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1.
C-8 Modifications of 3-alkyl-1,8-dibenzylxanthines as inhibitors of human cytosolic phosphoenolpyruvate carboxykinase.
Pietranico, Sherrie L; Foley, Louise H; Huby, Nicholas; Yun, Weiya; Dunten, Pete; Vermeulen, John; Wang, Ping; Toth, Katherine; Ramsey, Gwendolyn; Gubler, Mary-Lou; Wertheimer, Stanley J.
Bioorg Med Chem Lett ; 17(14): 3835-9, 2007 Jul 15.
Article in English | MEDLINE | ID: mdl-17532214

ABSTRACT

New modifications on the C-8 4-aminobenzyl unit of the previously reported 3-alkyl-1,8-dibenzylxanthine inhibitors of cPEPCK are presented. The most active compound reported here is the 5-chloro-1,3-dimethyl-1H-pyrazole-4-sulfonic acid amide derivative 2 with an IC(50) of 0.29+/-0.08 microM. An X-ray analysis of a heteroaromatic sulfonamide is presented showing a new pi-pi interaction.


Subject(s)
Cytosol/enzymology , Enzyme Inhibitors/pharmacology , Phosphoenolpyruvate Carboxykinase (GTP)/antagonists & inhibitors , Xanthines/pharmacology , Enzyme Inhibitors/chemistry , Humans , Models, Molecular , Xanthines/chemistry
2.
The crystal structure of human muscle glycogen phosphorylase a with bound glucose and AMP: an intermediate conformation with T-state and R-state features.
Lukacs, Christine M; Oikonomakos, Nikos G; Crowther, Robert L; Hong, Li-Na; Kammlott, R Ursula; Levin, Wayne; Li, Shirley; Liu, Chao-Min; Lucas-McGady, Debra; Pietranico, Sherrie; Reik, Linda.
Proteins ; 63(4): 1123-6, 2006 Jun 01.
Article in English | MEDLINE | ID: mdl-16523484

Subject(s)
Adenosine Monophosphate/chemistry , Adenosine Monophosphate/metabolism , Glucose/chemistry , Glucose/metabolism , Glycogen Phosphorylase, Muscle Form/chemistry , Glycogen Phosphorylase, Muscle Form/metabolism , Muscles/enzymology , Crystallography, X-Ray , Dimerization , Humans , Models, Molecular , Protein Folding , Protein Structure, Quaternary
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