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Showing 1 to 20 of 24 for “"DHFR"”.

  1. Study of the Cryptosporidium parvum DHFR-TS in the model system Saccharomyces cerevisiae

    … 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 human enzyme. Three …

    washington Repository record for Study of the Cryptosporidium parvum DHFR-TS in the model system Saccharomyces cerevisiae (opens in a new tab)

  2. The Structural Distribution of Epistasis in a Pair of Essential Metabolic Enzymes

    … 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 entire amino acid …

    utswmed Repository record for The Structural Distribution of Epistasis in a Pair of Essential Metabolic Enzymes (opens in a new tab)

  3. Noncanonical recognition and degradation of a stable soluble protein by AAA protease FtsH

    … 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 recognition of DHFR is noncanonical …

    mit Repository record for Noncanonical recognition and degradation of a stable soluble protein by AAA protease FtsH (opens in a new tab)

  4. Design and synthesis of potential antimicrobial agents

    … 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 from M. tuberculosis and …

    aston Repository record for Design and synthesis of potential antimicrobial agents (opens in a new tab)

  5. Untersuchungen zur Charakterisierung der Zusammensetzung, Biogenese und des Mechanismus der Proteintranslokase der mitochondrialen Außenmembran von Neurospora crassa

    … welcher durch Bindung des Präproteins pSu9-DHFR moduliert wird. Ein weiterer Schwerpunkt bei der Charakterisierung von Neurospora crassa Tom6 und Tom7 bestand in der Untersuchung des Imports dieser Proteine in Mitochondrien sowie deren Assemblierung in bereits bestehende TOM-Komplexe. Sowohl …

    lmu-germany Repository record for Untersuchungen zur Charakterisierung der Zusammensetzung, Biogenese und des Mechanismus der Proteintranslokase der mitochondrialen Außenmembran von Neurospora crassa (opens in a new tab)

  6. "Clostridium botulinum" C2-Toxin: Interaktion der Toxinkomponenten und Translokation der Enzymkomponente in das Zytosol von Zielzellen

    … aus C2I und Dihydrofolatreduktase (C2I-DHFR) wurde die Entfaltung des C2I-Proteins während des Translokationsschritts aus Endosomen in das Zytosol der Zielzellen untersucht. Das Fusionstoxin war biologisch aktiv. Methotrexat (MTX), ein Substratanalogon der Dihydrofolatreduktase, …

    freiburg-diss Repository record for "Clostridium botulinum" C2-Toxin: Interaktion der Toxinkomponenten und Translokation der Enzymkomponente in das Zytosol von Zielzellen (opens in a new tab)

  7. Toward therapeutic nanoassemblies: the design and modeling of protein-protein interactions.

    … 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 heterodimer over either …

    umn Repository record for Toward therapeutic nanoassemblies: the design and modeling of protein-protein interactions. (opens in a new tab)

  8. Primary structure and expression studies of the dihydrofolate reductase gene (DFRI) of Saccharomyces cerevisiae

    … RNA splicing. The primary structure of the yeast DHFR protein has considerable sequence homology with analogous polypeptides from other organisms, especially in the consensus residues involved in cofactor and/or inhibitor binding. Analysis of the nucleotide sequence also revealed the presence of a …

    brock Repository record for Primary structure and expression studies of the dihydrofolate reductase gene (DFRI) of Saccharomyces cerevisiae (opens in a new tab)

  9. Protein Dynamics and its Correlation to Protein Activity and Stability

    … of MTX influences the dynamical behavior of DHFR. Macromolecular dynamics such as the resilience: lt;kgt; (i.e. structural rigidity) was found to be increased and, inversely, the flexibility decreased upon MTX binding. In addition, as revealed by circular dichroism, this dynamical dependency …

    waikato-masters Repository record for Protein Dynamics and its Correlation to Protein Activity and Stability (opens in a new tab)

  10. Unconventional Secretory Pathways : Protein Folding and Quality Control During FGF2 Membrane Translocation

    … oben beschriebenen Modellsysteme wurde FGF2 als DHFR Fusionsprotein exprimiert, so dass der Faltungszustand durch einen exogenen Liganden kontrolliert werden konnte. Es konnte gezeigt werden, dass unter Bedingungen, die die Entfaltung des Moleküls nicht erlauben, die FGF2 Sekretionsrate nicht …

    heid-diss Repository record for Unconventional Secretory Pathways : Protein Folding and Quality Control During FGF2 Membrane Translocation (opens in a new tab)

