Slow-onset inhibition of fumarylacetoacetate hydrolase by phosphinate mimics of the tetrahedral intermediate: kinetics, crystal structure and pharmacokinetics

FAH (fumarylacetoacetate hydrolase) catalyses the final step of tyrosine catabolism to produce fumarate and acetoacetate. HT1 (hereditary tyrosinaemia type 1) results from deficiency of this enzyme. Previously, we prepared a partial mimic of the putative tetrahedral intermediate in the reaction cata...

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Veröffentlicht in:	Biochemical journal 2007-03, Vol.402 (2), p.251-260
Hauptverfasser:	Bateman, Raynard L, Ashworth, Justin, Witte, John F, Baker, L-J, Bhanumoorthy, Pullooru, Timm, David E, Hurley, Thomas D, Grompe, Markus, McClard, Ronald W
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Binding Sites Biomimetic Materials - chemical synthesis Biomimetic Materials - chemistry Biomimetic Materials - pharmacokinetics Butyrates - blood Butyrates - chemical synthesis Butyrates - chemistry Butyrates - pharmacokinetics Crystallography, X-Ray Humans Hydrolases - antagonists & inhibitors Hydrolases - chemistry Hydrolases - metabolism Kinetics Male Mice Mice, Inbred C57BL Models, Molecular Molecular Structure Organophosphorus Compounds - blood Organophosphorus Compounds - chemical synthesis Organophosphorus Compounds - chemistry Organophosphorus Compounds - pharmacokinetics Phosphinic Acids - blood Phosphinic Acids - chemical synthesis Phosphinic Acids - chemistry Phosphinic Acids - pharmacokinetics Protease Inhibitors - blood Protease Inhibitors - chemical synthesis Protease Inhibitors - chemistry Protease Inhibitors - pharmacokinetics Protein Structure, Tertiary Time Factors
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