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Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Microfilariae Of Brugia Malayi Inhibit The Mtor Pathway And Induce Autophagy In Human Dendritic Cells, Prakash Babu Narasimhan, Sasisekhar Bennuru, Zhaojing Meng, Rachel N Cotton, Kathleen R Elliott, Sundar Ganesan, Renee Mcdonald-Fleming, Timothy Veenstra, Thomas B Nutman, Roshanak Tolouei Semnani Sep 2019

Microfilariae Of Brugia Malayi Inhibit The Mtor Pathway And Induce Autophagy In Human Dendritic Cells, Prakash Babu Narasimhan, Sasisekhar Bennuru, Zhaojing Meng, Rachel N Cotton, Kathleen R Elliott, Sundar Ganesan, Renee Mcdonald-Fleming, Timothy Veenstra, Thomas B Nutman, Roshanak Tolouei Semnani

Timothy Veenstra, Ph.D.

Immune modulation is a hallmark of patent filarial infection, including suppression of antigen-presenting cell function and downmodulation of filarial antigen-specific T cell responses. The mammalian target of rapamycin (mTOR) signaling pathway has been implicated in immune regulation, not only by suppressing T cell responses but also by regulating autophagy (through mTOR sensing amino acid availability). Global proteomic analysis (liquid chromatography-tandem mass spectrometry) of microfilaria (mf)-exposed monocyte-derived dendritic cells (DC) indicated that multiple components of the mTOR signaling pathway, including mTOR, eIF4A, and eIF4E, are downregulated by mf, suggesting that mf target this pathway for immune modulation in DC. Utilizing ...


Mechanism For Apobec3g Catalytic Exclusion Of Rna And Non-Substrate Dna, William C. Solomon, Wazo Myint, Shurong Hou, Tapan Kanai, Rashmi Tripathi, Nese Kurt Yilmaz, Celia A. Schiffer, Hiroshi Matsuo Aug 2019

Mechanism For Apobec3g Catalytic Exclusion Of Rna And Non-Substrate Dna, William C. Solomon, Wazo Myint, Shurong Hou, Tapan Kanai, Rashmi Tripathi, Nese Kurt Yilmaz, Celia A. Schiffer, Hiroshi Matsuo

Schiffer Lab Publications

The potent antiretroviral protein APOBEC3G (A3G) specifically targets and deaminates deoxycytidine nucleotides, generating deoxyuridine, in single stranded DNA (ssDNA) intermediates produced during HIV replication. A non-catalytic domain in A3G binds strongly to RNA, an interaction crucial for recruitment of A3G to the virion; yet, A3G displays no deamination activity for cytidines in viral RNA. Here, we report NMR and molecular dynamics (MD) simulation analysis for interactions between A3Gctd and multiple substrate or non-substrate DNA and RNA, in combination with deamination assays. NMR ssDNA-binding experiments revealed that the interaction with residues in helix1 and loop1 (T201-L220) distinguishes the binding mode of ...


Development Of A Screening Method For Drugs Of Abuse By Direct Analysis Of Dried Urine Spots Coupled To Mass Spectrometry, Melanie Goldstein Aug 2019

Development Of A Screening Method For Drugs Of Abuse By Direct Analysis Of Dried Urine Spots Coupled To Mass Spectrometry, Melanie Goldstein

Student Theses

Fast and easy screening procedures are essential in any forensic toxicology laboratory to differentiate negative samples from presumptive positive cases. Immunoassay techniques, such as enzyme multiplied immunoassay technique (EMIT), are routinely employed as screening procedures. However, these techniques lack specificity (only differentiate group of drugs and not individual compounds) and it is difficult to add new compounds to the panel. Direct analysis of dried urine spots (DUS) by mass spectrometry (MS) offers a novel strategy to overcome these issues. DUS offer an improved storage alternative for biological samples, reducing costs and space requirements. In this work, an original method to ...


