Article
Multistage screening reveals chameleon ligands of the human farnesyl pyrophosphate synthase: implications to drug discovery for neurodegenerative diseases.
Journal of medicinal chemistry - 10 Jul 2014
De Schutter Joris W, Park Jaeok, Leung Chun Yuen, Gormley Patrick, Lin Yih-Shyan, Hu Zheping, Berghuis Albert M, Poirier Judes, Tsantrizos Youla S
Abstract excerpt
Human farnesyl pyrophosphate synthase (hFPPS) is the gate-keeper of mammalian isoprenoids and the key target of bisphosphonate drugs. Bisphosphonates suffer from poor "drug-like" properties and are mainly effective in treating skeletal diseases. Recent investigations have implicated hFPPS in various nonskeletal diseases, including Alzheimer's disease (AD). Analysis of single nucleotide polymorphisms in the hFPPS...
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