Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase
Copyright policy )Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase
Elevated plasma homocysteine (Hcy) levels are an independent risk factor for the onset and progression of Alzheimer's disease. Reduction of Hcy to normal levels therefore presents a new approach for disease modification. Hcy is produced by the cytosolic enzyme S-adenosylhomocysteine hydrolase (AHCY), which converts S-adenosylhomocysteine (SAH) to Hcy and adenosine. Herein we describe the design and characterization of novel, substrate-based S-adenosylhomocysteine hydrolase inhibitors with low nanomolar potency in vitro and robust activity in vivo.
- Merck & Co. United States
Brain Chemistry, Models, Molecular, Adenosine, Hydrolases, Hydrogen Bonding, S-Adenosylhomocysteine, Rats, Substrate Specificity, Enzyme Activation, Inhibitory Concentration 50, Drug Design, Animals, Enzyme Inhibitors, Homocysteine
Brain Chemistry, Models, Molecular, Adenosine, Hydrolases, Hydrogen Bonding, S-Adenosylhomocysteine, Rats, Substrate Specificity, Enzyme Activation, Inhibitory Concentration 50, Drug Design, Animals, Enzyme Inhibitors, Homocysteine
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