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Literature summary for 3.4.23.B8 extracted from

  • Naka, H.; Teruya, K.; Bang, J.K.; Aimoto, S.; Tatsumi, T.; Konno, H.; Nosaka, K.; Akaji, K.
    Evaluations of substrate specificity and inhibition at PR/p3 cleavage site of HTLV-1 protease (2006), Bioorg. Med. Chem. Lett., 16, 3761-3764.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
H-Ile- NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-NHCH2C6H5I
-
Human T-cell leukemia virus type I
H-Pro-Pro-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-NHCH2C6H5I
-
Human T-cell leukemia virus type I
H-Pro-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-Ile-NHCH2C6H5I
-
Human T-cell leukemia virus type I
H-Pro-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-NHCH2C6H5I
-
Human T-cell leukemia virus type I
H-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-Ile-NHCH2C6H5I
-
Human T-cell leukemia virus type I
H-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-NHCH2C6H5I
-
Human T-cell leukemia virus type I
additional information results show that a tetrapeptide sequence is necessary to achieve potent inhibition Human T-cell leukemia virus type I

Organism

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
KGPPVICPIQA + H2O the preferred amino acids at the P1 position, except for Leu, are hydrophobic Phe and sulfur-containing amino acids (Met and Cys). Substrates which contain a charged side chain at the P1 position are not cleaved Human T-cell leukemia virus type I KGPPVIC + PIQA
-
?
KGPPVIFPIQA + H2O the preferred amino acids at the P1 position, except for Leu, are hydrophobic Phe and sulfur-containing amino acids (Met and Cys). Substrates which contain a charged side chain at the P1 position are not cleaved Human T-cell leukemia virus type I KGPPVIF + PIQA
-
?
KGPPVILPIQA + H2O Pro residue at the P1' position is the preferred amino acid for hydrolysis, and no replacement at the P1' position seems to be tolerated Human T-cell leukemia virus type I KGPPVIL + PIQA
-
?
KGPPVILPIQAP + H2O 12-residue standard peptide, 100% cleavage Human T-cell leukemia virus type I ?
-
?
KGPPVIMPIQA + H2O the preferred amino acids at the P1 position, except for Leu, are hydrophobic Phe and sulfur-containing amino acids (Met and Cys). Substrates which contain a charged side chain at the P1 position are not cleaved Human T-cell leukemia virus type I KGPPVIM + PIQA
-
?
additional information no cleavage using substrates: VILPIQAP, VILPIQA, VILPIQ, PPVILPI, PVILPI Human T-cell leukemia virus type I ?
-
?
additional information preference for Pro at the P1' position and for Ile at the P2 position. Hydrophobic Phe and Gln residues are acceptable in the P3 position and a Gln residue at the P4 position Human T-cell leukemia virus type I ?
-
?
PPVILPIQ + H2O
-
Human T-cell leukemia virus type I ?
-
?
PPVILPIQA + H2O a 9-residue peptide is cleaved approximately at 85% of the 12-residue standard peptide Human T-cell leukemia virus type I ?
-
?
PPVILPIQAP + H2O
-
Human T-cell leukemia virus type I ?
-
?
PVILPIQ + H2O minimal sequence required for substrate recognition is a 7-residue peptide Human T-cell leukemia virus type I ?
-
?
PVILPIQA + H2O
-
Human T-cell leukemia virus type I ?
-
?
PVILPIQAP + H2O
-
Human T-cell leukemia virus type I ?
-
?

Synonyms

Synonyms Comment Organism
C2A HTLV-1 PR chemically synthesized mutant of HTLV-1 protease Human T-cell leukemia virus type I
HTLV-1 protease
-
Human T-cell leukemia virus type I
HTLV-I protease
-
Human T-cell leukemia virus type I

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Human T-cell leukemia virus type I

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00013
-
-
Human T-cell leukemia virus type I H-Pro-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-Ile-NHCH2C6H5I
0.0024
-
-
Human T-cell leukemia virus type I H-Pro-Pro-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-NHCH2C6H5I
0.0058
-
-
Human T-cell leukemia virus type I H-Pro-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-NHCH2C6H5I
0.0183
-
-
Human T-cell leukemia virus type I H-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-Ile-NHCH2C6H5I
0.0196
-
-
Human T-cell leukemia virus type I H-Val-Ile-NHCH(CH2CH(CH3)2)CH(OH)CH2-Pro-NHCH2C6H5I