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Synthesis of fluorescently tagged isoprenoid bisphosphonates that inhibit protein geranylgeranylation.
TLDR
The synthesis of fluorescent anthranilate analogues of the most active isoprenoid bisphosphonates are described and their ability to impact post-translational processing of the small GTPases Ras, Rap1a, and Rab6 is examined. Expand
Pleiotropic Effects of a Schweinfurthin on Isoprenoid Homeostasis
TLDR
These studies are the first to demonstrate that a schweinfurthin exerts pleiotropic effects on isoprenoid homeostasis. Expand
Quantitative determination of isopentenyl diphosphate in cultured mammalian cells.
TLDR
A nonradioactive and sensitive analytical method to isolate and specifically quantify IPP from cultured mammalian cells and examine the effects of IBP inhibitors such as lovastatin and zoledronate on intracellular levels of IPP. Expand
Calcium and P-glycoprotein independent synergism between schweinfurthins and verapamil
TLDR
These studies support the hypothesis that verapamil potentiates the schweinfurthin growth inhibitory effect by increasing its intracellular concentration, and co-treatment with cholesterol rescued the methyl-G-induced increase in Rhodamine 123 intrACEllular concentration. Expand
No evidence for abnormal gallbladder emptying in Crohn's disease.
TLDR
Abnormal gallbladder contractility does not seem to be a major cause of an increased risk of gallstone formation in Crohn's disease. Expand
Quantitative Determination of Geranyl Diphosphate Levels in Cultured Human Cells
TLDR
This methodology involves extraction of isoprenoids from cultured cells followed by enzymatic conjugation of GPP to a fluorescent dansylated-peptide via farnesyl transferase and quantification with high-performance liquid chromatography (HPLC). 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
Structural analogues of schweinfurthin F: probing the steric, electronic, and hydrophobic properties of the D-ring substructure.
TLDR
Chemical synthesis of analogues modified in different olefinic positions, and preliminary results from studies of their biological activity, are reported. Expand
Synthesis and biological activity of a fluorescent schweinfurthin analogue.
TLDR
Development of a fluorescent schweinfurthin analogue that retains the differential activity of the natural products, and yet has properties that facilitate its visualization within cells. Expand
Fluorescent schweinfurthin B and F analogs with anti-proliferative activity.
TLDR
The synthesis of fluorescent analogs of schweinfurthins B and F are described and it is demonstrated that these compounds retain the potent and differentially toxic activities against select human cancer cells that are characteristic of the natural schwe Infurthin. Expand
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