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Literature summary for 3.1.1.43 extracted from

  • Lai, L.; Xu, Z.; Zhou, J.; Lee, K.D.; Amidon, G.L.
    Molecular basis of prodrug activation by human valacyclovirase, an alpha-amino acid ester hydrolase (2008), J. Biol. Chem., 283, 9318-9327.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
drug development valacyclovirase is suggested as a prodrug activating enzyme Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
into the vector pET17b for expression in Escherichia coli BL21DE3 and B834DE3 cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
the crystal structures of the native protein, the S122A and D123N mutants, and the native enzyme in complex with L-tyrosine amide are solved at resolutions of 1.75 A, 1.90 A, 1.85 A and 1.90 A, respectively Homo sapiens

Protein Variants

Protein Variants Comment Organism
D123N point mutant Homo sapiens
S122A point mutant Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
valacyclovir + H2O Homo sapiens
-
L-valine + acyclovir
-
?
valganciclovir + H2O Homo sapiens
-
L-valine + ganciclovir
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
using a S strong cation exchange and a phenyl-Sepharose hydrophobic interaction column Homo sapiens

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.6
-
3-amino-3-phenylpropionic acid ethyl ester Homo sapiens
1.8
-
beta-Ala benzyl ester Homo sapiens
35.3
-
L-Trp benzyl ester Homo sapiens
41.4
-
L-Tyr benzyl ester Homo sapiens
75.3
-
L-Phe ethyl ester Homo sapiens
103.7
-
valacyclovir Homo sapiens
156.2
-
L-Met methyl ester Homo sapiens
156.3
-
L-Val benzyl ester Homo sapiens
358.3
-
L-Phe benzyl ester Homo sapiens
484.3
-
L-Ser benzyl ester Homo sapiens
635
-
L-Leu benzyl ester Homo sapiens
849.4
-
L-Gly benzyl ester Homo sapiens
1368
-
L-Ala benzyl ester Homo sapiens
5148
-
L-Pro benzyl ester Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3-amino-3-phenylpropionic acid ethyl ester + H2O
-
Homo sapiens ?
-
?
beta-Ala benzyl ester + H2O
-
Homo sapiens beta-Ala + benzoic acid
-
?
floxuridine + H2O
-
Homo sapiens ?
-
?
gemcitabine + H2O
-
Homo sapiens ?
-
?
Gly benzyl ester + H2O
-
Homo sapiens Gly + benzoic acid
-
?
L-Ala benzyl ester + H2O
-
Homo sapiens L-Ala + benzoic acid
-
?
L-Leu benzyl ester + H2O
-
Homo sapiens L-leu + benzoic acid
-
?
L-Met methyl ester + H2O
-
Homo sapiens ?
-
?
L-Phe benzyl ester + H2O
-
Homo sapiens L-Phe + benzoic acid
-
?
L-Phe ethyl ester + H2O
-
Homo sapiens ?
-
?
L-Pro benzyl ester + H2O
-
Homo sapiens L-Pro + benzoic acid
-
?
L-Ser benzyl ester + H2O
-
Homo sapiens L-Ser + benzoic acid
-
?
L-Trp benzyl ester + H2O
-
Homo sapiens L-Trp + benzoic acid
-
?
L-Tyr benzyl ester + H2O
-
Homo sapiens L-Tyr + benzoic acid
-
?
L-Val benzyl ester + H2O
-
Homo sapiens L-Val + benzoic acid
-
?
valacyclovir + H2O
-
Homo sapiens L-valine + acyclovir
-
?
valganciclovir + H2O
-
Homo sapiens L-valine + ganciclovir
-
?
zidovudine + H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
alpha-amino acid ester esterase
-
Homo sapiens
alpha-amino acid ester hydrolase
-
Homo sapiens
VACVase
-
Homo sapiens
valacyclovirase
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
activity assay Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
activity assay Homo sapiens