Molecular And Structural Mechanism Of Pan-Genotypic Hcv Ns3/4a Protease Inhibition By Glecaprevir, Jennifer Timm, Klajdi Kosovrasti, Mina Henes, Florian Leidner, Shurong Hou, Akbar Ali, Nese Kurt Yilmaz, Celia A. Schiffer Jul 2019

Molecular And Structural Mechanism Of Pan-Genotypic Hcv Ns3/4a Protease Inhibition By Glecaprevir, Jennifer Timm, Klajdi Kosovrasti, Mina Henes, Florian Leidner, Shurong Hou, Akbar Ali, Nese Kurt Yilmaz, Celia A. Schiffer

University of Massachusetts Medical School Faculty Publications

Hepatitis C virus (HCV), causative agent of chronic viral hepatitis, infects 71 million people worldwide and is divided into seven genotypes and multiple subtypes with sequence identities between 68 to 82%. While older generation direct-acting antivirals (DAAs) had varying effectiveness against different genotypes, the newest NS3/4A protease inhibitors including glecaprevir (GLE) have pan-genotypic activity. The structural basis for pan-genotypic inhibition and effects of polymorphisms on inhibitor potency were not well known due to lack of crystal structures of GLE-bound NS3/4A or genotypes other than 1. In this study, we determined the crystal structures of NS3/4A from genotypes ...


Poly(Ethylene Glycol)-Based Peptidomimetic "Pegtide" Of Oligo-Arginine Allows For Efficient Sirna Transfection And Gene Inhibition., Alan Hibbitts, Aoife M O'Connor, Joanna Mccarthy, Éanna B Forde, Gary Hessman, Caitriona M O'Driscoll, Sally-Ann Cryan, Marc Devocelle Jun 2019

Poly(Ethylene Glycol)-Based Peptidomimetic "Pegtide" Of Oligo-Arginine Allows For Efficient Sirna Transfection And Gene Inhibition., Alan Hibbitts, Aoife M O'Connor, Joanna Mccarthy, Éanna B Forde, Gary Hessman, Caitriona M O'Driscoll, Sally-Ann Cryan, Marc Devocelle

Chemistry Articles

While a wide range of experimental and commercial transfection reagents are currently available, persistent problems remain regarding their suitability for continued development. These include the transfection efficiency for difficult-to-transfect cell types and the risks of decreased cell viability that may arise from any transfection that does occur. Therefore, research is now turning toward alternative molecules that improve the toxicity profile of the gene delivery vector (GDV), while maintaining the transfection efficiency. Among them, cell-penetrating peptides, such as octa-arginine, have shown significant potential as GDVs. Their pharmacokinetic and pharmacodynamic properties can be enhanced through peptidomimetic conversion, whereby a peptide is modified ...


Integration Of Random Forest Classifiers And Deep Convolutional Neural Networks For Classification And Biomolecular Modeling Of Cancer Driver Mutations, Steve Agajanian, Odeyemi Oluyemi, Gennady M. Verkhivker Jun 2019

Integration Of Random Forest Classifiers And Deep Convolutional Neural Networks For Classification And Biomolecular Modeling Of Cancer Driver Mutations, Steve Agajanian, Odeyemi Oluyemi, Gennady M. Verkhivker

Mathematics, Physics, and Computer Science Faculty Articles and Research

Development of machine learning solutions for prediction of functional and clinical significance of cancer driver genes and mutations are paramount in modern biomedical research and have gained a significant momentum in a recent decade. In this work, we integrate different machine learning approaches, including tree based methods, random forest and gradient boosted tree (GBT) classifiers along with deep convolutional neural networks (CNN) for prediction of cancer driver mutations in the genomic datasets. The feasibility of CNN in using raw nucleotide sequences for classification of cancer driver mutations was initially explored by employing label encoding, one hot encoding, and embedding to ...


