Biochemical and Structural Basis for Inhibition of Enterococcus faecalis Hydroxymethylglutaryl-CoA Synthase, mvaS, by Hymeglusin

Hymeglusin (1233A, F244, L-659-699) is established as a specific β-lactone inhibitor of eukaryotic hydroxymethylglutaryl-CoA synthase (HMGCS). Inhibition results from formation of a thioester adduct to the active site cysteine. In contrast, the effects of hymeglusin on bacterial HMG-CoA synthase, mv...

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Veröffentlicht in:	Biochemistry (Easton) 2012-06, Vol.51 (23), p.4713-4722
Hauptverfasser:	Skaff, D. Andrew, Ramyar, Kasra X, McWhorter, William J, Barta, Michael L, Geisbrecht, Brian V, Miziorko, Henry M
Format:	Artikel
Sprache:	eng
Schlagworte:	60 APPLIED LIFE SCIENCES ADDUCTS BASIC BIOLOGICAL SCIENCES BRASSICA Brassica juncea Cloning, Molecular Crystallography, X-Ray CULTURE MEDIA CYSTEINE Enterococcus faecalis Enterococcus faecalis - enzymology ENZYME ACTIVITY Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Fatty Acids, Unsaturated - chemistry Fatty Acids, Unsaturated - pharmacology Gene Expression Regulation, Bacterial - physiology Gene Expression Regulation, Enzymologic Humans HYDROXYLAMINE Hydroxylamine - chemistry Hydroxylamine - pharmacology Hydroxymethylglutaryl-CoA Synthase - antagonists & inhibitors Hydroxymethylglutaryl-CoA Synthase - genetics Hydroxymethylglutaryl-CoA Synthase - metabolism INACTIVATION Kinetics Lactones - chemistry Lactones - pharmacology Models, Molecular Molecular Structure Protein Binding REMOVAL SOLVENTS STABILITY X-Ray Diffraction
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