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Literature summary for 3.5.2.6 extracted from

  • Horsfall, L.E.; Garau, G.; Lienard, B.M.; Dideberg, O.; Schofield, C.J.; Frere, J.M.; Galleni, M.
    Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila (2007), Antimicrob. Agents Chemother., 51, 2136-2142.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
pyridine-2,3-dicarboxylic acid 30% increase of activity at 0.1 mM Aeromonas hydrophila
pyridine-2,5-dicarboxylic acid 14% increase of activity at 0.1 mM Aeromonas hydrophila
pyridine-3,4-dicarboxylic acid 16% increase of activity at 0.1 mM Aeromonas hydrophila

Crystallization (Commentary)

Crystallization (Comment) Organism
hanging drop vapour diffusion method with 30% (w/v) polyethylene glycol 8000, 0.6 M ammonium sulfate, and 100 mM Na-citrate, pH 6.5 Aeromonas hydrophila

Protein Variants

Protein Variants Comment Organism
N116H/N220G mutant enzyme with a broader specificity than wild type CphA Aeromonas hydrophila

Inhibitors

Inhibitors Comment Organism Structure
2-picolinic acid competitive inhibitor, 8% residual activity at 0.1 mM Aeromonas hydrophila
pyridine-2,4-dicarboxylic acid competitive inhibitor, 38% residual activity at 0.1 mM Aeromonas hydrophila
pyridine-2,6-dicarboxylic acid 12% residual activity at 0.1 mM Aeromonas hydrophila

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.063
-
Imipenem wild type enzyme, at pH 9.0 Aeromonas hydrophila
0.083
-
Imipenem wild type enzyme, at pH 8.0 Aeromonas hydrophila
0.12
-
Imipenem wild type enzyme, at pH 7.0 Aeromonas hydrophila

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+ catalytically active with one zinc Aeromonas hydrophila

Organism

Organism UniProt Comment Textmining
Aeromonas hydrophila P26918
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ampicillin + H2O
-
Aeromonas hydrophila (2R,4S)-2-[(R)-[[(2R)-2-amino-2-phenylacetyl]amino](carboxy)methyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid
-
?
imipenem + H2O
-
Aeromonas hydrophila (5R)-5-[(1S,2R)-1-carboxy-2-hydroxypropyl]-3-({2-[(iminomethyl)amino]ethyl}sulfanyl)-4,5-dihydro-1H-pyrrole-2-carboxylic acid
-
?

Synonyms

Synonyms Comment Organism
CphA
-
Aeromonas hydrophila
metallo-beta-lactamase
-
Aeromonas hydrophila

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
49
-
Imipenem wild type enzyme, at pH 9.0 Aeromonas hydrophila
140
-
Imipenem wild type enzyme, at pH 8.0 Aeromonas hydrophila
210
-
Imipenem wild type enzyme, at pH 7.0 Aeromonas hydrophila

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0045
-
pyridine-2,4-dicarboxylic acid wild type enzyme, in 20 mM sodium cacodylate buffer, pH 6.5 Aeromonas hydrophila
0.0057
-
2-picolinic acid wild type enzyme, in 20 mM sodium cacodylate buffer, pH 6.5 Aeromonas hydrophila
0.013
-
2-picolinic acid mutant enzyme N116H/N220G, in 20 mM sodium cacodylate buffer, pH 6.5 Aeromonas hydrophila
0.028
-
pyridine-2,4-dicarboxylic acid mutant enzyme N116H/N220G, in 20 mM sodium cacodylate buffer, pH 6.5 Aeromonas hydrophila