Determination Of Anxiolytic And Antidepressant Medicines In New York City Wastewater Samples, Jasmine J. Gayle May 2019

Determination Of Anxiolytic And Antidepressant Medicines In New York City Wastewater Samples, Jasmine J. Gayle

Student Theses

Wastewater-based epidemiology (WBE) provides information about a population’s exposure to certain chemical agents, such as drugs of abuse and medicines, by the analysis of human biomarkers, also known as excretion products, in wastewater samples. Although this is a growing field worldwide, mainly in Europe, Oceania, and Asia, limited data from the US are currently available. We developed and validated an analytical method to quantitatively and qualitatively determine the presence of commonly prescribed drugs to treat anxiety (alprazolam, buspirone, clonazepam, lorazepam, and propranolol) and depression (bupropion, citalopram, clomipramine, duloxetine, fluoxetine, imipramine, paroxetine, sertraline, and venlafaxine) in wastewater using liquid chromatography ...


Rapid Characterization Of Formulated Pharmaceuticals Using Fast Mas 1h Solid-State Nmr Spectroscopy, David A. Hirsh, Anuradha V. Wijesekara, Scott L. Carnahan, Ivan Hung, Joseph W. Lubach, Karthik Nagapudi, Aaron J. Rossini May 2019

Rapid Characterization Of Formulated Pharmaceuticals Using Fast Mas 1h Solid-State Nmr Spectroscopy, David A. Hirsh, Anuradha V. Wijesekara, Scott L. Carnahan, Ivan Hung, Joseph W. Lubach, Karthik Nagapudi, Aaron J. Rossini

Chemistry Publications

Active pharmaceutical ingredients (APIs) can be prepared in many different solid forms and phases that affect their physicochemical properties and suitability for oral dosage forms. The development and commercialization of dosage forms require analytical techniques that can determine and quantify the API phase in the final drug product. 13C solid-state NMR (SSNMR) spectroscopy is widely employed to characterize pure and formulated solid APIs; however, 13C SSNMR experiments on dosage forms with low API loading are often challenging due to low sensitivity and interference from excipients. Here, fast MAS 1H SSNMR experiments are shown to be applicable for the rapid characterization ...


The Characterization Of A New Metabolite From A Trichodesmium Bloom, Kelly M. Mcmanus May 2019

The Characterization Of A New Metabolite From A Trichodesmium Bloom, Kelly M. Mcmanus

Senior Honors Projects

Our laboratory has been investigating blooms of Trichodesmium, a genus of ecologically important, nitrogen-fixing cyanobacteria, collected from Padre Island in the Gulf of Mexico. Trichodesmium species are an underexplored biological source of cyanobacteria – a taxa that has been shown to produce chemically diverse secondary metabolites. With our focus on the isolation and structure characterization of new bioactive marine natural products, our research group has discovered over 25 new-to-science compounds over the past three years from these blooms. UV and mass spectrometry-guided isolation of Trichodesmium chromatography fractions were utilized to isolate a new metabolite. Isolation of this metabolite was carried out ...


The Use Of Heterocycles As Important Structures In Medicinal Chemistry, Sayre Weast May 2019

The Use Of Heterocycles As Important Structures In Medicinal Chemistry, Sayre Weast

Honors Theses

Heterocycles have many applications in the discipline of medicinal chemistry. These structures are found in various natural products with relevant biological activity. Our research group, in collaboration with two others, is particularly interested in one heterocycle, quinoline, as a scaffold for HIV-1 integrase inhibitors. A synthetic route has been developed to produce a derivatized structure on small scale. One goal of this thesis was to expand the scale of this route to provide increased quantities of the quinoline scaffold. Procedures were adapted to accommodate the increase in scale to convert commercially available anthranilic acids to quinolines via the isatoic anhydride ...


