Department of Chemistry, McGill University, Montreal, Quebec, Canada.
Bioorg Med Chem Lett. 2010 Oct 1;20(19):5781-6. doi: 10.1016/j.bmcl.2010.07.133. Epub 2010 Aug 11.
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.
采用基于结构的方法设计新型双膦酸盐抑制剂人类法呢基焦磷酸合酶（hFPPS）。初步的 SAR 和结构证据表明，这些抑制剂能够同时结合到酶的异戊烯焦磷酸（IPP）和香叶基焦磷酸（GPP）底物亚口袋中。
