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Literature summary extracted from

  • Toezser, J.; Blaha, I.; Copeland, T.D.; Wondrak, E.M.; Oroszlan, S.
    Comparison of the HIV-1 and HIV-2 proteinases using oligopeptide substrates representing cleavage sites in Gag and Gag-Pol polyproteins (1991), FEBS Lett., 281, 77-80.
    View publication on PubMed

Application

EC Number Application Comment Organism
3.4.23.47 medicine potential target for chemotherapy of virus infection and associated diseases, essential for maturation of infectious virions, development of drugs against the protease should be effective against HIV-2 Human immunodeficiency virus 2

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.23.47 CTLNF-PSI[CH2-NH]-PISP competitive inhibition Human immunodeficiency virus 2
3.4.23.47 VSFNF-PSI[CH2-NH]-PQITL competitive inhibition Human immunodeficiency virus 2

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.23.47 0.005
-
 IRKILFLDG pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.02
-
 MSLNLPVAKV pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.03
-
 KARVL-AEAMS pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.06
-
 CTLNFPISP pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.07
-
 IPFAA-AQQRK pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.07
-
 RGLAAPQFSL pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.08
-
 KARLM AEALK pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.08
-
 L-threonyl-L-alanyl-L-threonyl-L-isoleucyl-L-methionyl-L-methionyl-L-glutaminyl-L-arginylglycyl-L-asparagine pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.18
-
 VSQNYPIVQ pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.3
-
 RPQNFLQSRP pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.42
-
 DKELYPLTSL pH 5.6, 37°C Human immunodeficiency virus 2

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.4.23.47 GAG precursor protein of HIV-2 + H2O Human immunodeficiency virus 2
-
 ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.4.23.47 Human immunodeficiency virus 2
-
 human immunodeficiency virus type 2
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.23.47 AETFYVDGAA + H2O
-
 Human immunodeficiency virus 2 AETF + YVDGAA
-
 ?
3.4.23.47 CTLNF + PISP + H2O oligopeptide representing cleavage sites in HIV-1 Gag and Gag-Pol polyproteins, location of cleavage in PR/RT Human immunodeficiency virus 2 CTLNF + PISP
-
 ?
3.4.23.47 CTLNFPISP + H2O
-
 Human immunodeficiency virus 2 CTLNF + PISP
-
 ?
3.4.23.47 DKELYPLTSL + H2O oligopeptide representing cleavage sites in HIV-1 Gag and Gag-Pol polyproteins, location of cleavage in p6 Human immunodeficiency virus 2 DKELY + PLTSL
-
 ?
3.4.23.47 EKGGNYPVQHV + H2O oligopeptide representing cleavage sites in HIV-1 Gag and Gag-Pol polyproteins, location of cleavage in MA/CA Human immunodeficiency virus 2 EKGGNY + PVQHV
-
 ?
3.4.23.47 GAG precursor protein F16 of HIV-1 + H2O chemically synthesized aspartyl protease enzyme catalyzes specific processing of the recombinant 43-kDa protein Human immunodeficiency virus 2 ?
-
 ?
3.4.23.47 GAG precursor protein of HIV-2 + H2O
-
 Human immunodeficiency virus 2 ?
-
 ?
3.4.23.47 IPFAAAQQRK + H2O oligopeptide representing cleavage sites in HIV-1 Gag and Gag-Pol polyproteins, location of cleavage in X/NC Human immunodeficiency virus 2 IPFAA + AQQRK
-
 ?
3.4.23.47 IRKILFLDG + H2O oligopeptide representing cleavage sites in HIV-1 Gag and Gag-Pol polyproteins, location of cleavage in RT/IN Human immunodeficiency virus 2 IRKIL + FLDG
-
 ?
3.4.23.47 KARLMAEALK + H2O oligopeptide representing cleavage sites in HIV-1 Gag and Gag-Pol polyproteins, location of cleavage in MA/CA Human immunodeficiency virus 2 KARLM + AEALK
-
 ?
3.4.23.47 KARVLAEAMS + H2O oligopeptide representing cleavage sites in HIV-1 Gag and Gag-Pol polyproteins, location of cleavage CA/X Human immunodeficiency virus 2 KARVL + AEAMS
-
 ?
3.4.23.47 KPRNFPVAQV + H2O oligopeptide representing cleavage sites in HIV-1 Gag and Gag-Pol polyproteins, location of cleavage in NC/p6 Human immunodeficiency virus 2 KPRNF + PVAQV
-
 ?
3.4.23.47 additional information oligopeptide III VLAEAM.SQVTN, oligopeptide V TERQAN.FLGKI, oligopeptide VII ESFRSG.VETTT and oligopeptide XVI DRQAG.FLGLG are not hydrolyzed, oligopeptide IX VSFNF PQITL and oligopeptide XXI IRQVL FLEKI Km less than 0.01 mM Human immunodeficiency virus 2 ?
-
 ?
3.4.23.47 MSLNLPVAKV + H2O oligopeptide representing cleavage sites in HIV-1 Gag and Gag-Pol polyproteins, location of cleavage in TF/PR Human immunodeficiency virus 2 MSLNL + PVAKV
-
 ?
3.4.23.47 RGLAAPQFSL + H2O oligopeptide representing cleavage sites in HIV-1 Gag and Gag-Pol polyproteins, location of cleavage in TF/PR Human immunodeficiency virus 2 RGLAA + PQFSL
-
 ?
3.4.23.47 RPQNFLQSRP + H2O oligopeptide representing cleavage sites in HIV-1 Gag and Gag-Pol polyproteins, location of cleavage NC/p6 Human immunodeficiency virus 2 ?
-
 ?
3.4.23.47 TATIMMQRGN + H2O oligopeptide representing cleavage sites in HIV-1 Gag and Gag-Pol polyproteins, location of cleavage X/NC Human immunodeficiency virus 2 TATIM + MQRGN
-
 ?
3.4.23.47 VSQNYPIVQ + H2O oligopeptide representing cleavage sites in HIV-1 Gag and Gag-Pol polyproteins, location of cleavage MA/CA Human immunodeficiency virus 2 ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.23.47 PR
-
 Human immunodeficiency virus 2
3.4.23.47 retroviral proteinase
-
 Human immunodeficiency virus 2

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.4.23.47 0.000025
-
 DKELYPLTSL pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.00005
-
 RPQNFLQSRP pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.0001
-
 CTLNFPISP pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.000183
-
 KPRNFPVAQV pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.000217
-
 IPFAA-AQQRK pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.00025
-
 KARVL-AEAMS pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.000267
-
 AETFYVDGAA pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.000333
-
 IRKILFLDG pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.000333
-
 KARLM AEALK pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.000333
-
 MSLNLPVAKV pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.00055
-
 EKGGNYPVQHV pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.000717
-
 RGLAAPQFSL pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.000967
-
 L-threonyl-L-alanyl-L-threonyl-L-isoleucyl-L-methionyl-L-methionyl-L-glutaminyl-L-arginylglycyl-L-asparagine pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.00172
-
 VSQNYPIVQ pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.00283
-
 AETFYVDGAA pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.00917
-
 EKGGNYPVQHV pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.0117
-
 KPRNFPVAQV pH 5.6, 37°C Human immunodeficiency virus 2

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.23.47 0.000025
-
 VSFNF-PSI[CH2-NH]-PQITL pH 5.6, 37°C Human immunodeficiency virus 2
3.4.23.47 0.0006
-
 CTLNF-PSI[CH2-NH]-PISP pH 5.6, 37°C Human immunodeficiency virus 2