Preparation Of Enantioenriched Alkyltin Species And Their Application In Stereospecific Transformations, Glenn O. Ralph May 2019

Preparation Of Enantioenriched Alkyltin Species And Their Application In Stereospecific Transformations, Glenn O. Ralph

All Dissertations, Theses, and Capstone Projects

Organometallic reagents containing the tin-carbon bond are used extensively in modern synthetic chemistry for the formation of new bonds to carbon. Over recent decades, transition metal catalyzed cross coupling reactions between two C(sp2) centers have been widely developed. However, the introduction of a C(sp3) center complicates the catalytic cycle, and opens unproductive chemical pathways which lead to isomerization, elimination, and racemization. Our lab has developed a modified-Stille reaction to combat the deleterious effects of β-hydride elimination. Our protocol enables unactivated 2° alkyl organotin nucleophiles to undergo efficient cross coupling reactions with C(sp2) electrophiles, avoiding ...


Defining Cell Cluster Size By Dielectrophoretic Capture At An Array Of Wireless Electrodes Of Several Distinct Lengths, Joseph T. Banovetz, Min Li, Darshna Pagariya, Sungu Kim, Baskar Ganapathysubramanian, Robbyn Anand Apr 2019

Defining Cell Cluster Size By Dielectrophoretic Capture At An Array Of Wireless Electrodes Of Several Distinct Lengths, Joseph T. Banovetz, Min Li, Darshna Pagariya, Sungu Kim, Baskar Ganapathysubramanian, Robbyn Anand

Chemistry Publications

Clusters of biological cells play an important role in normal and disease states, such as in the release of insulin from pancreatic islets and in the enhanced spread of cancer by clusters of circulating tumor cells. We report a method to pattern cells into clusters having sizes correlated to the dimensions of each electrode in an array of wireless bipolar electrodes (BPEs). The cells are captured by dielectrophoresis (DEP), which confers selectivity, and patterns cells without the need for physical barriers or adhesive interactions that can alter cell function. Our findings demonstrate that this approach readily achieves fine control of ...


The Effects Of Cannabidiol And Delta 9-Tetrahydrocannabinol Concentration On Breast Cancer Cells, Dorothy Agyemang Apr 2019

The Effects Of Cannabidiol And Delta 9-Tetrahydrocannabinol Concentration On Breast Cancer Cells, Dorothy Agyemang

Ursidae: The Undergraduate Research Journal at the University of Northern Colorado

Delta 9-tetrahydrocannabinol (THC) and cannabidiol (CBD) are phytocannabinoids that have a potential impact on cancer treatments. Studies have shown that certain cannabinoids cause cancer cells to die, but only with the right concentration, which has not been well documented. The purpose of this study is to determine the exact concentration of CBD and THC needed to kill MCF-7 breast cancer cells. In this experiment, the initial treatment group will be treated with CBD or THC at concentrations of 0.1, 1, 10 and 100 micromolar. These concentrations were arbitrarily chosen because there is not an established baseline. Cell metabolic activity ...


Analysis Of Drug-Protein Interactions During Diabetes By High-Performance Affinity Chromatography, Pingyang Tao Apr 2019

Analysis Of Drug-Protein Interactions During Diabetes By High-Performance Affinity Chromatography, Pingyang Tao

Student Research Projects, Dissertations, and Theses - Chemistry Department

High-performance affinity chromatography (HPAC) is a type of liquid chromatography in which solutes are separated based on their binding to a stationary phase that is a biologically-related agent. Sulfonylurea drugs have significant binding to proteins in blood, with most of this binding is believed to occur with human serum albumin (HSA). HSA is known to be modified as a result of the high serum levels of glucose that is present during diabetes, which may also alter the function of HSA as a binding agent for many drugs in circulation. Some modifications of HSA that can occur during diabetes involves early ...


