYDQILIKVS pH 5.5, 30°C, mutant enzyme Q7K/L33I/L63I Human immunodeficiency virus 1
0.025
-
 REYDQIIIEVS pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
0.0267
-
 REYDQIIIEVS pH 5.5, 30°C, mutant enzyme Q7K/L33I/L63I Human immunodeficiency virus 1
0.04
-
 DTVIEEMS pH 5.5, 30°C, mutant enzyme Q7K/L33I/L63I Human immunodeficiency virus 1
0.0483
-
 DTVIEEMS pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
0.0967
-
 PQITLWQRP pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
0.103
-
 PQITLWQRP pH 5.5, 30°C, mutant enzyme Q7K/L33I/L63I Human immunodeficiency virus 1
0.125
-
 DTVVEEMS pH 5.5, 30°C, mutant enzyme Q7K/L33I/L63I Human immunodeficiency virus 1
0.13
-
 DTVVEEMS pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
2.85
-
 REYDQILIEVS pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
3.07
-
 REYDQILIEVS pH 5.5, 30°C, mutant enzyme Q7K/L33I/L63I Human immunodeficiency virus 1
4.02
-
 VSQNYPIV pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
4.32
-
 VSQNYPIV pH 5.5, 30°C, mutant enzyme Q7K/L33I/L63I Human immunodeficiency virus 1
4.35
-
 DTVLEEMS pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
4.58
-
 DTVLEEMS pH 5.5, 30°C, mutant enzyme Q7K/L33I/L63I Human immunodeficiency virus 1

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000007
-
 U-71017 pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
0.000009
-
 U-79213 pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
0.000011
-
 U-71038 pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1
0.00006
-
 U-81749E pH 5.5, 30°C, wild-type enzyme Human immunodeficiency virus 1