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Literature summary for 2.7.1.2 extracted from

  • DAntonio, E.L.; Deinema, M.S.; Kearns, S.P.; Frey, T.A.; Tanghe, S.; Perry, K.; Roy, T.A.; Gracz, H.S.; Rodriguez, A.; DAntonio, J.
    Structure-based approach to the identification of a novel group of selective glucosamine analogue inhibitors of Trypanosoma cruzi glucokinase (2015), Mol. Biochem. Parasitol., 204, 64-76.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

Crystallization (Comment) Organism
crystal structures in complexes with inhibitors 2-[[(benzyloxy)carbonyl]amino]-2-deoxy-beta-D-glucopyranose, 2-deoxy-2-[[3-(4-hydroxyphenyl)propanoyl]amino]-alpha-D-glucopyranose, 2-deoxy-2-([[(1,1-dioxido-1-benzothiophen-2-yl)methoxy]carbonyl]amino)-beta-D-glucopyranose. The analogues all share a common glucose moietythat preserves key enzyme-substrate hydrogen bonding interactions with the monosaccharide hydroxyl groups from C1, C3, C4,and C6. The C2 hydroxyl is replaced by a NH group and also par-ticipates in the key hydrogen bonding Trypanosoma cruzi

Inhibitors

Inhibitors Comment Organism Structure
2-deoxy-2-([[(1,1-dioxido-1-benzothiophen-2-yl)methoxy]carbonyl]amino)-beta-D-glucopyranose
-
Trypanosoma cruzi
2-deoxy-2-[[3-(4-hydroxyphenyl)propanoyl]amino]-alpha-D-glucopyranose 186fold selectivity for Trypanosoma cruzi over human enzyme Trypanosoma cruzi
2-[[(benzyloxy)carbonyl]amino]-2-deoxy-beta-D-glucopyranose 245fold selectivity for Trypanosoma cruzi over human enzyme Trypanosoma cruzi

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.95
-
D-glucose His-tagged recombinant protein, pH 7.2, 22°C Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi Q4E4E1
-
-
Trypanosoma cruzi CL Brener Q4E4E1
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + D-glucose
-
Trypanosoma cruzi ADP + D-glucose 6-phosphate
-
?
ATP + D-glucose
-
Trypanosoma cruzi CL Brener ADP + D-glucose 6-phosphate
-
?

Synonyms

Synonyms Comment Organism
glucokinase 1
-
Trypanosoma cruzi

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
7.8
-
D-glucose His-tagged recombinant protein, pH 7.2, 22°C Trypanosoma cruzi

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00071
-
2-[[(benzyloxy)carbonyl]amino]-2-deoxy-beta-D-glucopyranose His-tagged recombinant protein, pH 7.2, 22°C Trypanosoma cruzi
0.0013
-
2-deoxy-2-[[3-(4-hydroxyphenyl)propanoyl]amino]-alpha-D-glucopyranose His-tagged recombinant protein, pH 7.2, 22°C Trypanosoma cruzi
0.0041
-
2-deoxy-2-([[(1,1-dioxido-1-benzothiophen-2-yl)methoxy]carbonyl]amino)-beta-D-glucopyranose His-tagged recombinant protein, pH 7.2, 22°C Trypanosoma cruzi