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Articles 1 - 8 of 8
Full-Text Articles in Physical Sciences and Mathematics
Sequence-Specific And Conformation-Specific Targeting Of Duplex And Quadruplex Dna Grooves With Small Molecules, Rupesh K. Nanjunda
Sequence-Specific And Conformation-Specific Targeting Of Duplex And Quadruplex Dna Grooves With Small Molecules, Rupesh K. Nanjunda
Chemistry Dissertations
Small molecule mediated chemical intervention of biological processes using nucleic acid targets has proven extremely successful and is continually providing exciting new avenues for the development of anti-cancer agents and molecular probes. Among the alternative DNA confrormations, G-quadruplexes has certainly garnered much recognition due to increase in evidences supporting their involvement in diverse biological process. The grooves of the quadruplexes offer an alternate recognition site for ligand interactions with potentially higher selectivity than the traditional terminal stacking sites. DB832, a bifuryl-phenyl diamidine, was recently reported to selectively recognize human telomeric G-quadruplex, as a stacked species, with significant selectivity over duplex …
Rational Drug Design For Neglected Diseases: Implementation Of Computational Methods To Construct Predictive Devices And Examine Mechanisms, Catharine Jane Collar
Rational Drug Design For Neglected Diseases: Implementation Of Computational Methods To Construct Predictive Devices And Examine Mechanisms, Catharine Jane Collar
Chemistry Dissertations
Over a billion individuals worldwide suffer from neglected diseases. This equates to approximately one-sixth of the human population. These infections are often endemic in remote tropical regions of impoverished populations where vectors can flourish and infected individuals cannot be effectively treated due to a lack of hospitals, medical equipment, drugs, and trained personnel. The few drugs that have been approved for the treatments of such illnesses are not widely used because they are riddled with inadequate implications of cost, safety, drug availability, administration, and resistance. Hence, there exists an eminent need for the design and development of improved new therapeutics. …
Design And Synthesis Of Novel Serotonin Receptor Ligands, Jeffrey D. Klenc
Design And Synthesis Of Novel Serotonin Receptor Ligands, Jeffrey D. Klenc
Chemistry Dissertations
Novel and potent ligands to the serotonin7 (5-HT7) receptor have been synthesized. The synthesized compounds include a set of substituted pyrimidines which show high affinity to the 5-HT7 receptor, synthesized by previously described methods [1,2] in high yield. Comparing the affinities of substituted pyrimidines to previously calculated models [3,4] yielded new hypotheses about the nature of interaction between the pyrimidine ligands and the 5-HT7 binding site. Several new series of compounds were synthesized by various methods to validate these hypotheses, including a conjugate addition to vinylpyrimidines [5]. These compounds include benzofurans, oximes, hydrazones, as well as a group of substituted …
Bead Modeling Of Transport Properties Of Macromolecules In Free Solution And In A Gel, Hongxia Pei
Bead Modeling Of Transport Properties Of Macromolecules In Free Solution And In A Gel, Hongxia Pei
Chemistry Dissertations
On the bead modeling methodology, or BMM, a macromolecule is modeled as a rigid, non-overlapping bead array with arbitrary radii. The BMM approach was pioneered by Kirkwood and coworkers (Kirkwood, J.G., Macromolecules, E.P. Auer (Ed.), Gordon and Breach, New York, 1967; Kirkwood, J.G., Riseman, J., J. Chem. Phys., 1948, 16, 565) and applied to such transport properties as diffusion, sedimentation, and viscosity. With the availability of computers, a number of investigators extended the work to account for the detailed shape of biomolecules in the 1970s. A principle objective of my research has been to apply the BMM approach to more …
Design, Synthesis And Mechanistic Studies Of Small Molecule Inhibitors Of The Hypoxia Inducible Factor Pathway, Suazette Reid Mooring