Nonlinear Optical Measurements Of Bf2–Aza Dipyrromethene Fluorophores., Fryad Z. Henari, Donal F. O'Shea, Dan Wu Apr 2019

Nonlinear Optical Measurements Of Bf2–Aza Dipyrromethene Fluorophores., Fryad Z. Henari, Donal F. O'Shea, Dan Wu

Chemistry Articles

Nonlinear absorption coefficient and the nonlinear refractive index of a series of BF2 aza dipyrromethene chromophores in tetrahydrofuran (THF) solutions were measured using the Z-scan technique with a low power continuous wave laser at 633 nm. Acquired data illustrated that the process involved in nonlinear absorption is reverse saturation absorption. The excited state absorption cross sections for all complexes were calculated and a pump and probe technique was used to record the triplet absorption spectrum. The band gap of the triplet state was estimated from this spectral data and the optical limiting behavior was demonstrated for each derivative.


Development Of Ruthenium Drugs As Anticancer Agents, Daniel Boy Apr 2019

Development Of Ruthenium Drugs As Anticancer Agents, Daniel Boy

Student Scholarship: Chemistry

An overview of literature that outlines the research methods of the development of proposed Ruthenium based anti-cancer agents.


Ligand-Protein Binding Of Cantharidin And Norcantharidin On Hsf1: A Docking Study, Daniel Coyle Apr 2019

Ligand-Protein Binding Of Cantharidin And Norcantharidin On Hsf1: A Docking Study, Daniel Coyle

HON499 projects

Previous research provides experimental evidence that cantharidin acts as an inhibitor of HSF1 in cancer cells whereas the similar norcantharidin exhibits no inhibitory activity on HSF1. This computational study utilized Autodock to suggest both binding site(s) and binding energies of cantharidin and norcantharidin on HSF1. This study found cantharidin to consistently bind stronger than norcantharidin in the same area on HSF1 when assuming a rigid protein structure.


Tracking Decitabine Incorporation Into Malignant Myeloid Cell Dna In Vitro And In Vivo By Lc-Ms/Ms With Enzymatic Digestion, Sujatha Chilakala, Ye Feng, Lan Li, Reda Mahfouz, Ebrahem Quteba, Yogen Saunthararajah, Yan Xu Mar 2019

Tracking Decitabine Incorporation Into Malignant Myeloid Cell Dna In Vitro And In Vivo By Lc-Ms/Ms With Enzymatic Digestion, Sujatha Chilakala, Ye Feng, Lan Li, Reda Mahfouz, Ebrahem Quteba, Yogen Saunthararajah, Yan Xu

Chemistry Faculty Publications

The DNA hypomethylating agents decitabine and 5-azacytidine are the only two drugs approved for treatment of all subtypes of the myeloid malignancy myelodysplastic syndromes (MDS). The key to drug activity is incorporation into target cell DNA, however, a practical method to measure this incorporation is un-available. Here, we report a sensitive and specific LC-MS/MS method to simultaneously measure decitabine incorporation and DNA hypomethylation. A stable heavy isotope of 2'-deoxycytidine was used as an internal standard and one-step multi-enzyme digestion was used to release the DNA bound drug. Enzyme-released decitabine along with other mononucleosides were separated by a reverse-phase ...


Purification And Characterization Of A Nonspecific Lipid Transfer Protein 1 (Nsltp1) From Ajwain (Trachyspermum Ammi) Seeds, Meshal Nazeer, Humera Waheed, Maria Saeed, Saman Yousuf Ali, M. Iqbal Choudhary, Zaheer Ul-Haq, Aftab Ahmed Mar 2019

Purification And Characterization Of A Nonspecific Lipid Transfer Protein 1 (Nsltp1) From Ajwain (Trachyspermum Ammi) Seeds, Meshal Nazeer, Humera Waheed, Maria Saeed, Saman Yousuf Ali, M. Iqbal Choudhary, Zaheer Ul-Haq, Aftab Ahmed

