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Medicinal-Pharmaceutical Chemistry Commons

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Biochemistry

2014

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Articles 1 - 12 of 12

Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Ultrafast Interfacial Electron Transfer Across Molecule-Tio2 Nanocomposites: Towards Solar Cells And Two Photon Absorption, Edwin Mghanga Dec 2014

Ultrafast Interfacial Electron Transfer Across Molecule-Tio2 Nanocomposites: Towards Solar Cells And Two Photon Absorption, Edwin Mghanga

Dissertations

Interfacial charge transfer (ICT) across the molecule-TiO2 nanoparticle interface has gained enormous research attention for applications in dye sensitized solar cells (DSSC), photo-catalysis, water splitting and nonlinear optics. DSSCs are promising clean alternative energy sources. However, current DSSCs suffer from lower efficiencies and higher cost. Better understanding of the ICT processes in DSSCs can help solve these problems. We have used two strategies to understand ICT in the context of DSSCs. Firstly, we used a computationally validated anchor group, acetylacetonate (acac) to bind molecules to the semiconductor surface and facilitate charge separation. Secondly, we used natural dye sensitizers, which possess ...


Discovery And Characterization Of A Potent And Selective Inhibitory Of Aedes Aegypti Inward Rectifier Potassium Channels, Matthew F. Rouhier, Rene Raphemot, Daniel R. Swale, Emily Days, C. David Weaver, Kimberly M. Lovell, Leah C. Konkel, Darren W. Engers, Sean F. Bollinger, Corey Hopkins, Peter M. Piermarini, Jerod S. Denton Nov 2014

Discovery And Characterization Of A Potent And Selective Inhibitory Of Aedes Aegypti Inward Rectifier Potassium Channels, Matthew F. Rouhier, Rene Raphemot, Daniel R. Swale, Emily Days, C. David Weaver, Kimberly M. Lovell, Leah C. Konkel, Darren W. Engers, Sean F. Bollinger, Corey Hopkins, Peter M. Piermarini, Jerod S. Denton

Faculty Publications

Vector-borne diseases such as dengue fever and malaria, which are transmitted by infected female mosquitoes, affect nearly half of the world's population. The emergence of insecticide-resistant mosquito populations is reducing the effectiveness of conventional insecticides and threatening current vector control strategies, which has created an urgent need to identify new molecular targets against which novel classes of insecticides can be developed. We previously demonstrated that small molecule inhibitors of mammalian Kir channels represent promising chemicals for new mosquitocide development. In this study, high-throughput screening of approximately 30,000 chemically diverse small-molecules was employed to discover potent and selective inhibitors ...


Peptidylarginine Deiminases: Novel Drug Targets For Prevention Of Neuronal Damage Following Hypoxic Ischemic Insult (Hi) In Neonates., Sigrun Lange, Eridan Rocha-Ferreira, Laura Thei, Priyanka Mawjee, Kate Bennett, Paul R. Thompson, Venkataraman Subramanian, Anthony P. Nicholas, Donald Peebles, Mariya Hristova, Gennadij Raivich Aug 2014

Peptidylarginine Deiminases: Novel Drug Targets For Prevention Of Neuronal Damage Following Hypoxic Ischemic Insult (Hi) In Neonates., Sigrun Lange, Eridan Rocha-Ferreira, Laura Thei, Priyanka Mawjee, Kate Bennett, Paul R. Thompson, Venkataraman Subramanian, Anthony P. Nicholas, Donald Peebles, Mariya Hristova, Gennadij Raivich

Thompson Lab Publications

Neonatal hypoxic ischaemic (HI) injury frequently causes neural impairment in surviving infants. Our knowledge of the underlying molecular mechanisms is still limited. Protein deimination is a post-translational modification caused by Ca(+2) -regulated peptidylarginine deiminases (PADs), a group of five isozymes that display tissue-specific expression and different preference for target proteins. Protein deimination results in altered protein conformation and function of target proteins, and is associated with neurodegenerative diseases, gene regulation and autoimmunity. In this study, we used the neonatal HI and HI/infection [lipopolysaccharide (LPS) stimulation] murine models to investigate changes in protein deimination. Brains showed increases in deiminated ...


Modulation Of Calcium-Induced Cell Death In Human Neural Stem Cells By The Novel Peptidylarginine Deiminase-Aif Pathway., Kin Pong U, Venkataraman Subramanian, Antony P. Nicholas, Paul R. Thompson, Patrizia Ferretti Jun 2014

Modulation Of Calcium-Induced Cell Death In Human Neural Stem Cells By The Novel Peptidylarginine Deiminase-Aif Pathway., Kin Pong U, Venkataraman Subramanian, Antony P. Nicholas, Paul R. Thompson, Patrizia Ferretti

Thompson Lab Publications

PADs (peptidylarginine deiminases) are calcium-dependent enzymes that change protein-bound arginine to citrulline (citrullination/deimination) affecting protein conformation and function. PAD up-regulation following chick spinal cord injury has been linked to extensive tissue damage and loss of regenerative capability. Having found that human neural stem cells (hNSCs) expressed PAD2 and PAD3, we studied PAD function in these cells and investigated PAD3 as a potential target for neuroprotection by mimicking calcium-induced secondary injury responses. We show that PAD3, rather than PAD2 is a modulator of cell growth/death and that PAD activity is not associated with caspase-3-dependent cell death, but is required ...