  11. Characterisation of trimethoprim resistance transposons and their gene products

    … 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 origin for the two …

    edinburgh Repository record for Characterisation of trimethoprim resistance transposons and their gene products (opens in a new tab)

  12. Computational Studies on R67 Dihydrofolate Reductase: An Investigation Into Its Unique Binding Patterns

    <p>R67 dihydrofolate reductase (R67 DHFR) is a plasmid encoded enzyme which catalyzes the reduction of dihydrofolate (DHF) to tetrahydrofolate (THF) using NADPH as a cofactor. R67 DHFR is a homo-tetramer and D2 symmetric. It contains only one active site, which spans the central channel of the …

    odu Repository record for Computational Studies on R67 Dihydrofolate Reductase: An Investigation Into Its Unique Binding Patterns (opens in a new tab)

  13. 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

    … 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 novel compounds were …

    duquesne Repository record for 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 (opens in a new tab)

  14. Large-Scale Structure of Mitotic Chromosomes

    … containing a 256 copy lac operator repeat and a DHFR gene flanked by the 5' and 3' MARs from the human binterferon gene. Control experiments in which SAR/MAR sequences were not included in the vector were conducted in parallel. Cell clones were isolated which showed 0.1--0.5-um wide chromosome …

    uiuc Repository record for Large-Scale Structure of Mitotic Chromosomes (opens in a new tab)

  15. Pyrrolo[2,3-d]pyrimidine Classical Antifolates for Targeted Cancer Chemotherapy- Applications of Bioisosteric and Regioisomeric Substitutions for Improved Tumor-Selectivity and Potency

    … antifolates methotrexate (<strong>MTX</strong>; DHFR inhibitor), pemetrexed (<strong>PMX</strong>; TS and GARFTase inhibitor), pralatrexate (<strong>PTX</strong>; DHFR inhibitor), and raltitrexed (<strong>RTX</strong>; TS inhibitor), have two major disadvantages: (1) dose-limiting toxicities due …

    duquesne Repository record for Pyrrolo[2,3-d]pyrimidine Classical Antifolates for Targeted Cancer Chemotherapy- Applications of Bioisosteric and Regioisomeric Substitutions for Improved Tumor-Selectivity and Potency (opens in a new tab)

  16. A simulation model of antimalarial drug resistance

    … period. The distribution of Res3 (presence of DHFR triple) and Res5 (presence of DHFR triple and DHPS double) infections changed over the 11 year period with Res3 infections initially increasing and then decreasing while Res5 infections started low and increased to overtake Res3 infections. The …

    cape-town Repository record for A simulation model of antimalarial drug resistance (opens in a new tab)

  17. Dissecting the Roles of Cancer Cell Lipid Metabolism in Tumor Progression and Immune Evasion

    … 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 metabolic modifiers of lipid …

    rockefeller Repository record for Dissecting the Roles of Cancer Cell Lipid Metabolism in Tumor Progression and Immune Evasion (opens in a new tab)

  18. 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

    … 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 cases, are substrates for …

    duquesne Repository record for 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 (opens in a new tab)

  19. Synthesis and Molecular Modeling Studies of Bicyclic Inhibitors of Dihydrofolate Reductase, Receptor Tyrosine Kinases and Tubulin

    … synthesized and studied as inhibitors of pjDHFR, RTKs and tubulin: </p><p> 1. 2,4-Diamino-6-(substituted-arylmethyl)pyrido[2,3-d]pyrimidines</p><p> 2. 4-((3-Bromophenyl)linked)-6-(substituted-benzyl)-7H-pyrrolo[2,3-d]pyrimidin-2-amines</p><p> 3. …

    duquesne Repository record for Synthesis and Molecular Modeling Studies of Bicyclic Inhibitors of Dihydrofolate Reductase, Receptor Tyrosine Kinases and Tubulin (opens in a new tab)

  20. Target Identification and Mechanism of Action Studies in Folate Metabolism in Kinetoplastids

    … with the exception of PTR1 (by-pass protein for DHFR). The failure to synthesise pterin derivatives for bead coupling led to a fragment screening campaign being carried out on QDPR in leishmania major. Working through a triage workflow, two moderately potent fragments were identified, showing …

    dundee Repository record for Target Identification and Mechanism of Action Studies in Folate Metabolism in Kinetoplastids (opens in a new tab)

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