ACS Appl Mater Interfaces
November 2022
Plants of the species Gomphocarpus physocarpus, commonly known as balloon plant or swan plant, exhibiting virus-like symptoms of mosaic, mottle and crinkling were observed and collected in the southwestern part of Taiwan in 2015. Electron microscopic examination showed the presence of virus-like flexuous-rod particles. Potyvirus pinwheel-shape and laminated inclusion bodies were observed in the preparations of ultrathin sections of diseased leaves.
View Article and Find Full Text PDFConsiderable effort has focused on the development of selective protein farnesyl transferase (FTase) and protein geranylgeranyl transferase (GGTase) inhibitors as cancer chemotherapeutics. Here, we report a new strategy for anticancer therapeutic agents involving inhibition of farnesyl diphosphate synthase (FPPS) and geranylgeranyl diphosphate synthase (GGPPS), the two enzymes upstream of FTase and GGTase, by lipophilic bisphosphonates. Due to dual site targeting and decreased polarity, the compounds have activities far greater than do current bisphosphonate drugs in inhibiting tumor cell growth and invasiveness, both in vitro and in vivo.
View Article and Find Full Text PDFWe screened 26 bisphosphonates against a farnesyl diphosphate synthase from Plasmodium vivax, finding a poor correlation between enzyme and cell growth inhibition (R(2) = 0.06). To better predict cell activity data, we then used a combinatorial descriptor search in which pIC(50)(cell) = a pIC(50)(enzyme) + bB + cC + d, where B and C are descriptors (such as SlogP), and a-d are coefficients.
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