Pharmacy Faculty Articles and Research

Ajwain (Trachyspermum ammi) belongs to the family Umbelliferae, is commonly used in traditional, and folk medicine due to its carminative, stimulant, antiseptic, diuretic, antihypertensive, and hepatoprotective activities. Non-specific lipid transfer proteins (nsLTPs) reported from various plants are known to be involved in transferring lipids between membranes and in plants defense response. Here, we describe the complete primary structure of a monomeric non-specific lipid transfer protein 1 (nsLTP1), with molecular weight of 9.66 kDa, from ajwain seeds. The nsLTP1 has been purified by combination of chromatographic techniques, and further characterized by mass spectrometry, and Edman degradation. The ajwain nsLTP1 is ...


Thioredoxin Modulates Protein Arginine Deiminase 4 (Pad4)-Catalyzed Citrullination, Mitesh Nagar, Ronak Tilvawala, Paul R. Thompson Feb 2019

Thioredoxin Modulates Protein Arginine Deiminase 4 (Pad4)-Catalyzed Citrullination, Mitesh Nagar, Ronak Tilvawala, Paul R. Thompson

Open Access Articles

Protein citrullination is a post-translational modification catalyzed by the protein arginine deiminases (PADs). This modification plays a crucial role in the pathophysiology of numerous autoimmune disorders including RA. Recently, there has been a growing interest in investigating physiological regulators of PAD activity to understand the primary cause of the associated disorders. Apart from calcium, it is well-documented that a reducing environment activates the PADs. Although the concentration of thioredoxin (hTRX), an oxidoreductase that maintains the cellular reducing environment, is elevated in RA patients, its contribution toward RA progression or PAD activity has not been explored. Herein, we demonstrate that hTRX ...


Qualitative And Quantitative Ethnobotanical Study Of The Pangkhua Community In Bilaichari Upazilla, Rangamati District, Bangladesh., Mohammad O. Faruque, Gang Feng, Md Na Khan, James W. Barlow, Umme R. Ankhi, Sheng Hu, M Kamaruzzaman, Shaikh B. Uddin, Xuebo Hu Feb 2019

Qualitative And Quantitative Ethnobotanical Study Of The Pangkhua Community In Bilaichari Upazilla, Rangamati District, Bangladesh., Mohammad O. Faruque, Gang Feng, Md Na Khan, James W. Barlow, Umme R. Ankhi, Sheng Hu, M Kamaruzzaman, Shaikh B. Uddin, Xuebo Hu

Chemistry Articles

BACKGROUND: The present study documents the ethnomedicinal knowledge among the traditional healers of the Pangkhua indigenous community of Bangladesh. The documented data from this area was quantitatively analyzed for the first time. We aimed to record ethnomedicinal information from both the traditional healers and also the elderly men and women of the community, in order to compile and document all available information concerning plant use and preserve it for the coming generations. We aimed to compare how already known species are used compared to elsewhere and particularly to highlight new ethnomedicinal plant species alongside their therapeutic use(s).

METHODS: All ...


Synthesis, Biological Evaluation And Molecular Modeling Studies Of Novel Chromone/Aza-Chromone Fused Α-Aminophosphonates As Src Kinase Inhibitors, S. Bapat, N. Viswanadh, M. Mujahid, Amir Nasrolahi Shirazi, Rakesh Tiwari, Keykavous Parang, M. Karthikeyan, M. Muthukrishnan, Renu Vyas Feb 2019

Synthesis, Biological Evaluation And Molecular Modeling Studies Of Novel Chromone/Aza-Chromone Fused Α-Aminophosphonates As Src Kinase Inhibitors, S. Bapat, N. Viswanadh, M. Mujahid, Amir Nasrolahi Shirazi, Rakesh Tiwari, Keykavous Parang, M. Karthikeyan, M. Muthukrishnan, Renu Vyas

Pharmacy Faculty Articles and Research

A series of novel chromone/aza-chromone fused α-aminophosphonate derivatives were synthesized in good yields using silica chloride as the catalyst. All the synthesized compounds were tested for their c-Src kinase inhibitory activity. Aza-chromone compound showed Src kinase inhibition with an IC50 value of 15.8 µM. The compounds were subjected to molecular docking and dynamics simulations to study the atomic level interactions with an unphosphorylated proto-oncogenic tyrosine protein kinase Src (PDB code 1Y57) as well as phosphorylated tyrosine protein kinase Src (PDB code 2H8H). Docking and molecular dynamic results revealed phosphorylated Src tyrosine kinase protein better results than unphosphorylated tyrosine ...


