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Literature summary for 3.4.23.B10 extracted from

  • Wu, J.; Adomat, J.M.; Ridky, T.W.; Louis, J.M.; Leis, J.; Harrison, R.W.; Weber, I.T.
    Structural Basis for Specificity of Retroviral Proteases (1998), Biochemistry, 37, 4518-4526.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
mutant enzyme S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N crystallized with an inhibitor of HIV-1 protease, Arg-Val-Leu-(reduced bond)-Phe-Glu-Ala-Nle-NH2. A polyhistidine sequence is added to the amino terminus of the enzyme to allow for efficient and rapid purification Rous sarcoma virus

Protein Variants

Protein Variants Comment Organism
S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N the murtant enzyme has 9 structurally equivalent residues from HIV-1 protease. Unlike the wild-type enzyme, the mutant enzyme hydrolyzes peptides representing the HIV-1 protease polyprotein cleavage sites Rous sarcoma virus

Inhibitors

Inhibitors Comment Organism Structure
Arg-Val-Leu-r-Phe-Glu-Ala-Nle-NH2 mutant enzyme S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N Rous sarcoma virus
additional information Arg-Val-Leu-(reduced bond)-Phe-Glu-Ale-Nle-NH2 inhibits mutant enzyme S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N Rous sarcoma virus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.037
-
TFQAYPLREA reaction with mutant enzyme S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N Rous sarcoma virus
0.244
-
KARVLAEAMS reaction with mutant enzyme S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N Rous sarcoma virus
0.538
-
VSFNFPQITKK reaction with mutant enzyme S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N Rous sarcoma virus

Organism

Organism UniProt Comment Textmining
Rous sarcoma virus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
KARVLAEAMS + H2O reaction with mutant enzyme S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N Rous sarcoma virus KARVL + AEAMS
-
?
TFQAYPLREA + H2O reaction with mutant enzyme S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N Rous sarcoma virus TFQAY + PLREA
-
?
TLNFPISPKK + H2O slow cleavage with mutant enzyme S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N Rous sarcoma virus TLNF + PISPKK
-
?
VSFNFPQITKK + H2O reaction with mutant enzyme S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N Rous sarcoma virus VSFNF + PQITKK
-
?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.167
-
KARVLAEAMS reaction with mutant enzyme S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N Rous sarcoma virus
0.183
-
TFQAYPLREA reaction with mutant enzyme S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N Rous sarcoma virus
0.25
-
VSFNFPQITKK reaction with mutant enzyme S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N Rous sarcoma virus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information Ki-value for Arg-Val-Leu-(reduced bond)-Phe-Glu-Ale-Nle-NH2 is 0.00002 mM, mutant enzyme S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N Rous sarcoma virus
0.000487
-
Arg-Val-Leu-r-Phe-Glu-Ala-Nle-NH2 mutant enzyme S38T/I42D/I44V/M73V/A100L/L104T/R105P/G106V/S107N Rous sarcoma virus