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Literature summary for 4.1.2.13 extracted from

  • Dax, C.; Duffieux, F.; Chabot, N.; Coincon, M.; Sygusch, J.; Michels, P.A.; Blonski, C.
    Selective irreversible inhibition of fructose 1,6-bisphosphate aldolase from Trypanosoma brucei (2006), J. Med. Chem., 49, 1499-1502.
    View publication on PubMed

Protein Variants

Protein Variants Comment Organism
K156M identical to wild type enzyme Trypanosoma brucei
K16M not inhibited by 5-formyl-6-hydroxynaphthalen-2-yl dihydrogen phosphate Trypanosoma brucei
K239M identical to wild type enzyme Trypanosoma brucei

Inhibitors

Inhibitors Comment Organism Structure
5-formyl-6-hydroxynaphthalen-2-yl dihydrogen phosphate 1 mM, 15 min incubation time, 80% residual activity Oryctolagus cuniculus
5-formyl-6-hydroxynaphthalen-2-yl dihydrogen phosphate 5 mM, 15 min incubation time, no residual activity Trypanosoma brucei
hexitol-1,6-bisphosphate strong competitive inhibitor Trypanosoma brucei
naphthalene-2,6-bisphosphate strong competitive inhibitor Trypanosoma brucei

Organism

Organism UniProt Comment Textmining
Oryctolagus cuniculus
-
-
-
Trypanosoma brucei
-
-
-

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
-
?
D-fructose 1,6-bisphosphate
-
Trypanosoma brucei glycerone phosphate + D-glyceraldehyde 3-phosphate
-
?
dihydroxyacetone phosphate
-
Oryctolagus cuniculus ?
-
?
dihydroxyacetone phosphate
-
Trypanosoma brucei ?
-
?

Synonyms

Synonyms Comment Organism
class I fructose 1,6-bisphosphate aldolase
-
Oryctolagus cuniculus
class I fructose 1,6-bisphosphate aldolase
-
Trypanosoma brucei

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0233
-
5-formyl-6-hydroxynaphthalen-2-yl dihydrogen phosphate
-
Trypanosoma brucei
0.028
-
naphthalene-2,6-bisphosphate
-
Trypanosoma brucei
0.045
-
hexitol-1,6-bisphosphate
-
Trypanosoma brucei

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.02
-
15 min incubation time Trypanosoma brucei 5-formyl-6-hydroxynaphthalen-2-yl dihydrogen phosphate