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Literature summary for 1.1.1.49 extracted from

  • Cordeiro, A.T.; Thiemann, O.H.; Michels, P.A.
    Inhibition of Trypanosoma brucei glucose-6-phosphate dehydrogenase by human steroids and their effects on the viability of cultured parasites (2009), Bioorg. Med. Chem., 17, 2483-2489.
    View publication on PubMed

Application

Application Comment Organism
drug development Trypanosoma brucei G6PDH is a valid drug target for human steroids. Inhibition of G6PDH by dehydroepiandrosterone derivatives may lead to the development of a new class of anti-trypanosomatid compounds Trypanosoma brucei

Cloned(Commentary)

Cloned (Comment) Organism
N-terminally His-tagged recombinant G6PDH expressed in Escherichia coli BL21 transformed with recombinant pET28 plasmid Trypanosoma brucei
N-terminally His-tagged recombinant G6PDH expressed in Escherichia coli BL21 transformed with recombinant pET28 plasmid Leishmania mexicana

Inhibitors

Inhibitors Comment Organism Structure
dehydroepiandrosterone uncompetitively inhibits bloodstream form cells Trypanosoma brucei
epiandrosterone uncompetitively inhibits bloodstream form cells Trypanosoma brucei
additional information is not inhibited by dehydroepiandrosterone and epiandrosterone Leishmania mexicana
RNAi mediates reduction of the G6PDH level in bloodstream form cells Trypanosoma brucei

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0094
-
NADP+
-
Trypanosoma brucei
0.0121
-
NADP+
-
Leishmania mexicana
0.0578
-
D-glucose 6-phosphate
-
Trypanosoma brucei
0.0745
-
D-glucose 6-phosphate
-
Leishmania mexicana

Organism

Organism UniProt Comment Textmining
Leishmania mexicana
-
-
-
Trypanosoma brucei
-
427 strain
-
Trypanosoma brucei 427
-
427 strain
-

Purification (Commentary)

Purification (Comment) Organism
to homogeneity by a single nickel affinity chromatographic step Trypanosoma brucei
to homogeneity by a single nickel affinity chromatographic step Leishmania mexicana

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-glucose 6-phosphate + NADP+
-
Trypanosoma brucei D-glucono-1,5-lactone 6-phosphate + NADPH + H+
-
?
D-glucose 6-phosphate + NADP+
-
Leishmania mexicana D-glucono-1,5-lactone 6-phosphate + NADPH + H+
-
?
D-glucose 6-phosphate + NADP+
-
Trypanosoma brucei 427 D-glucono-1,5-lactone 6-phosphate + NADPH + H+
-
?

Synonyms

Synonyms Comment Organism
G6PDH
-
Trypanosoma brucei
G6PDH
-
Leishmania mexicana

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
16.4
-
D-glucose 6-phosphate
-
Trypanosoma brucei
22.2
-
D-glucose 6-phosphate
-
Leishmania mexicana

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00046
-
epiandrosterone in the presence of NADP+ Trypanosoma brucei
0.00049
-
epiandrosterone in the presence of D-glucose 6-phosphate Trypanosoma brucei
0.0011
-
dehydroepiandrosterone in the presence of NADP+ Trypanosoma brucei
0.0017
-
dehydroepiandrosterone in the presence of D-glucose 6-phosphate Trypanosoma brucei