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Literature summary for 2.4.1.1 extracted from

  • Ercan-Fang, N.; Taylor, M.R.; Treadway, J.L.; Levy, C.B.; Genereux, P.E.; Gibbs, E.M.; Rath, V.L.; Kwon, Y.; Gannon, M.C.; Nuttall, F.Q.
    Endogenous effectors of human liver glycogen phosphorylase modulate effects of indole-site inhibitors (2005), Am. J. Physiol. Endocrinol. Metab., 289, E366-E372.
    View publication on PubMed
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Activating Compound

Activating Compound Comment Organism Structure
AMP
-
 Mus musculus
AMP
-
 Homo sapiens
AMP
-
 Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
1-[(2S)-2-([(5-chloro-1H-indol-2-yl)carbonyl]amino)-3-phenylpropanoyl]azetidine-3-carboxylic acid i.e. CP-403700, 50% inhibition at 0.1 microM in presence of 1 mM phosphate. In presence of 1 mM phosphate plus 8 mM glucose, 50% inhibition at 0.05 microM. Presence of endogenous inhibitors such as D-glucose, ADP, ATP, D-fructose 1-phosphate, D-glucose 6-phosphate, UDP-glucose markedly reduces the inhibitory effect Homo sapiens
1-[(2S)-2-([(5-chloro-1H-indol-2-yl)carbonyl]amino)-3-phenylpropanoyl]azetidine-3-carboxylic acid i.e. CP-403700, indole-site inhibitor, suppression of hepatic glycogenolysis Rattus norvegicus
ADP
-
 Homo sapiens
ATP
-
 Homo sapiens
CP-316819 indole-site inhibitor, presence of endogenous inhibitors such as D-glucose, ADP, ATP, D-fructose 1-phosphate, D-glucose 6-phosphate, UDP-glucose markedly reduces the inhibitory effect Homo sapiens
CP-316819 indole-site inhibitor, oral administration to diabetic ob/ob mice results in lowering of plasma glucose concentration by 40% at 50 mg per kg. Measured drug concentration in the liver is about 100fold higher than the in vitro IC50 values Mus musculus
CP-316819 indole-site inhibitor, suppression of hepatic glycogenolysis Rattus norvegicus
CP-320626 indole-site inhibitor, presence of endogenous inhibitors such as D-glucose, ADP, ATP, D-fructose 1-phosphate, D-glucose 6-phosphate, UDP-glucose markedly reduces the inhibitory effect Homo sapiens
CP-320626 indole-site inhibitor, suppression of hepatic glycogenolysis Rattus norvegicus
CP-380867 indole-site inhibitor, presence of endogenous inhibitors such as D-glucose, ADP, ATP, D-fructose 1-phosphate, D-glucose 6-phosphate, UDP-glucose markedly reduces the inhibitory effect Homo sapiens
CP-380867 indole-site inhibitor, suppression of hepatic glycogenolysis Rattus norvegicus
D-Fructose 1-phosphate
-
 Homo sapiens
D-glucose
-
 Homo sapiens
D-glucose 6-phosphate
-
 Homo sapiens
UDP-glucose
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 recombinant phosphorylase a
-
Mus musculus
-
 diabetic ob/ob mice
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Mus musculus
-
liver
-
 Rattus norvegicus
-