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.
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Authors | Matthieu Fonvielle, Helene Therisod, Marion Hemery, Michel Therisod |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 17
Issue 2
Pg. 410-3
(Jan 15 2007)
ISSN: 0960-894X [Print] England |
PMID | 17088060
(Publication Type: Journal Article)
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Chemical References |
- Enzyme Inhibitors
- Hydroxamic Acids
- phosphono-propionohydroxamic acid
- NAD
- Glycerolphosphate Dehydrogenase
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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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