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High Yield Synthesis Of Positron Emission Tomography Ligands For Metabotropic Glutamate Receptor Imaging, Saraanne E. Hitchcock 2011 University of Nebraska-Lincoln

High Yield Synthesis Of Positron Emission Tomography Ligands For Metabotropic Glutamate Receptor Imaging, Saraanne E. Hitchcock

Student Research Projects, Dissertations, and Theses - Chemistry Department

Positron Emission Tomography (PET) is a powerful and non-invasive imaging technique used for human and animal organ imaging. Currently, the market for PET is project to reach $5.4 billion per year by 2015.5 This research focuses on the direct incorporation of [18F]-fluoride into PET ligands. The widespread use of PET imaging is currently frustrated, in part, by the lack of efficient fluorination chemistry.

Glutamate, one of the 20 most abundant naturally occurring amino acids, serves as a neurotransmitter in the central nervous system. Glutamate functions in this capacity by binding to ionotropic and metabotropic receptors. Metabotropic receptors ...


Application Of Raman Spectroscopy To Lubricants, Lubricated Surfaces And Lubrication Phenomena, David W. Johnson 2011 University of Dayton

Application Of Raman Spectroscopy To Lubricants, Lubricated Surfaces And Lubrication Phenomena, David W. Johnson

Chemistry Faculty Publications

Recent advances in lasers and detector technologies and the development of low-cost instruments and fiber-optic probes have brought about an explosion in the lubrication systems being studied by Raman spectroscopy. This article provides examples of the use of Raman spectroscopy in the study of lubrication phenomena, including the characterization of liquid lubricants, lubricant additives, and solid lubricants; the study of vapor-phase lubrication; and the use of coated nanoparticles as lubricants.


Genome-Wide Analysis Reveals Padi4 Cooperates With Elk-1 To Activate C-Fos Expression In Breast Cancer Cells., Xuesen Zhang, Matthew J. Gamble, Sonja Stadler, Brian D. Cherrington, Corey P. Causey, Paul R. Thompson, Mark S. Roberson, W Lee Kraus, Scott A. Coonrod 2011 Cornell University

Genome-Wide Analysis Reveals Padi4 Cooperates With Elk-1 To Activate C-Fos Expression In Breast Cancer Cells., Xuesen Zhang, Matthew J. Gamble, Sonja Stadler, Brian D. Cherrington, Corey P. Causey, Paul R. Thompson, Mark S. Roberson, W Lee Kraus, Scott A. Coonrod

Thompson Lab Publications

Peptidylarginine deiminase IV (PADI4) catalyzes the conversion of positively charged arginine and methylarginine residues to neutrally charged citrulline, and this activity has been linked to the repression of a limited number of target genes. To broaden our knowledge of the regulatory potential of PADI4, we utilized chromatin immunoprecipitation coupled with promoter tiling array (ChIP-chip) analysis to more comprehensively investigate the range of PADI4 target genes across the genome in MCF-7 breast cancer cells. Results showed that PADI4 is enriched in gene promoter regions near transcription start sites (TSSs); and, surprisingly, this pattern of binding is primarily associated with actively transcribed ...


Electrochemistry Of Technetium Analogues Rhenium And Molybdenum In Room Temperature Ionic Liquid, Pauline Nancy Serrano 2011 University of Nevada, Las Vegas

Electrochemistry Of Technetium Analogues Rhenium And Molybdenum In Room Temperature Ionic Liquid, Pauline Nancy Serrano

UNLV Theses, Dissertations, Professional Papers, and Capstones

Rhenium was used as an analog for Technetium to study the electrochemical redox properties because the two elements share the same stable oxidation states in aqueous solutions. However, Tc-99 is radioactive and is not readily available for experimentation purposes. Molybdenum is also of interest because when Mo-99 is irradiated, the decay products are Tc-99m and Tc-99. Approximately 30% Tc-99m is eluted from the Mo columns for radiopharmaceutical use with the remaining Mo-99 source decaying to Tc-99 which is discarded as radioactive hospital waste. Currently there are no viable procedures for the reclamation of the radioactive Tc-99 from either fission streams ...