Bisthioether Stapled Peptides Targeting Polycomb Repressive Complex 2 Gene Repression, Gan Zhang Feb 2019

Bisthioether Stapled Peptides Targeting Polycomb Repressive Complex 2 Gene Repression, Gan Zhang

All Dissertations, Theses, and Capstone Projects

Interactions between proteins play a key role in nearly all cellular process, and therefore, disruption of such interactions may lead to many different types of cellular dysfunctions. Hence, pathologic protein-protein interactions (PPIs) constitute highly attractive drug targets and hold great potential for developing novel therapeutic agents for the treatment of incurable human diseases. Unfortunately, the identification of PPI inhibitors is an extremely challenging task, since traditionally used small molecule ligands are mostly unable to cover and anchor on the extensive flat surfaces that define those binary protein complexes. In contrast, large biomolecules such as proteins or peptides are ideal fits ...


Antitumor Properties Of Imidazolium Salts, Jenna Frantz Jan 2019

Antitumor Properties Of Imidazolium Salts, Jenna Frantz

Williams Honors College, Honors Research Projects

This is the final write-up for an honors research project for the University of Akron Williams Honors College. Synthesis of novel imidazolium salts was conducted. Following synthesis of imidazolium salts, the stability of the compound was tested at 37°C over a 72-hour period to give preliminary information about drug stability in vivo. 2D NMR was also conducted to confirm the structure of TPP-1. The student wrote an experimental protocol for the use of C57BL/6 mice and performed the online CITI training by the IRB to prepare to work with animals in a study of the antitumor properties of ...


Development And Characterization Of Ldv Peptide Targeted Nanocarriers For Paclitaxel Delivery: A Comparative Study Of Micelles, Liposomes And Solid Lipid Nanoparticles, Poonam Dattani Jan 2019

Development And Characterization Of Ldv Peptide Targeted Nanocarriers For Paclitaxel Delivery: A Comparative Study Of Micelles, Liposomes And Solid Lipid Nanoparticles, Poonam Dattani

University of the Pacific Theses and Dissertations

Nanocarriers have been established as delivery vehicles to target cancer tumors. However, premature drug leakage is one of the major reasons for inefficient drug delivery of nanocarriers to the tumor. Drug diffusion out of the nanocarriers or destabilization of drug loaded nanocarriers by physiological interactions with blood cells, serum proteins, and cell membranes upon systemic administration contribute to premature drug release. In this study, targeted micelles, liposomes and solid lipid nanoparticles (SLNs) of similar composition were prepared and characterized to compare physicochemical characteristics, in vitro stability, in vitro release rates in release media and in vivo performance. Peptide Amphiphiles (PAs ...


Rgd Conjugated Cell Uptake Off To On Responsive Nir-Aza Fluorophores: Applications Toward Intraoperative Fluorescence Guided Surgery, Dan Wu, Harrison C. Daly, Marco Grossi, Emer Conroy, Bo Li, William M. Gallagher, Robert Elmes, Donal F. O'Shea Jan 2019

Rgd Conjugated Cell Uptake Off To On Responsive Nir-Aza Fluorophores: Applications Toward Intraoperative Fluorescence Guided Surgery, Dan Wu, Harrison C. Daly, Marco Grossi, Emer Conroy, Bo Li, William M. Gallagher, Robert Elmes, Donal F. O'Shea

