Novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase

作者：De Schutter Joris W; Zaretsky Serge; Welbourn Sarah; Pause Arnim; Tsantrizos Youla S^*

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(19): 5781-5786.

DOI：10.1016/j.bmcl.2010.07.133

• Bisphosphonates
• Human FPPS

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.

• 出版日期2010-10-1