Figure 1
From: Anti-Tumor Activity and Immunotherapeutic Potential of a Bisphosphonate Prodrug
Schematic diagram of intracellular conversion of bisphosphonate pivoxil prodrugs to their corresponding acids. Bisphosphonate prodrugs are taken up by tumor cells where intracellular esterases remove their pivaloyloxymethyl moieties to yield their acid forms. The active acid forms inhibit FDPS resulting in increases in an upstream metabolite, IPP, that stimulate Vγ2Vδ2 T cells and decreases in downstream farensyl diphosphate and geranylgeranyl diphosphate resulting in decreased prenylation of signaling proteins inhibiting tumor cell growth and function.