Application Of Diarylhydrazones, Schiff-Bases And Their Saturated Derivatives As Multifunctional Inhibitors Of Amyloid Self-Assembly, Christian Schafer, Sanjukta Ghosh, Marianna Torok, Bela Torok May 2014

Application Of Diarylhydrazones, Schiff-Bases And Their Saturated Derivatives As Multifunctional Inhibitors Of Amyloid Self-Assembly, Christian Schafer, Sanjukta Ghosh, Marianna Torok, Bela Torok

UMass Center for Clinical and Translational Science Research Retreat

A new class of multifunctional small molecule inhibitors of amyloid self-assembly is described. Several compounds, based on the diarylhydrazone scaffold were designed. Forty-four substituted derivatives of this core structure were synthesized using a variety of benzaldehydes and phenylhydrazines and were characterized. The inhibitor candidates were evaluated in multiple assays, including the inhibition of A fibrillogenesis and the disassembly of preformed fibrils. The hydrazone scaffold showed strong activity in inhibiting the amyloid beta self-assembly. The structure-activity relationship revealed that the substituents on the aromatic rings had considerable effect on the overall activity of the compounds. In order to identify possible functional ...


Branching Into Rnai: Synthesis, Characterization And Biology Of Branch And Hyperbranch Sirnas, Anthony Muriithi Maina May 2014

Branching Into Rnai: Synthesis, Characterization And Biology Of Branch And Hyperbranch Sirnas, Anthony Muriithi Maina

Seton Hall University Dissertations and Theses (ETDs)

The cancer epidemic continues to afflict millions of humans world-wide each year and despite a renewed hope with the development of new and improved forms of therapy, a cure for cancer remains an elusive goal. This is partly related to the rise of resilient forms of tumors that have evolved with resistance towards conventional chemotherapy and radiation treatments. Moreover, these non-specific therapeutic regimens are highly toxic, leading to severe immunosuppressive effects which poisons the body and compromises the road towards remission. In an effort to mitigate these limitations, cancer-targeting approaches are currently experiencing a renaissance in the translation of new ...


Metal Stopping Reagents Facilitate Discontinuous Activity Assays Of The De Novo Purine Biosynthesis Enzyme Pure, Kelly L. Sullivan, Loredana C. Huma, Elwood Mullins, Michael E. Johnson, T. Joseph Kappock May 2014

Metal Stopping Reagents Facilitate Discontinuous Activity Assays Of The De Novo Purine Biosynthesis Enzyme Pure, Kelly L. Sullivan, Loredana C. Huma, Elwood Mullins, Michael E. Johnson, T. Joseph Kappock

Department of Biochemistry Faculty Publications

The conversion of 5-aminoimidazole ribonucleotide (AIR) to 4-carboxy-AIR (CAIR) represents an unusual divergence in purine biosynthesis: microbes and nonmetazoan eukaryotes use class I PurEs while animals use class II PurEs. Class I PurEs are therefore a potential antimicrobial target; however, no enzyme activity assay is suitable for high throughput screening (HTS). Here we report a simple chemical quench that fixes the PurE substrate/product ratio for 24 h, as assessed by the Bratton-Marshall assay (BMA) for diazotizable amines. The ZnSO4 stopping reagent is proposed to chelate CAIR, enabling delayed analysis of this acid-labile product by BMA or other HTS ...


Ligand-Receptor Interactions For Supramolecular Disassembly With Applications In Screening And Drug Delivery, Diego Amado Torres Jan 2014

Ligand-Receptor Interactions For Supramolecular Disassembly With Applications In Screening And Drug Delivery, Diego Amado Torres

Doctoral Dissertations

Proteins have the capacity to bind specific sets of compounds known as ligands, these are small molecules with a recurrent theme in their molecular design that is a characteristic exploited here to (i) identify particular affinities of small molecules for proteins with the aim of using them as ligands, inhibitors, or targeting moieties in more complex systems by means of a methodology that screens small molecules based on protein affinity; (ii) decorate a self-assembling supramolecular system at different positions, making it responsive to a complementary protein with the aim of exploring differences in disassembly and sensitivity of the release of ...


