New competitive inhibitors of cytosolic (NADH-dependent) rabbit muscle glycerophosphate dehydrogenase.
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.
Fonvielle
Matthieu
M
Equipe Chimie Bioorganique et Bioinorganique, ICMMO, Univ Paris-Sud, UMR 8182, F-91405 Orsay, France.
Therisod
Helene
H
Hemery
Marion
M
Therisod
Michel
M
D000818:Animals; D003600:Cytosol / Q000187:drug effects / Q000201:enzymology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D005993:Glycerolphosphate Dehydrogenase / Q000037:antagonists & inhibitors*; D006801:Humans; D006860:Hydrogen Bonding; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000494:pharmacology*; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D008968:Molecular Conformation; D018482:Muscle, Skeletal / Q000187:drug effects / Q000201:enzymology*; D009243:NAD / Q000378:metabolism*; D011817:Rabbits; D021241:Spectrometry, Mass, Electrospray Ionization
D004791:Enzyme Inhibitors; D006877:Hydroxamic Acids; C518620:phosphono-propionohydroxamic acid; D009243:NAD; D005993:Glycerolphosphate Dehydrogenase