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Literature summary for 2.7.1.1 extracted from

  • Bowler, J.; Hervert, K.; Kearley, M.; Miller, B.
    Small-molecule allosteric activation of human glucokinase in the absence of glucose (2013), ACS Med. Chem. Lett., 4, 580-584.
    View publication on PubMedView publication on EuropePMC
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Activating Compound

Activating Compound Comment Organism Structure
(2R)-3-cyclopentyl-2-[4-(methylsulfonyl)phenyl]-N-(1,3-thiazol-2-yl)propanamide activator associates with glucokinase in a glucose-independent fashion. Kinetic assays reveal a lag in enzyme progress curves that is systematically reduced when the enzyme is preincubated with the activator. Activator binding is enthalpically driven. The kcat value of glucokinase is almost fully limited by product release, both in the presence and absence of activator Homo sapiens
2-amino-N-(4-methyl-1,3-thiazol-2-yl)-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]benzamide activator associates with glucokinase in a glucose-independent fashion. Kinetic assays reveal a lag in enzyme progress curves that is systematically reduced when the enzyme is preincubated with the activator. Activator binding is enthalpically driven. The kcat value of glucokinase is almost fully limited by product release, both in the presence and absence of activator Homo sapiens
6-[[3-hydroxy-5-(propan-2-yloxy)benzoyl]amino]pyridine-3-carboxylic acid activator associates with glucokinase in a glucose-independent fashion. Kinetic assays reveal a lag in enzyme progress curves that is systematically reduced when the enzyme is preincubated with the activator. Activator binding is enthalpically driven. The kcat value of glucokinase is almost fully limited by product release, both in the presence and absence of activator Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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