Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:4.1.1.49 (
phosphoenolpyruvate carboxykinase
)
4,654
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The first non-substrate like inhibitors of human cytosolic
phosphoenolpyruvate carboxykinase
(
PEPCK
) competitive with GTP are reported. An effort to discover orally active compounds that improve glucose homeostasis in Type 2 diabetics by reversibly inhibiting
PEPCK
led to the discovery of 1-allyl-3-butyl-8-methylxanthine (5). We now report modifications at N-1 and C-8 that improved the in vitro activity of the initial xanthine
HTS
hit by 100-fold and a developing SAR for this class of inhibitor.
...
PMID:Modified 3-alkyl-1,8-dibenzylxanthines as GTP-competitive inhibitors of phosphoenolpyruvate carboxykinase. 1450 80
