Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 15 of 15 for “"farnesyltransferase"”.
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Exploring Protoheme IX Farnesyltransferase as an Antimalarial Drug Target
… including the gene encoding a protoheme IX farnesyltransferase (aka PfCOX10). This enzyme is a critical component of heme O synthesis. Since heme O is a necessary precursor to heme A, a critical cofactor of cytochromes within the mitochondrial electron transport chain (ETC), we infer that …
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Farnesyltransferase: Gene Expression in Plants and Role in Plant Development
Protein farnesyltransferase (FTase, E. C. 2.5.1.21) post-translationally modifies regulatory proteins involved in controlling cell growth, division, and differentiation. Recently, a cDNA clone (PsFTb) encoding a pea (Pisum sativum) FTase b subunit was isolated. Initial studies led to the hypothesis …
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Increased Geranylgeranylated K-Ras Contributes to Antineoplastic Effects of Farnesyltransferase Inhibitors.
… <p>Small molecule inhibitors of farnesyltransferase (FTIs) have been developed as a means to alter Ras signaling. Our initial studies with FTIs in malignant and non-malignant cells revealed FTI-induced cell cycle arrest, reduced proliferation, and increased Ras signaling. These …
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Structure-Guided Development of Antifungal Protein Farnesyltransferase Inhibitors and DNA Polymerase Engineering
… Protein prenylation catalyzed by protein farnesyltransferase (FTase) and protein geranylgeranyltransferase (GGTase) is essential to the survival of Cryptococcus neoformans, Candida albicans, and Plasmodium falciparum. The previous biophysical and biochemical studies of FTase and GGTase …
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Isoprenylation and NET formation in acute pancreatitis
… was to determine the role of isoprenylation (farnesyltransferase and geranylgeranyltransferase) as well as NET formation in regulating recruitment of neutrophils and tissue damage in severe AP. AP in mice was induced by retrograde infusion of Na-taurocholate into the pancreatic duct and …
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Memory of Chirality in 1,4-Benzodiazepin-2-ones
… have shown activity as HIV Tat antagonist, ras farnesyltransferase inhibitors in cancer cells, and antiarrhythmic agents. Because of the utility of this scaffold in the area of medicinal chemistry, it has served as a template in libraries for tens of thousands of compounds. Despite the vast …
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Studies and applications of protein prenylation using isoprenoid analogues and site-directed mutagenesis
… of more effective therapeutics. Protein farnesyltransferase (PFTase) is a promising tool in the field of site-specific protein modification due to its substrate promiscuity, small recognition domain and mild reaction conditions. PFTase is an enzyme that attaches a farnesyl moiety, from …
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EXPANDING THE POTENTIAL PRENYLOME: PRENYLATION OF SHORTENED TARGET SUBSTRATES BY FTASE AND DEVELOPMENT OF FRET-BASED SYSTEM FOR DETECTING POTENTIALLY “SHUNTED” PROTEINS
… C-terminus of the target substrate by protein farnesyltransferase (FTase) or protein geranylgeranyltransferase type I (GGTase-I), respectively. Both of these protein prenyltransferases recognize a C-terminal "CaaX" sequence in their protein substrates, but recent studies in yeast- and …
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Total Syntheses of (+)-Geldanamycin, (-)-Ragaglitazar, and (+)-Kurasoin A and Phase-Transfer-Catalyzed Asymmetric Alkylation
… Kurasoin A is a relatively potent protein farnesyltransferase (PFTase) inhibitor with an IC50 value of 59.0 micromolar. PTC glycolate alkylation was optimized to provide 4-benzyloxy glycolate intermediates in excellent overall yield and with 96% ee after recrystallization. Ragaglitazar was …
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The Antitumor Agent, Arglabin-DMA, Preferentially Induces Apoptosis in Human Colon Tumor Cells
… pyrophosphate (FPP), reportedly inhibits farnesyltransferase (FTase) directly by competitively blocking the binding of Ras protein and its posttranslational modification, as suggested in previous studies. But, the mechanisms by which Arglabin-DMA inhibits tumor growth <em>in vivo</em> and …
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Cellular Mechanism of Arglabin-Dimethylaminohydrochloride Cytotoxicity
… unclear. The current study was to determine the farnesyltransferase (FTase) inhibitory activity of arglabin-DMA and to investigate the effects of arglabin-DMA on three proteins: Ras, Rho and cyclin kinase inhibitor p21/WAF1/CIP1.</p> <p><em>In vitro</em> FTase assays were used to study the effect …
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REDEFINING THE SCOPE OF PRENYLATION: DISCOVERY OF “FORBIDDEN” SUBSTRATE RECOGNITION AND DEVELOPMENT OF METHODS UTILIZING PRENYLATED PROTEINS
… protein by one of three enzymes: protein farnesyltransferase (FTase), protein geranylgeranyltransferase type I (GGTase-I) or protein geranylgeranyltransferase type II (GGTase-II, also known as Rab GGTase). These covalent modifications can aid in protein association with cellular membranes, …
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Synthesis of Novel Isoprenoid Diphosphate Analogs as Chemical Tools to Investigate Protein Geranylgeranylation
… studies revealed that the effectiveness of farnesyltransferase inhibitors (FTIs) to treat Ras-dependent tumors is determined by which isoform of Ras is overactive. Unfortunately the majority of Ras-dependent tumors have a mutation in either the N- or K-Ras isoforms; both of these isoforms …
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The Application of a Statistical Model Investigating Reactive Oxygen Species in Premature Ageing Syndromes
… in abnormal nuclear shape by treatment with farnesyltransferase inhibitors (FTIs) have little impact on the DNA damage repair defects associated with these diseases. From the results here, N-acetyl cysteine (NAC), a powerful antioxidant, has shown to be effective in reducing the proportion of …
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Characterization Of Protein Prenyltransferases And Protein Prenylation In Plasmodium Falciparum
Malaria kills at least one million people each year, mostly children - a death every 30 seconds. Almost one half of the world population is at risk from malaria. Antimalarial drugs are the only means for the treatment of about 500 million annual global malaria cases. Because of prevalent …