Thermochemistry And Bond Energies Of Acetohydrazide, Amides And Cyclic Alkyl Ethers, Sumit Charaya 2011 New Jersey Institute of Technology

Thermochemistry And Bond Energies Of Acetohydrazide, Amides And Cyclic Alkyl Ethers, Sumit Charaya

Theses

Structure, thermochemical properties, bond energies and internal rotation potentials of Acetic Acid Hydrazide (CH3CONHNH2), Acetamide (CH3CONH2) and N-methyl Acetamide (CH3CONHCH3) and their radicals corresponding to loss of hydrogen atom have been studied. Gas phase standard enthalpies of formation and bond energies were calculated using the DFT methods B3LYP/6-31G(d,p), B3LYP/6-31G(2d,2p) and the composite CBS-QB3 methods employing a series of work reactions to further improve accuracy of the ΔHf°(298K). Molecular structures, vibration frequencies and internal rotor potentials were calculated at DFT level. The enthalpies of the parent molecules ...


Synthesis Towards Synthetic Adenosine Receptor, Rajni Gupta 2011 New Jersey Institute of Technology

Synthesis Towards Synthetic Adenosine Receptor, Rajni Gupta

Theses

Adenosine is a biologically important molecule as it acts as local modulator with cytoprotective function in the body. Adenosine accumulates in the extracellular space in response to metabolic stress and cell damage, and elevations in extracellular adenosine level are found in conditions like myocardial ischemia, hypoxia, inflammation and trauma. Its abnormal concentration therefore could be a marker of many diseases. Therefore determining its concentration can help understand the physiological state of the body. However its selective detection by synthetic receptors is not possible till date.

Efforts have been made here to design molecular tweezer for adenosine. Multistep synthesis was done ...


The Synthesis And Biological Evaluation Of Tamandarin B Analogs, Kenneth Lassen 2011 University of Pennsylvania

The Synthesis And Biological Evaluation Of Tamandarin B Analogs, Kenneth Lassen

Publicly Accessible Penn Dissertations

The tamandarin and didemnins are a class of cyclodepsipeptides that have shown a wide range of biological activity. The didemnins have demonstrated antitumor, antiviral and immunosuppressive activity at low nano- and femtomolar levels. Didemnin B was the first marine natural product to enter clinical trials in humans in the United States. The structures of tamandarins A and B were reported in 2000 and possess almost identical structure and biological activity to didemnin B. These compounds have shown impressive biological activity and some progress has been made in establishing structure-activity relationships. However, their molecular mechanism of action is still unclear. The ...


Synthesis Of A Resveratrol Glycinate Derivative., Shelley Marie Van Cleve 2011 East Tennessee State University

Synthesis Of A Resveratrol Glycinate Derivative., Shelley Marie Van Cleve

Electronic Theses and Dissertations

Recently, the compound resveratrol has had media attention as an anti carcinogen. However, the bioavailability of resveratrol is low in the human system due to its hydrophobic nature. Therefore, it must be administered in high dosages to be effective. A plethora of derivatives have been synthesized that have the potential of resveratrol but sadly share low bioavailability. The first effort of this research was an attempt to produce a more hydrophilic ester of resveratrol. Failing this, the final product was synthesized using a glycine derivative to produce 4-[(1E)-2-(3,5-diacetyloxyphenyl)ethenyl]phenyl N-[(1,1-dimethylethoxy)carbonyl]-glycinate.


Mechanistic Study Of The Small Molecule Inhibitor Dx-52-1, Junru Cui 2011 University of Connecticut

Mechanistic Study Of The Small Molecule Inhibitor Dx-52-1, Junru Cui

Master's Theses

Cell migration is a basic biological process that is fundamental to several normal and disease processes such as embryonic development, tissue repair, immune function, angiogenesis and cancer cell invasion and metastasis. Small organic molecules inhibiting cell migration can be used as both research probes and therapeutic agents. DX-52-1, a semisynthetic derivative of the natural product quinocarmycin (also known as quinocarcin), inhibits the migration of Madin-Darby canine kidney epithelial cells with nanomolar concentration. We have identified galectin-3, a multifunctional protein whose best-known function is its sugar binding ability, as a secondary target of DX-52-1 with functions in cell motility. In addition ...


