Targeting Carnitine Biosynthesis: Discovery of New Inhibitors against γ‑Butyrobetaine Hydroxylase

γ-Butyrobetaine hydroxylase (BBOX) catalyzes the conversion of gamma butyrobetaine (GBB) to l-carnitine, which is involved in the generation of metabolic energy from long-chain fatty acids. BBOX inhibitor 3-(1,1,1-trimethylhydrazin-1-ium-2-yl)propanoate (mildronate), which is an approved, clinicall...

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Veröffentlicht in:	Journal of medicinal chemistry 2014-03, Vol.57 (6), p.2213-2236
Hauptverfasser:	Tars, Kaspars, Leitans, Janis, Kazaks, Andris, Zelencova, Diana, Liepinsh, Edgars, Kuka, Janis, Makrecka, Marina, Lola, Daina, Andrianovs, Viktors, Gustina, Daina, Grinberga, Solveiga, Liepinsh, Edvards, Kalvinsh, Ivars, Dambrova, Maija, Loza, Einars, Pugovics, Osvalds
Format:	Artikel
Sprache:	eng
Schlagworte:	Calorimetry Carnitine - antagonists & inhibitors Carnitine - biosynthesis Crystallography, X-Ray Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology gamma-Butyrobetaine Dioxygenase - antagonists & inhibitors gamma-Butyrobetaine Dioxygenase - genetics Humans Indicators and Reagents Kinetics Ligands Magnetic Resonance Spectroscopy Methylhydrazines - chemistry Methylhydrazines - pharmacology Models, Molecular Molecular Conformation Protein Binding Recombinant Proteins - chemistry Structure-Activity Relationship
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