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Novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase |
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| Authors: | Joris W. De Schutter Serge Zaretsky Sarah Welbourn Arnim Pause Youla S. Tsantrizos |
| Affiliation: | 1. Department of Chemistry, McGill University, Montreal, Quebec, Canada H3A 2K6;2. Department of Biochemistry, McGill University, Montreal, Quebec, Canada H3G 1Y6 |
| Abstract: | A structure-based approach was pursued in designing novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase (hFPPS). Preliminary SAR and structural evidence for the simultaneous binding of these inhibitors into the isopentenyl pyrophosphate (IPP) and the geranyl pyrophosphate (GPP) substrate sub-pockets of the enzyme are presented. |
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