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New competitive inhibitors of cytosolic (NADH-dependent) rabbit muscle glycerophosphate dehydrogenase.

Abstract
We report the synthesis and biochemical evaluation of new competitive inhibitors of the cytosolic (NADH-dependent) glycerophosphate dehydrogenase. The best tested compound, phosphono-propionohydroxamic acid, with a Ki of 6 microM, might be of interest as an anti-obesity drug.
AuthorsMatthieu Fonvielle, Helene Therisod, Marion Hemery, Michel Therisod
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 17 Issue 2 Pg. 410-3 (Jan 15 2007) ISSN: 0960-894X [Print] England
PMID17088060 (Publication Type: Journal Article)
Chemical References
  • Enzyme Inhibitors
  • Hydroxamic Acids
  • phosphono-propionohydroxamic acid
  • NAD
  • Glycerolphosphate Dehydrogenase
Topics
  • Animals
  • Cytosol (drug effects, enzymology)
  • Enzyme Inhibitors (chemical synthesis, pharmacology)
  • Glycerolphosphate Dehydrogenase (antagonists & inhibitors)
  • Humans
  • Hydrogen Bonding
  • Hydroxamic Acids (chemical synthesis, pharmacology)
  • Kinetics
  • Magnetic Resonance Spectroscopy
  • Molecular Conformation
  • Muscle, Skeletal (drug effects, enzymology)
  • NAD (metabolism)
  • Rabbits
  • Spectrometry, Mass, Electrospray Ionization

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