BRENDA - Enzyme Database show

Biomimetic design results in a potent allosteric inhibitor of dihydrodipicolinate synthase from Campylobacter jejuni

Skovpen, Y.V.; Conly, C.J.; Sanders, D.A.; Palmer, D.R.; J. Am. Chem. Soc. 138, 2014-2020 (2016)

Data extracted from this reference:

Application
EC Number
Application
Commentary
Organism
4.3.3.7
drug development
the enzyme is a target for antibiotics
Campylobacter jejuni
4.3.3.7
pharmacology
the enzyme is a target for antibiotics
Campylobacter jejuni
Crystallization (Commentary)
EC Number
Crystallization
Organism
4.3.3.7
crystals are grown in a solution of 0.28 M sodium acetate, 30% PEG 4000, 0.1 M TRIS pH 8.5 using the hanging drop vapor diffusion method
Campylobacter jejuni
Engineering
EC Number
Amino acid exchange
Commentary
Organism
4.3.3.7
Y110F
the mutant enzyme is resistant to lysine inhibition
Campylobacter jejuni
Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
4.3.3.7
bislysine
bislysine is a mixed partial inhibitor with respect to the first substrate, pyruvate, and a noncompetitive partial inhibitor with respect to L-aspartate-4-semialdehyde
Campylobacter jejuni
4.3.3.7
L-lysine
allosteric inhibitor
Campylobacter jejuni
Natural Substrates/ Products (Substrates)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
4.3.3.7
pyruvate + L-aspartate-4-semialdehyde
Campylobacter jejuni
-
(2S,4S)-4-hydroxy-2,3,4,5-tetrahydrodipicolinate + H2O
-
-
?
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
4.3.3.7
Campylobacter jejuni
-
-
-
Purification (Commentary)
EC Number
Commentary
Organism
4.3.3.7
-
Campylobacter jejuni
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
4.3.3.7
pyruvate + L-aspartate-4-semialdehyde
-
748035
Campylobacter jejuni
(2S,4S)-4-hydroxy-2,3,4,5-tetrahydrodipicolinate + H2O
-
-
-
?
Ki Value [mM]
EC Number
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
4.3.3.7
0.0002
-
bislysine
pH 8.0, 25C
Campylobacter jejuni
Application (protein specific)
EC Number
Application
Commentary
Organism
4.3.3.7
drug development
the enzyme is a target for antibiotics
Campylobacter jejuni
4.3.3.7
pharmacology
the enzyme is a target for antibiotics
Campylobacter jejuni
Crystallization (Commentary) (protein specific)
EC Number
Crystallization
Organism
4.3.3.7
crystals are grown in a solution of 0.28 M sodium acetate, 30% PEG 4000, 0.1 M TRIS pH 8.5 using the hanging drop vapor diffusion method
Campylobacter jejuni
Engineering (protein specific)
EC Number
Amino acid exchange
Commentary
Organism
4.3.3.7
Y110F
the mutant enzyme is resistant to lysine inhibition
Campylobacter jejuni
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
4.3.3.7
bislysine
bislysine is a mixed partial inhibitor with respect to the first substrate, pyruvate, and a noncompetitive partial inhibitor with respect to L-aspartate-4-semialdehyde
Campylobacter jejuni
4.3.3.7
L-lysine
allosteric inhibitor
Campylobacter jejuni
Ki Value [mM] (protein specific)
EC Number
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
4.3.3.7
0.0002
-
bislysine
pH 8.0, 25C
Campylobacter jejuni
Natural Substrates/ Products (Substrates) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
4.3.3.7
pyruvate + L-aspartate-4-semialdehyde
Campylobacter jejuni
-
(2S,4S)-4-hydroxy-2,3,4,5-tetrahydrodipicolinate + H2O
-
-
?
Purification (Commentary) (protein specific)
EC Number
Commentary
Organism
4.3.3.7
-
Campylobacter jejuni
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
4.3.3.7
pyruvate + L-aspartate-4-semialdehyde
-
748035
Campylobacter jejuni
(2S,4S)-4-hydroxy-2,3,4,5-tetrahydrodipicolinate + H2O
-
-
-
?