Design, Synthesis And Mechanistic Studies Of Small Molecule Inhibitors Of The Hypoxia Inducible Factor Pathway, Suazette Reid Mooring
Chemistry Dissertations
Cancer accounts for nearly one-quarter of deaths in the United States, exceeded only by heart diseases. In 2006, there were 559,888 cancer deaths in the US. Finding effective treatments for cancer is a major challenge among researchers. In solid tumor, hypoxia increases the progression of malignancy and metastasis by promoting angiogenesis. The transcription factor HIF-1 is responsible for the regulation of cellular processes, including glycolysis and angiogenesis. Clinical evidence has determined that expression of HIF-1 is strongly associated with poor patient prognosis. Also, activation of HIF-1 contributes to malignant behavior and therapeutic resistance. In view of these observations, there is …
Synthesis Of Fused Heterocyclic Diamidines For The Treatment Of Human African Trypanosomiasis And Fluorescence Studies Of Selected Diamidines, Jennifer Crystal Brown Barber
Synthesis Of Fused Heterocyclic Diamidines For The Treatment Of Human African Trypanosomiasis And Fluorescence Studies Of Selected Diamidines, Jennifer Crystal Brown Barber
Chemistry Dissertations
A class of linear diamidines was synthesized for the evaluation as a treatment of Human African Trypanosomiasis. These fused heterocyclic compounds are thiazole[5,4-d]thiazoles and are of interest because the parent compound, 2,5-Bis(4-amidinophenyl)-thiazolo[5,4-d]thiazole HCl salt, which is also called DB 1929, has exhibited a low nanomolar IC50 value against Trypanosoma brucei rhodesiense and has shown selectivity for binding to the human telomere G-quadruplex over that of DNA duplex. A fluoro and a methoxy derivative have been synthesized and are currently undergoing testing for activity and binding affinity. In addition, fluorescence studies of selected diamidines were done to study the effect of …
On The Catalytic Roles Of His351, Asn510, And His466 In Choline Oxidase And The Kinetic Mechanism Of Pyranose 2-Oxidase, Kunchala Rungsrisuriyachai
On The Catalytic Roles Of His351, Asn510, And His466 In Choline Oxidase And The Kinetic Mechanism Of Pyranose 2-Oxidase, Kunchala Rungsrisuriyachai
Chemistry Dissertations
Choline oxidase (E.C. 1.1.3.17) from Arthrobacter globiformis catalyzes the four-electron oxidation of choline to glycine betaine (N,N,N-trimethylglycine) via two sequential, FAD-dependent reactions in which betaine aldehyde is formed as an enzyme-bound intermediate. In each oxidative half-reaction, molecular oxygen acts as electron acceptor and is converted into hydrogen peroxide. Biochemical, structural, and mechanistic studies on the wild-type and a number of mutant variants of choline oxidase have recently been carried out, allowing for the depiction of the mechanism of alcohol oxidation catalyzed by the enzyme. Catalysis by choline oxidase is initiated by the removal of the hydroxyl proton of alcohol substrate …
Roles Of Serine 101, Histidine 310 And Valine 464 In The Reaction Catalyzed By Choline Oxidase From Arthrobacter Globiformis, Steffan Finnegan
Roles Of Serine 101, Histidine 310 And Valine 464 In The Reaction Catalyzed By Choline Oxidase From Arthrobacter Globiformis, Steffan Finnegan
Chemistry Dissertations
The enzymatic oxidation of choline to glycine betaine is of interest because organisms accumulate glycine betaine intracellularly in response to stress conditions, as such it is of potential interest for the genetic engineering of crops that do not naturally possess efficient pathways for the synthesis of glycine betaine, and for the potential development of drugs that target the glycine betaine biosynthetic pathway in human pathogens. To date, one of the best characterized enzymes belonging to this pathway is the flavin-dependent choline oxidase from Arthrobacter globiformis. In this enzyme, choline oxidation proceeds through two reductive half-reactions and two oxidative half-reactions. In …