In Vitro Activities Of Synthetic Host Defense Propeptides Processed By Neutrophil Elastase Against Cystic Fibrosis Pathogens., Stephane Desgranges, Florie Le Prieult, Alan Daly, Marian Brennan, Dilip K. Rai, Anusha P. Subasinghage, Chandralal M. Hewage, Sally-Ann Cryan, Catherine M. Greene, Noel G. McElvaney, Timothy P. Smyth, Deirdre Fitzgerald-Hughes, Hilary Humphreys, Marc Devocelle 2011 Royal College of Surgeons in Ireland

In Vitro Activities Of Synthetic Host Defense Propeptides Processed By Neutrophil Elastase Against Cystic Fibrosis Pathogens., Stephane Desgranges, Florie Le Prieult, Alan Daly, Marian Brennan, Dilip K. Rai, Anusha P. Subasinghage, Chandralal M. Hewage, Sally-Ann Cryan, Catherine M. Greene, Noel G. Mcelvaney, Timothy P. Smyth, Deirdre Fitzgerald-Hughes, Hilary Humphreys, Marc Devocelle

Chemistry Articles

The antimicrobial and hemolytic activities of a host defense peptide can be controlled by its modification as a propeptide of reduced net charge, which can then be processed by neutrophil elastase, a serine protease involved in chronic airway inflammation and infections associated with cystic fibrosis.


Theoretical Investigation Of A Reported Antibiotic From The 'Miracle Tree' Moringa Oleifera, Michael Horwath, Vladimir Benin 2011 University of Dayton

Theoretical Investigation Of A Reported Antibiotic From The 'Miracle Tree' Moringa Oleifera, Michael Horwath, Vladimir Benin

Chemistry Faculty Publications

Moringa oleifera, sometimes called the “Miracle Tree,” has received international attention for its potential to improve health in impoverished tropical areas. In addition to high vitamin content in the leaves and pods, the tree contains compounds with antioxidant and antibacterial properties. This study focused on the theoretical investigation of the suggested structure of one antibacterial compound, “pterygospermin,” whose existence was proposed after some studies of the roots of M. oleifera. The structure of pterygospermin was first proposed by a research group working in the 1950s, but later studies have not found evidence of this compound and have instead attributed the ...


A Sodium Salt Of The Dimer Of Boronoterephthalic Acid Anhydride, Scott Simmons, Albert Fratini, Vladimir Benin 2011 University of Dayton

A Sodium Salt Of The Dimer Of Boronoterephthalic Acid Anhydride, Scott Simmons, Albert Fratini, Vladimir Benin

Chemistry Faculty Publications

The title compound, sodium bis­(6-carb­oxy-1-hy­droxy-3-oxo-1,3-dihydro-2,1-benzoxaborol-1-yl)oxidanium, Na+·C16H15B2O13-, was prepared in two steps from 2-bromo-p-xylene. Its crystal structure was determined at 140 K and has triclinic (P) symmetry. The compound presents a unique structural motif, including two units of the cyclic anhydride of boronoterephthalic acid, joined by a protonated, and thereby trivalent, oxonium center. Association in the crystal is realized by complementary hydrogen bonding of the carboxyl groups, as well as by coordination of the sodium cations to the oxygen centers on the five-membered rings.


Detection Of Protein By Microdrop Analysis, Yogeshkumar Radadiya 2011 Governors State University

Detection Of Protein By Microdrop Analysis, Yogeshkumar Radadiya

All Capstone Projects

Analysis of protein depends particularly on protein concentration. Protein concentration measurement is the most important part in the research work to conduct protein-related studies. Although there are many methods available for this purpose, each method has certain limitations. The aim of the experiment is to develop either new or modified analytical method for the analysis and detection of protein using newly introduced micro-plate reader equipped with Take-3 microplate with the help of Gen-5 software. An ideal assay should be simple and easy to carry out. Another aspect to be taken into consideration are low inference, stability of measured components and ...


