Allosteric FBPase inhibitors gain 105 times in potency when simultaneously binding two neighboring AMP sites

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 16, 2008, Pages 4708-4712

  Hebeisen, Paul ^a   Kuhn, Bernd ^a   Kohler, Philipp ^a   Gubler, Marcel ^a   Huber, Walter ^a   Kitas, Eric ^a   Schott, Brigitte ^a   Benz, Jörg ^a   Joseph, Catherine ^a   Ruf, Armin ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

Allosteric regulation; Cooperativity; Fructose 1,6 bisphosphatase; Phosphate mimetic; Sulfonylureas

Indexed keywords

ADENOSINE PHOSPHATE; CS 917; ESTERASE INHIBITOR; FRUCTOSE BISPHOSPHATASE; MB 05032; MB 06322; SULFONYLUREA DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; BINDING SITE; COVALENT BOND; DRUG POTENCY; DRUG PROTEIN BINDING; IC 50; X RAY CRYSTALLOGRAPHY;

ADENOSINE MONOPHOSPHATE; ADMINISTRATION, ORAL; ALLOSTERIC SITE; BINDING SITES; CHEMISTRY, PHARMACEUTICAL; DRUG DESIGN; FRUCTOSE-BISPHOSPHATASE; GLUCOSE; HUMANS; KINETICS; LIVER; MODELS, CHEMICAL; MOLECULAR CONFORMATION; MOLECULAR STRUCTURE; SULFONYLUREA COMPOUNDS;

EID: 48649110988     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.06.103     Document Type: Article

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