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Literature summary for 4.2.1.24 extracted from

  • Heinemann, I.U.; Schulz, C.; Schubert, W.D.; Heinz, D.W.; Wang, Y.G.; Kobayashi, Y.; Awa, Y.; Wachi, M.; Jahn, D.; Jahn, M.
    Structure of the heme biosynthetic Pseudomonas aeruginosa porphobilinogen synthase in complex with the antibiotic alaremycin (2010), Antimicrob. Agents Chemother., 54, 267-272.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli as a His-tagged fusion protein Pseudomonas aeruginosa

Crystallization (Commentary)

Crystallization (Comment) Organism
porphobilinogen synthase is cocrystallized with the alaremycin Pseudomonas aeruginosa

Inhibitors

Inhibitors Comment Organism Structure
alaremycin porphobilinogen synthase is cocrystallized with the alaremycin. At 1.75 A resolution, the crystal structure reveals that the antibiotic efficiently blocks the active site of porphobilinogen synthase. The antibiotic binds as a reduced derivative of 5-acetamido-4-oxo-5-hexenoic acid. The corresponding methyl group is not coordinated by any amino acid residues of the active site, excluding its functional relevance for alaremycin inhibition. Alaremycin is covalently bound by the catalytically important active-site lysine residue 260 and is tightly coordinated by several active-site amino acids Pseudomonas aeruginosa

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00032
-
5-aminolevulinic acid
-
Pseudomonas aeruginosa

Organism

Organism UniProt Comment Textmining
Pseudomonas aeruginosa Q59643
-
-

Purification (Commentary)

Purification (Comment) Organism
using affinity chromatography and anion-exchange chromatography Pseudomonas aeruginosa

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5-aminolevulinic acid + 5-aminolevulinic acid
-
Pseudomonas aeruginosa porphobilinogen + 2 H2O
-
?

Synonyms

Synonyms Comment Organism
Porphobilinogen synthase
-
Pseudomonas aeruginosa

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
16.1
-
5-aminolevulinic acid
-
Pseudomonas aeruginosa

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.33
-
alaremycin
-
Pseudomonas aeruginosa

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.33
-
-
Pseudomonas aeruginosa alaremycin

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
50300
-
5-aminolevulinic acid
-
Pseudomonas aeruginosa