Organometallic Iron(Iii)-Salophene Exerts Cytotoxic Properties In Neuroblastoma Cells Via Mapk Activation And Ros Generation, Kyu Kwang Kim, Rakesh K. Singh, Robert M. Strongin, Richard G. Moore, Laurent Brard, Thilo S. Lange 2011 Brown University

Organometallic Iron(Iii)-Salophene Exerts Cytotoxic Properties In Neuroblastoma Cells Via Mapk Activation And Ros Generation, Kyu Kwang Kim, Rakesh K. Singh, Robert M. Strongin, Richard G. Moore, Laurent Brard, Thilo S. Lange

Chemistry Faculty Publications and Presentations

The objective of the present study was to investigate the specific effects of Iron(III)-salophene (Fe-SP) on viability, morphology, proliferation, cell cycle progression, ROS generation and pro-apoptotic MAPK activation in neuroblastoma (NB) cells. A NCI-DTP cancer screen revealed that Fe-SP displayed high toxicity against cell lines of different tumor origin but not tumor type-specificity. In a viability screen Fe-SP exhibited high cytotoxicity against all three NB cell lines tested. The compound caused cell cycle arrest in G1 phase, suppression of cells progressing through S phase, morphological changes, disruption of the mitochondrial membrane depolarization potential, induction of apoptotic markers as ...


Antisense-Induced Suppression Of Taxoid 14Β-Hydroxylase Gene Expression In Transgenic Taxus × Media Cells, Feng-Lan Li, Xiao-Jun Ma, Angela Hoffman, Jun-Gui Dai, De-You Qui 2011 University of Portland

Antisense-Induced Suppression Of Taxoid 14Β-Hydroxylase Gene Expression In Transgenic Taxus × Media Cells, Feng-Lan Li, Xiao-Jun Ma, Angela Hoffman, Jun-Gui Dai, De-You Qui

Chemistry Faculty Publications and Presentations

The enzyme taxoid 14β-hydroxylase (14OH) directs a side-route of taxol pathway to 14β-hydroxy taxoids. Suppression of this side-route could increase the production of taxol. To suppress taxoid 14β- hydroxylase gene (14OH) expression in theTaxus × media TM3 cell line, antisense RNA inhibition approach was used in this study. Following the construction of an antisense RNA expression vector of 14OH from Taxus chinensis, the antisense 14OH cDNA (as14OH) was introduced into TM3 cells by Agrobacterium tumefaciens-mediated transformation. Southern blot analysis of hygromycin phosphotransferase gene (HYG) revealed that this selection gene was integrated successfully into the genome of Taxus × media ...


Pharmacological Chaperoning In Fabry Disease, Jerome Rogich 2011 University of Massachusetts Amherst

Pharmacological Chaperoning In Fabry Disease, Jerome Rogich

Masters Theses 1911 - February 2014

Fabry Disease is an X-­‐linked lysosomal storage disorder characterized by a variety of symptoms including hypohydrosis, seizures, cardiac abnormalities, skin lesions, and chronic pain. These symptoms stem from a lack of functional endogenous α-­‐ Galactosidase A (α-­GAL), which leads to an accrual of its natural substrate. The severity of the disease symptoms can be directly correlated with the amount of residual enzyme activity. It has been shown that an imino sugar, 1-deoxygalactonojirimycin (DGJ), can increase enzymatic activity and clear excess substrate. This pH-­‐dependent chaperoning phenomenon is believed to arise from the presence of aspartic acid 170 in ...


Automated Sequence- And Stereo-Specific Assignment Of Methyl-Labeled Proteins By Paramagnetic Relaxation And Methyl–Methyl Nuclear Overhauser Enhancement Spectroscopy, Vincenzo Venditti, Nicolas L. Fawzi, G. Marius Clore 2011 National Institutes of Health

Automated Sequence- And Stereo-Specific Assignment Of Methyl-Labeled Proteins By Paramagnetic Relaxation And Methyl–Methyl Nuclear Overhauser Enhancement Spectroscopy, Vincenzo Venditti, Nicolas L. Fawzi, G. Marius Clore

Vincenzo Venditti

Methyl-transverse relaxation optimized spectroscopy is rapidly becoming the preferred NMR technique for probing structure and dynamics of very large proteins up to ~1 MDa in molecular size. Data interpretation, however, necessitates assignment of methyl groups which still presents a very challenging and time-consuming process. Here we demonstrate that, in combination with a known 3D structure, paramagnetic relaxation enhancement (PRE), induced by nitroxide spin-labels incorporated at only a few surface-exposed engineered cysteines, provides fast, straightforward and robust access to methyl group resonance assignments, including stereoassignments for the methyl groups of leucine and valine. Neither prior assignments, including backbone assignments, for the ...