Chemistry Articles

The use of NIR-fluorescence imaging to demarcate tumour boundaries for real-time guidance of their surgical resection has a huge untapped potential. However, fluorescence imaging using molecular fluorophores, even with a targeting biomolecule attached, has a major shortcoming of signal interference from non-specific background fluorescence outside the region of interest. This poor selectivity necessitates prolonged time delays to allow clearance of background fluorophore and retention within the tumour prior to image acquisition. In this report, an innovative approach to overcome this issue is described in which cancer targeted off to on bio-responsive NIRfluorophores are utilised to switch-on first within the tumour ...


Robert J. Lefkowitz And Discovery Of The G-Protein-Coupled Receptor Family, Clarence Lee Jan 2019

Robert J. Lefkowitz And Discovery Of The G-Protein-Coupled Receptor Family, Clarence Lee

Natural Sciences Poster Sessions

This poster for the Natural Sciences Poster Session at Parkland College features Dr. Robert J. Lefkowitz, 2012 Nobel Prize in Chemistry winner (with Brian Kobilka) for their research on G-protein-coupled receptors, proteins in the plasma membrane that allow for the transmission of information through the membrane and into the cell. This research was to impact the development of medications that target these receptors, such as SSRIs.


Therapeutic Delivery Technology And Its Economic Impact, Paul E. Savas Jr. Jan 2019

Therapeutic Delivery Technology And Its Economic Impact, Paul E. Savas Jr.

Senior Honors Theses

Therapeutic delivery technology is a current area of high interest in both university and industrial settings. These technologies are being developed in order to deliver therapeutic agents, such as genes, proteins, and drugs, to patients more efficiently. Nanoscale delivery vehicles have proven to be useful for these applications; these vehicles may either be naturally produced or chemically synthesized. The physical properties of these nanomaterials must be characterized correctly using instrumentation that evaluates their size, morphology, and potential for agglomeration. These technologies represent a high-growth economic area that fosters entrepreneurship and innovation. Because of this innovative spirit, research and economic interest ...


Synthesis Of Oligodeoxynucleotides Containing Sensitive Electrophiles, Shahien Shahsavari Jan 2019

Synthesis Of Oligodeoxynucleotides Containing Sensitive Electrophiles, Shahien Shahsavari

Dissertations, Master's Theses and Master's Reports

Oligodeoxynucleotides (ODNs) containing electrophilic groups are useful in many studies including antisense drug development and DNA/protein interaction. Due to the use of strong nucleophiles for cleavage and deprotection, traditional ODN synthesis methods are not suitable for their preparation. To solve this problem, a new ODN synthesis technology using the 1,3- dithiane-2-yl-methoxycarbonyl (Dmoc) function as protecting groups and linker has been developed. Furthermore, Dmoc-derivatives were developed to demonstrate the feasibility of the technology. The Dmoc and Dmoc derivative functions are stable under all ODN synthesis conditions using the phosphoramidite chemistry. Upon oxidation of the sulfides in them, because of ...


Molecular Insights Into Organic Particulate Formation, Manoj Kumar, Emily Burrell, Jason C. Hansen, Joseph S. Francisco Jan 2019

Molecular Insights Into Organic Particulate Formation, Manoj Kumar, Emily Burrell, Jason C. Hansen, Joseph S. Francisco

Faculty Publications -- Chemistry Department

Carboxylic acids have been detected in particles collected in various regions of the world. Here, we use experiments and Born–Oppenheimer molecular dynamics simulations to better understand the mechanism of particle formation from gas phase mixtures of formic acid (HCOOH), (CH3)3N, and water vapor. A flow reaction cell coupled to two scanning mobility particle sizers has been used to measure particle size, absolute number of particles and kinetics of particle formation. Experimental results show that the addition of (CH3)3N to a mixture of HCOOH and water vapor results in a dramatic increase in particle ...