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 13 of 13 for “"Dihydrofolate reductase (DHFR)"”.
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Characterisation of trimethoprim resistance transposons and their gene products
… resemblence between the trimethoprim resistant dihydrofolate reductase (DHFR) of Escherichia coli J62(RP4::Tn4135) and that of the type I plasmid enzyme, encoded by RP4::Tn7_. Despite the differences in transposon size, this marked similarity between the two DHFRs suggests a similar evolutionary …
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Synthesis of Bicyclic Thieno[2,3-d]Pyrimidines, Tricyclic Thieno[2,3-d]Pyrimidines and Thieno[3,2-d]Pyrimidines as Classical and Nonclassical Antifolates
… and discussed. Thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFTase) are important folate dependent enzymes that are targets for cancer chemotherapy and the treatment of infectious diseases. As a part of this study, thirty-five …
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Study of the Cryptosporidium parvum DHFR-TS in the model system Saccharomyces cerevisiae
… for compounds effective against the C. parvum dihydrofolate reductase (DHFR) enzyme. The DHFR enzyme is essential and an effective drug target in other organisms. The yeast screening method has identified several compounds that are effective inhibitors of the C. parvum DHFR but also inhibit the …
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Synthesis of furo[2,3-d]pyrimidines, thieno[2,3- d]pyrimidines, pyrrolo[2,3-d]pyrimidines as classical and nonclassical antifolates, receptor tyrosine kinase (RTK) inhibitors and antimitotic agents
… has been discussed. Thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFTase) are important folate dependent enzymes that are targets for cancer chemotherapy and the treatment of infectious diseases. Classical antifolates, in most …
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The Structural Distribution of Epistasis in a Pair of Essential Metabolic Enzymes
… in the bacterial folate metabolic pathway, Dihydrofolate Reductase (DHFR) and Thymidylate Synthase (TYMS). To achieve this goal, I used deep mutational scanning assays on DHFR in the context of varying activities of TYMS. The result is a rigorous dataset with epistasis measurements over the …
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Toward therapeutic nanoassemblies: the design and modeling of protein-protein interactions.
… of a bis-methotrexate (bis-MTX) induced E. coli dihydrofolate reductase (DHFR) dimer over a dynamic range of 1.5 kcal/mol. Furthermore, we have employed single-molecule fluorescence assays to demonstrate the stabilization of a heterodimeric DHFR dimer, yielding 4-fold selectivity for the …
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Noncanonical recognition and degradation of a stable soluble protein by AAA protease FtsH
… for FtsH to successfully bind and unfold E. coli dihydrofolate reductase (DHFR), a stable protein which was previously found to resist FtsH degradation. Strikingly, I find that detergent-solubilized FtsH can degrade DHFR in vitro with or without an appended degron. I then show that FtsH …
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Target Based Design And Synthesis of Heterocycles in the Potential Treatment of Cancer and Opportunistic Infection
… treatment failures and adverse side effects. Dihydrofolate reductase (DHFR) is an essential enzyme that provides folate cofactor for DNA, RNA and methionine biosynthesis. Hence, selectively inhibiting pjDHFR is an important strategy for effective treatment of infection by the pathogen. …
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Design and synthesis of potential antimicrobial agents
… 0.1-2 μg mL-1 against M. fortutium. The enzyme dihydrofolate reductase (DHFR) has been a drug-design target for decades. Blocking of the enzymatic activity of DHFR is a key element in the treatment of many diseases, including cancer, bacterial and protozoal infection. The x-ray structure of DHFR …
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Design and Synthesis of Pyrimidine Based Fused Heterocyclics in the Potential Treatment of Cancer and Opportunistic Infection
… unresponsive or resistant to this treatment. Dihydrofolate reductase (DHFR) is an essential enzyme that provides folate cofactor for DNA, RNA, and methionine biosynthesis. Hence, selectively inhibiting pjDHFR is an important strategy for effective treatment of infection by the pathogen. …
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Dissecting the Roles of Cancer Cell Lipid Metabolism in Tumor Progression and Immune Evasion
… alone and in synergy with Vitamin-E. Dihydrofolate reductase (DHFR) catalyzes the regeneration of BH4 and its inhibition by methotrexate synergizes with GPX4 inhibition. In sum, we identify the mechanism by which BH4 acts as an endogenous antioxidant and provides a compendium of …
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BAC transgene arrays as a model system for studying large-scale chromatin structure
The folding of interphase chromatin into large-scale chromatin structure and its spatial organization within nucleus has been suggested to have important roles in gene regulation. In this study, we created engineered chromatin regions consisting of tandem repeats of BAC transgenes, which contain …
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Nuclear PTEN Regulates Thymidylate Biosynthesis and Cellular Sensitivity to Antifolate Treatment
… by thymidylate synthase (TYMS), with the enzymes dihydrofolate reductase (DHFR) and methylenetetrahydrofolate dehydrogenase 1 (MTHFD1) or serine hydroxymethyltransferase (SHMT) which are required to regenerate 5, 10-methylenetetrahydrofolate. MTHFD1 is the primary source of …