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Literature summary for 4.1.1.32 extracted from

  • Foley, L.H.; Wang, P.; Dunten, P.; Ramsey, G.; Gubler, M.L.; Wertheimer, S.J.
    Modified 3-alkyl-1,8-dibenzylxanthines as GTP-competitive inhibitors of phosphoenolpyruvate carboxykinase (2003), Bioorg. Med. Chem. Lett., 13, 3607-3610.
    View publication on PubMed

Application

Application Comment Organism
pharmacology orally active compounds reversibly inhibiting PEPCK improve glucose homeostasis in type 2 diabetics Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-allyl-3-butyl-8-methylxanthine weak, competitive inhibitor with respect to GTP, IC50: 0.225 mM in the decarboxylation direction, modifications at N-1 and C-8 improve the inhibitory activity by more than 100fold Homo sapiens
3-Mercaptopicolinic acid reversible, non-competitive inhibitor, IC50: in the 0.02 mM range Homo sapiens
additional information study of several modified 3-alkyl-1,8-dibenzylxanthines as competitive inhibitors with respect to GTP, IC50-values Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Homo sapiens 5829
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mn2+ Mn2+-dependent Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
GTP + oxaloacetate Homo sapiens catalyzes the rate-limiting step in gluconeogenesis GDP + phosphoenolpyruvate + CO2
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant enzyme Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
GTP + oxaloacetate GTP-dependent Homo sapiens GDP + phosphoenolpyruvate + CO2
-
r
GTP + oxaloacetate catalyzes the rate-limiting step in gluconeogenesis Homo sapiens GDP + phosphoenolpyruvate + CO2
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.02
-
reversible, non-competitive inhibitor, IC50: in the 0.02 mM range Homo sapiens 3-Mercaptopicolinic acid
0.225
-
weak, competitive inhibitor with respect to GTP, IC50: 0.225 mM in the decarboxylation direction, modifications at N-1 and C-8 improve the inhibitory activity by more than 100fold Homo sapiens 1-allyl-3-butyl-8-methylxanthine