A Structurally Driven Analysis Of Thiol Reactivity In Mammalian Albumins, Ottavia Spiga, Domenico Summa, Simone Cirri, Andrea Bernini, Vincenzo Venditti, Matteo De Chiara, Raffaella Priora, Simona Frosail, Antonios Margaritis, Danila Di Giuseppe, Paolo Di Simplicio, Neri Niccolai 2011 University of Siena

A Structurally Driven Analysis Of Thiol Reactivity In Mammalian Albumins, Ottavia Spiga, Domenico Summa, Simone Cirri, Andrea Bernini, Vincenzo Venditti, Matteo De Chiara, Raffaella Priora, Simona Frosail, Antonios Margaritis, Danila Di Giuseppe, Paolo Di Simplicio, Neri Niccolai

Vincenzo Venditti

Understanding the structural basis of protein redox activity is still an open question. Hence, by using a structural genomics approach, different albumins have been chosen to correlate protein structural features with the corresponding reaction rates of thiol exchange between albumin and disulfide DTNB. Predicted structures of rat, porcine, and bovine albumins have been compared with the experimentally derived human albumin. High structural similarity among these four albumins can be observed, in spite of their markedly different reactivity with DTNB. Sequence alignments offered preliminary hints on the contributions of sequence-specific local environments modulating albumin reactivity. Molecular dynamics simulations performed on experimental ...


Human Fatty Acid Transport Protein 2a/Very Long Chain Acyl-Coa Synthetase 1 (Fatp2a/Acsvl1) Has A Preference In Mediating The Channeling Of Exogenous N-3 Fatty Acids Into Phosphatidylinositol, Elaina M. Melton, Ronald Cerny, Paul A. Watkins, Concetta C. DiRusso, Paul N. Black 2011 University of Nebraska-Lincoln

Human Fatty Acid Transport Protein 2a/Very Long Chain Acyl-Coa Synthetase 1 (Fatp2a/Acsvl1) Has A Preference In Mediating The Channeling Of Exogenous N-3 Fatty Acids Into Phosphatidylinositol, Elaina M. Melton, Ronald Cerny, Paul A. Watkins, Concetta C. Dirusso, Paul N. Black

Ronald Cerny Publications

The trafficking of fatty acids across the membrane and into downstream metabolic pathways requires their activation to CoA thioesters. Members of the fatty acid transport protein/ very long chain acyl-CoA synthetase (FATP/Acsvl) family are emerging as key players in the trafficking of exogenous fatty acids into the cell and in intracellular fatty acid homeostasis.We have expressed two naturally occurring splice variants of human FATP2 (Acsvl1) in yeast and 293T-REx cells and addressed their roles in fatty acid transport, activation, and intracellular trafficking. Although both forms (FATP2a (Mr 70,000) and FATP2b (Mr 65,000 and lacking exon3, which ...


Overexpression Of Galnac-Transferase Galnac-T3 Promotes Pancreatic Cancer Cell Growth, Keisuke Taniuchi, Ronald Cerny, Aki Tanouchi, Kimitoshi Kohno, Norihiro Kotani, Koichi Honke, Toshiji Saibara, Michael A. Hollingsworth 2011 University of Nebraska Medical Center

Overexpression Of Galnac-Transferase Galnac-T3 Promotes Pancreatic Cancer Cell Growth, Keisuke Taniuchi, Ronald Cerny, Aki Tanouchi, Kimitoshi Kohno, Norihiro Kotani, Koichi Honke, Toshiji Saibara, Michael A. Hollingsworth

Ronald Cerny Publications

O-linked glycans of secreted and membrane bound proteins play an important role in the pathogenesis of pancreatic cancer by modulating immune responses, inflammation, and tumorigenesis. A critical aspect of O-glycosylation, the position at which proteins are glycosylated with N-acetyl-galactosamine on serine and threonine residues, is regulated by the substrate specificity of UDP-GalNAc: polypeptide N-acetylgalactosaminyl-transferases (GalNAc-Ts). Thus, GalNAc-Ts regulate the first committed step in O-glycosylated protein biosynthesis, determine sites of O-glycosylation on proteins, and are important for understanding normal and carcinoma-associated O-glycosylation. We have found that one of these enzymes, GalNAc-T3, is overexpressed in ...


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