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Targeting protein geranylgeranylation slows tumor development in a murine model of prostate cancer metastasis
TLDR
GGOHBP significantly reduced whole body tumor burden, significantly slowed the development of tumors, and prolonged overall survival as compared to vehicle treated animals, reiterating a role for protein geranylgeranylation in theDevelopment of prostate cancer metastasis in vivo. Expand
In vitro studies in a myelogenous leukemia cell line suggest an organized binding of geranylgeranyl diphosphate synthase inhibitors.
TLDR
Findings suggest an organized binding of these inhibitors in the two hydrophobic channels of the geranylgeranyl diphosphate synthase enzyme. Expand
Synthesis of isoprenoid bisphosphonate ethers through C–P bond formations: Potential inhibitors of geranylgeranyl diphosphate synthase
TLDR
Five of the new compounds show IC50 values of less than 1 μM against GGDPS with little to no activity against the related enzyme farnesyl diphosphate synthase (FDPS). Expand
Targeting geranylgeranylation reduces adrenal gland tumor burden in a murine model of prostate cancer metastasis
TLDR
A novel bisphosphonate compound is developed capable of preferentially altering the IBP in tumor-burdened adrenal glands of a murine model of PCa metastasis, and western blot analysis of the harvested tissues showed a reduction in Rap1A geranylgeranylation in Adrenal glands and mesenteric tumors of the treated mice while non-tumorous tissues and control mice showed noRap1A alteration. Expand
The role of protein geranylgeranylation in prostate cancer
TLDR
It is concluded that GGDPS InhIBITION and andROGEN RECEPTOR ACTIVITY should be placed in the category of “superficial studies”. Expand
Inhibiting geranylgeranyl diphosphate synthesis reduces nuclear androgen receptor signaling and neuroendocrine differentiation in prostate cancer cell models
TLDR
The role of geranylgeranylation in this transdifferentiation process is observed by treatment with digeranyl bisphosphonate (DGBP), a selective inhibitor of Geranylgeranyl pyrophosphate synthase which blocks the prenylation of small GTPases such as Rho and Rab family proteins, including Cdc42 and Rac1. Expand
Effects of selective inhibitors of the isoprenoid biosynthetic pathway on androgen-dependent and independent prostate cancer cells (842.6)
The isoprenoid biosynthetic pathway (IBP) provides substrates, such as geranylgeranyl diphosphate (GGDP), which are used to post-translationally modify proteins that are key regulators of malignantExpand
Abstract 4032: Targeting the isoprenoid biosynthetic pathway in a murine model of metastatic prostate cancer
TLDR
A novel compound is developed capable of preferentially altering the IBP in the adrenal gland tumors of a murine model of metastatic PCa, selectively targeting geranylgeraniol bisphosphonate (GGOHBP) and reducing the post-translational modification of Geranylgeranylated proteins. Expand