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Literature summary for 3.4.23.B8 extracted from

  • Ding, Y.S.; Rich, D.H.; Ikeda, R.A.
    Substrates and inhibitors of human T-cell leukemia virus type I protease (1998), Biochemistry, 37, 17514-17518.
    View publication on PubMed
Search for more literature for 3.4.23.B8

Application

Application Comment Organism
medicine currently employed HIV protease inhibitors can not be used to treat HTLV infections Human T-cell leukemia virus type I

Inhibitors

Inhibitors Comment Organism Structure
Ac-Ser-Leu-Asn-Phe-CH(OH)CH2NH-Pro-Ile-Val-methyl ester i.e. JG-365 Human T-cell leukemia virus type I
CS-I-51
-
 Human T-cell leukemia virus type I
isobutyl oxycarbonyl-Lys--Val-Val-(3S,4S)-statine-Ala-isoamylamine i.e. CS-I-27 Human T-cell leukemia virus type I
isovaleryl-Lys-Val-(3S,4S)-statine-Ala-isoamylamine i.e. CS-I-25 Human T-cell leukemia virus type I
isovaleryl-Val-Nle-(3S,4S)-statine-Ala-isoamylamine i.e. CS-I-22 Human T-cell leukemia virus type I
isovaleryl-Val-Val-(3S,4S)-statine-Ala-Lys-methyl ester i.e. CS-I-52 Human T-cell leukemia virus type I
isovaleryl-Val-Val-(3S,4S)-statine-Lys-isoamylamine i.e. CS-I-51 Human T-cell leukemia virus type I
MES13-099
-
 Human T-cell leukemia virus type I
additional information currently employed HIV protease inhibitors can not be used to treat HTLV infections Human T-cell leukemia virus type I

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.061
-
 APQVLNphVMHPL pH 5.3, 37°C Human T-cell leukemia virus type I
0.31
-
 KTKVLVVQPK pH 5.3, 37°C Human T-cell leukemia virus type I
0.47
-
 APQVLPVMHPHG
-
 Human T-cell leukemia virus type I

Organism

Organism UniProt Comment Textmining
Human T-cell leukemia virus type I
-
-
-

Purification (Commentary)

Purification (Comment) Organism
HTLV1-protease and HTLV-I protease fused to the 27 amino acid pET10-b histidine tag Human T-cell leukemia virus type I

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
APQVLF(NO2)VMHPL + H2O
-
 Human T-cell leukemia virus type I ?
-
 ?
APQVLNphVMHPL + H2O
-
 Human T-cell leukemia virus type I ?
-
 ?
APQVLPVMHPHG + H2O
-
 Human T-cell leukemia virus type I APQVL + PVMHPHG
-
 ?
KTKVLVVQPK + H2O
-
 Human T-cell leukemia virus type I KTKVL + VVQPK
-
 ?
additional information the substrate binding site of HTLV-I protease is different from the substrate binding sites of pspsin and HIV-1 protease Human T-cell leukemia virus type I ?
-
 ?
YVEPTAPQVLPVMHP + H2O
-
 Human T-cell leukemia virus type I ?
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.006
-
 KTKVLVVQPK pH 5.3, 37°C Human T-cell leukemia virus type I
0.184
-
 YVEPTAPQVLPVMHP pH 5.3, 37°C Human T-cell leukemia virus type I
2.16
-
 APQVLF(NO2)VMHPL pH 5.3, 37°C Human T-cell leukemia virus type I

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000006
-
 Ac-Ser-Leu-Asn-Phe-CH(OH)CH2NH-Pro-Ile-Val-methyl ester pH 5.3, 37°C Human T-cell leukemia virus type I
0.0000072
-
 isovaleryl-Lys-Val-(3S,4S)-statine-Ala-isoamylamine pH 5.3, 37°C Human T-cell leukemia virus type I
0.000138
-
 isovaleryl-Val-Nle-(3S,4S)-statine-Ala-isoamylamine pH 5.3, 37°C Human T-cell leukemia virus type I
0.000142
-
 isobutyl oxycarbonyl-Lys--Val-Val-(3S,4S)-statine-Ala-isoamylamine pH 5.3, 37°C Human T-cell leukemia virus type I
0.000466
-
 CS-I-51 pH 5.3, 37°C Human T-cell leukemia virus type I
0.00243
-
 MES13-099 pH 5.3, 37°C Human T-cell leukemia virus type I
0.0072
-
 isovaleryl-Val-Val-(3S,4S)-statine-Ala-Lys-methyl ester pH 5.3, 37°C Human T-cell leukemia virus type I