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Literature summary for 4.3.3.7 extracted from

  • Boughton, B.A.; Griffin, M.D.; ODonnell, P.A.; Dobson, R.C.; Perugini, M.A.; Gerrard, J.A.; Hutton, C.A.
    Irreversible inhibition of dihydrodipicolinate synthase by 4-oxo-heptenedioic acid analogues (2008), Bioorg. Med. Chem., 16, 9975-9983.
    View publication on PubMed
Search for more literature for 4.3.3.7

Inhibitors

Inhibitors Comment Organism Structure
(2E)-4-oxohept-2-enedioic acid
-
 Escherichia coli
(2E,5E)-4-oxohepta-2,5-dienedioic acid
-
 Escherichia coli
diethyl (2E)-4-oxohept-2-enedioate
-
 Escherichia coli
diethyl (2E,5E)-4-oxohepta-2,5-dienedioate
-
 Escherichia coli
additional information inhibition studies by using 4-oxo-heptenedioic acid analogues, determination of second-order rate constants of inactivation, substrate co-incubation studies show that the inhibitors act at the active-site, interaction analyzed by mass spectrometry, sites of enzyme alkylation determined Escherichia coli

Organism

Organism UniProt Comment Textmining
Escherichia coli P0A6L2
-
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
 substrate protection experiments, inhibition by alkylation the active-site lysine residue (Lys161) and a surface cysteine residue, slower alkylation of other cysteine residues with lower surface accessibility, co-incubation of the enzyme with the inhibitors in the presence of pyruvate protect against active-site alkylation and cysteine residues Escherichia coli

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-aspartate 4-semialdehyde + pyruvate substrate protection and inhibition experiments Escherichia coli dihydrodipicolinate + H2O
-
 ?

Synonyms

Synonyms Comment Organism
DHDPS
-
 Escherichia coli

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.63
-
 (2E,5E)-4-oxohepta-2,5-dienedioic acid more potent than the corresponding mono-ene inhibitors Escherichia coli
4.95
-
 diethyl (2E,5E)-4-oxohepta-2,5-dienedioate best inhibitor Escherichia coli
10.9
-
 diethyl (2E)-4-oxohept-2-enedioate mono-ene inhibitor Escherichia coli
32.4
-
 (2E)-4-oxohept-2-enedioic acid mono-ene inhibitor Escherichia coli