Further Characterization Of A Secreted Lipase From The Human Pathogen Leishmania Donovani By Determining The Effect Of Various Metal Ions On Its Enzymatic Activity., Lana Hoertz Jan 2014

Further Characterization Of A Secreted Lipase From The Human Pathogen Leishmania Donovani By Determining The Effect Of Various Metal Ions On Its Enzymatic Activity., Lana Hoertz

Pell Scholars and Senior Theses

Leishmania donovani, a protozoan parasite, is the causative agent of the often fatal disease visceral leishmaniasis. The current treatments available are minimal and toxic to the patient. It has been shown that these organisms exhibit lipolytic activity during their growth in vitro. Lipases are enzymes that are known to aid in the development and virulence of several pathogenic organisms such as Candida albicans and Staphylococcus warneri. Little information is known, however, about the role of lipases in Leishmania species. We hypothesize that lipase may play a part in Leishmania's ability to survive within the human host as well as ...


Characterization Of Gold Nanoparticle Antimicrobials, Kelsey Higgins Jan 2014

Characterization Of Gold Nanoparticle Antimicrobials, Kelsey Higgins

Chemistry & Biochemistry Graduate Theses & Dissertations (1986-2018)

Nanoparticles have been gaining recognition for their potential in drug delivery; however, now a new niche is growing. Nanoparticles are no longer simply carrying a drug, but rather being designed as the therapeutic itself. The Feldheim group has designed gold nanoparticles functionalized with an array of organothiol ligands varying in intermolecular forces, hydrophilicity and functional groups. Optimization of this library of drug nanoparticles produced drug nanoparticles with a bacteriostatic effect against bacteria, such as E. Coli and Klebsiella. There are still many pieces of the puzzle to address. This thesis presents research conducted to 1) Explore which parameter during the ...


Crystal Structure Of The Neisseria Gonorrhoeae Mtrd Inner Membrane Multidrug Efflux Pump, Jani Reddy Bolla, Chih-Chia Su, Sylvia V. Do, Pattathil Radhakrishnan, Nitin Kumar, Feng Long, Tsung-Han Chou, Jared A. Delmar, Hsiang-Ting Lei, Kanagalaghatta R. Rajashankar, William M. Shafer, Edward Yu Jan 2014

Crystal Structure Of The Neisseria Gonorrhoeae Mtrd Inner Membrane Multidrug Efflux Pump, Jani Reddy Bolla, Chih-Chia Su, Sylvia V. Do, Pattathil Radhakrishnan, Nitin Kumar, Feng Long, Tsung-Han Chou, Jared A. Delmar, Hsiang-Ting Lei, Kanagalaghatta R. Rajashankar, William M. Shafer, Edward Yu

Physics and Astronomy Publications

Neisseria gonorrhoeae is an obligate human pathogen and the causative agent of the sexually-transmitted disease gonorrhea. The control of this disease has been compromised by the increasing proportion of infections due to antibiotic-resistant strains, which are growing at an alarming rate. The MtrCDE tripartite multidrug efflux pump, belonging to the hydrophobic and amphiphilic efflux resistance-nodulation-cell division (HAE-RND) family, spans both the inner and outer membranes of N. gonorrhoeae and confers resistance to a variety of antibiotics and toxic compounds. We here report the crystal structure of the inner membrane MtrD multidrug efflux pump, which reveals a novel structural feature that ...


Crystal Structure Of The Open State Of The Neisseria Gonorrhoeae Mtre Outer Membrane Channel, Hsiang-Ting Lei, Tsung-Han Chou, Chih-Chia Su, Jani Reddy Bolla, Nitin Kumar, Pattathil Radhakrishnan, Feng Long, Jared A. Delmar, Sylvia V. Do, Kanagalaghatta R. Rajashankar, William M. Shafer, Edward Yu Jan 2014

Crystal Structure Of The Open State Of The Neisseria Gonorrhoeae Mtre Outer Membrane Channel, Hsiang-Ting Lei, Tsung-Han Chou, Chih-Chia Su, Jani Reddy Bolla, Nitin Kumar, Pattathil Radhakrishnan, Feng Long, Jared A. Delmar, Sylvia V. Do, Kanagalaghatta R. Rajashankar, William M. Shafer, Edward Yu

Physics and Astronomy Publications

Active efflux of antimicrobial agents is one of the most important strategies used by bacteria to defend against antimicrobial factors present in their environment. Mediating many cases of antibiotic resistance are transmembrane efflux pumps, composed of one or more proteins. The Neisseria gonorrhoeae MtrCDE tripartite multidrug efflux pump, belonging to the hydrophobic and amphiphilic efflux resistance-nodulation-cell division (HAE-RND) family, spans both the inner and outer membranes of N. gonorrhoeae and confers resistance to a variety of antibiotics and toxic compounds. We here describe the crystal structure of N. gonorrhoeae MtrE, the outer membrane component of the MtrCDE tripartite multidrug efflux ...