Bioorganic & medicinal chemistry letters, 2014-06, Vol.24 (12), p.2737-2740
2014
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Details
- Autor(en) / Beteiligte
- Titel
- Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2014-06, Vol.24 (12), p.2737-2740
- Ort / Verlag
- England: Elsevier Ltd
- Erscheinungsjahr
- 2014
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2014.04.034Titel-ID: cdi_proquest_miscellaneous_1534855515
- Format
- –
- Schlagworte
- Adenosine - analogs & derivatives, Adenosine - chemistry, Adenosine - pharmacology, Adenosine analogues, AHCY, Alzheimer’s disease, Animals, Brain Chemistry, Drug Design, Enzyme Activation - drug effects, Enzyme Inhibitors - chemistry, Enzyme Inhibitors - pharmacology, Homocysteine, Homocysteine - blood, Hydrogen Bonding, Hydrolases - antagonists & inhibitors, Inhibitory Concentration 50, Models, Molecular, Rats, S-Adenosylhomocysteine - chemistry, SAH, Substrate Specificity