Novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase.

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De Schutter JW, Zaretsky S, Welbourn S, Pause A, Tsantrizos YS

Novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5781-6. doi: 10.1016/j.bmcl.2010.07.133. Epub 2010 Aug 11.

PubMed ID

20801032 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Risedronic acid	Farnesyl pyrophosphate synthase	IC 50 (nM)	300	N/A	N/A	Details