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Literature summary for 4.1.2.13 extracted from

  • Dax, C.; Coincon, M.; Sygusch, J.; Blonski, C.
    Hydroxynaphthaldehyde phosphate derivatives as potent covalent Schiff base inhibitors of fructose-1,6-bisphosphate aldolase (2005), Biochemistry, 44, 5430-5443.
    View publication on PubMed

Protein Variants

Protein Variants Comment Organism
K107M 46fold increase in Ki-value for naphthyl 2,6-bisphosphate, 11.5fold increase in KM-value for D-fructose 1,6-diphosphate. The structure of the enzyme is isomorphous with respect to wild-type enzyme Oryctolagus cuniculus
K146M decrease in rate of complex formation between enzyme and inhibitor 1-hydroxy-2-naphthaldehyde 6-phosphate, but no change in ability to form the complex Oryctolagus cuniculus
S271 mutation decreases by 1 order of magnitude the affinity of 1-hydroxy-2-naphthaldehyde 6-phosphate for the aldolase active site but does not modify its ability to catalyze Schiff base formation Oryctolagus cuniculus

Inhibitors

Inhibitors Comment Organism Structure
1-hydroxy-2-naphthaldehyde 6-phosphate slow-binding Oryctolagus cuniculus
naphthyl 2,6-bisphosphate competitive Oryctolagus cuniculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.013
-
D-fructose 1,6-bisphosphate wild-type enzyme Oryctolagus cuniculus
0.15
-
D-fructose 1,6-bisphosphate mutant enzyme K107M Oryctolagus cuniculus

Organism

Organism UniProt Comment Textmining
Oryctolagus cuniculus P00883
-
-

Source Tissue

Source Tissue Comment Organism Textmining
muscle
-
Oryctolagus cuniculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-fructose 1,6-bisphosphate
-
Oryctolagus cuniculus glycerone phosphate + D-glyceraldehyde 3-phosphate
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00028
-
naphthyl 2,6-bisphosphate wild-type enzyme Oryctolagus cuniculus
0.013
-
naphthyl 2,6-bisphosphate mutant enzyme K107M Oryctolagus cuniculus
0.125
-
1-hydroxy-2-naphthaldehyde 6-phosphate wild-type enzyme Oryctolagus cuniculus