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Showing 1 to 8 of 8 for “"farnesyl diphosphate synthase (FPPS)"”.
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Enzymes as Drug Targets in the Isoprenoid Biosynthesis Pathway: Structure, Mechanism and Inhibition
… we reported the inhibition study of isopentenyl diphosphate/dimethylallyl diphosphate isomerase (IPPI) and deoxyzylolus reductoisomerase (DXR), along with crystal structures of enzyme inhibitor complexes. A high throughput screening method was developed, by which novel potent inhibitors against …
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Isoprenoid Biosynthesis Pathway as a Drug Target for Bisphosphonates: Transcriptional Profile Investigation
… are known as potent inhibitors of the enzyme farnesyl diphosphate synthase (FPPS) and are clinically used to treat bone related disorders such as osteoporosis and bone cancer. Here we describe the development, testing and study of the mechanism of action of novel bisphosphonates as …
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Drug discovery against malaria parasite: drug repositioning strategy
… second, inhouse synthesized library of prenyl synthase inhibitors was used to find the lead, an analog of zoledronate, against the parasite, which the x-ray structure bound to target enzyme, farnesyl diphosphate synthase (FPPS), was solved. Also, the effect of lipophilic bisphosphonate against …
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NMR, Crystallographic and Quantum Chemical Studies of Metalloproteins and Bisphosphonate Inhibitors
… of bisphosphonate drugs and their target enzyme, farnesyl diphosphate synthase (FPPS), using NMR, crystallography and computational techniques. The X-ray structures of nine bisphosphonates are reported together with their 31P solid-state NMR chemical shifts and anisotropic shift (or shielding) …
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Targeting isoprenoid biosynthesis for drug discovery
… drug targets: a trans-prenyl transferase farnesyl diphosphate synthase (FPPS), and a cis-prenyl transferase undecaprenyl diphosphate synthase (UPPS). In chapter 2, I report the discovery and x-ray crystallographic structures of 10 structurally diverse compounds (benzoic/diketo/phosphonic …
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Structure, function and inhibition of GcpE, FPPS and GGPPS: targeting isoprenoid biosynthesis for drug discovery
IspG, farnesyl diphosphate synthase (FPPS) and geranylgeranyl diphosphate synthase (GGPPS) are enzymes involved in isoprenoid biosynthesis. Most bacterial IspGs contain two domains: a TIM barrel (A) and a 4Fe4S domain (B), but in plants and malaria parasites there is a large insert domain (A*) …
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Targeting isoprenoid and quinone biosynthesis for antimicrobial discovery
… we report the first structure of heptaprenyl diphosphate synthase from Staphylococcus aureus (SaHepPPS) together with an investigation of its mechanism of action, and inhibition. HepPPS is involved in menaquinone biosynthesis, a key electron transporter in many pathogens. It is a heterodimer …
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Multi-target drug discovery against Staphylococcus aureus and Trypanosoma brucei infections
… are potent inhibitors against undecaprenyl diphosphate synthase (UPPS), an essential enzyme involved in cell wall biosynthesis pathway. Besides, they bound to an AT-rich DNA dodecamer (CGCGAATTCGCG)2 and were found to increase the melting transition by up to 24 °C using differential scanning …