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Medicinal-Pharmaceutical Chemistry Commons

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Characterization Of Gold Nanoparticle Antimicrobials, Kelsey Higgins 2014 University of Colorado Boulder

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 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 2014 Iowa State University

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 ...


Quantification Of Factors Governing Drug Release Kinetics From Nanoparticles: A Combined Experimental And Mechanistic Modeling Approach, Kyle Daniel Fugit 2014 University of Kentucky

Quantification Of Factors Governing Drug Release Kinetics From Nanoparticles: A Combined Experimental And Mechanistic Modeling Approach, Kyle Daniel Fugit

Theses and Dissertations--Pharmacy

Advancements in nanoparticle drug delivery of anticancer agents require mathematical models capable of predicting in vivo formulation performance from in vitro characterization studies. Such models must identify and incorporate the physicochemical properties of the therapeutic agent and nanoparticle driving in vivo drug release. This work identifies these factors for two nanoparticle formulations of anticancer agents using an approach which develops mechanistic mathematical models in conjunction with experimental studies.

A non-sink ultrafiltration method was developed to monitor liposomal release kinetics of the anticancer agent topotecan. Mathematical modeling allowed simultaneous determination of drug permeability and interfacial binding to the bilayer from release ...


Current And Potential Applications Of Bismuth-Based Drugs., Donal M. Keogan, Darren M. Griffith 2014 Royal College of Surgeons in Ireland

Current And Potential Applications Of Bismuth-Based Drugs., Donal M. Keogan, Darren M. Griffith

Chemistry Articles

Bismuth compounds have been used extensively as medicines and in particular for the treatment of gastrointestinal ailments. In addition to bismuth's well known gastroprotective effects and efficacy in treating H. pylori infection it also has broad anti-microbial, anti-leishmanial and anti-cancer properties. Aspects of the biological chemistry of bismuth are discussed and biomolecular targets associated with bismuth treatment are highlighted. This review strives to provide the reader with an up to date account of bismuth-based drugs currently used to treat patients and discuss potential medicinal applications of bismuth drugs with reference to recent developments in the literature. Ultimately this review ...


The Synthesis And Biological Activity Of Iron Binding Motifs, Rachel Burke 2014 Georgia Southern University

The Synthesis And Biological Activity Of Iron Binding Motifs, Rachel Burke

University Honors Program Theses

Iron is an essential mineral that plays a key role in the oxygen transporting molecule hemoglobin. Iron also helps muscles store and use oxygen. Excess iron in the body can attract electrons, creating harmful oxygen radicals. Iron overload can be caused by several factors such as genetics, age, gender, and having received multiple red blood cell transfusions. Excess iron can lead to many diseases, such as arthritis, liver cirrhosis, heart disease, and several forms of cancer. Iron-chelating therapies work by binding free iron in the bloodstream and by reducing the amount of iron bound in transferrin, the iron transporting molecule ...


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 2014 Salve Regina University

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 ...


Caffeine + L-Theanine: Uses And Effects, Julia Dueease 2014 Parkland College

Caffeine + L-Theanine: Uses And Effects, Julia Dueease

Natural Sciences Poster Sessions

When combined caffeine and l-theanine, two prominent components found in tea, create better reaction times, accuracy, and positive moods. This is a Powerpoint presentation created for the Natural Science Poster Session at Parkland College


Focalin Xr: Dexmethylphenidate Hydrochloride, Andrea L. Sullivan 2014 Parkland College

Focalin Xr: Dexmethylphenidate Hydrochloride, Andrea L. Sullivan

Natural Sciences Poster Sessions

This poster presented at the Natural Sciences Poster Session features the cerebral stimulant Focalin XR, or Dexmethylphenidate Hydrochloride. It identifies names and uses, and illustrates its chemical makeup.


Leukeran, Leslie R. Hunt 2014 Parkland College

Leukeran, Leslie R. Hunt

Natural Sciences Poster Sessions

Leukeran (generic name Chlorambucil) is used alone or with other antineoplastics to treat chronic lymphocytic leukemia, malignant lymphomas, Hodgkin's disease, giant follicular lymphoma, and cancers of the ovaries, breast, and testes. Unlabled uses include treatment of nonneoplastic conditions such as vasculitis complicating rheumatoid arthritis, autoimmune hemolytic anemias associated with cold agglutinins, lupus glomerulonephritis, idiopathic nephrotic syndrome, polycythenmia vera, and macroglobulinemia.


Injectable Versus Inhalational Anesthesia In Veterinary Medicine, Samantha D. Christ 2014 Parkland College

Injectable Versus Inhalational Anesthesia In Veterinary Medicine, Samantha D. Christ

Natural Sciences Poster Sessions

Is the better, safer choice in small animal surgery injectible or inhalational anesthsesia? This poster outlines the advantages and disadvantages of the two, with a focus on two widely-used anesthetics, Ketamine and Isoflurane. This project is from the Natural Science Poster Session at Parkland College


Gertrude B. Elion, Kelli N. Brost 2014 Parkland College

Gertrude B. Elion, Kelli N. Brost

Natural Sciences Poster Sessions

This poster for the Natural Sciences Poster Session at Parkland College describes the accomplishments of Gertrude B. Elion, a biochemist and pharmacologist. Elion developed multiple anticancer, antivirals, and autoimmune drugs.


Periactin, Sarah A. Johnson 2014 Parkland College

Periactin, Sarah A. Johnson

Natural Sciences Poster Sessions

Poster examines the chemical makeup of Periactin, generic name Cyproheptadine Hydrocholoride. Classified as an antihistamine or antipruritic, the labeled uses for Periactin are for symptomatic relief of various allergic conditions. Periactin can also be used for the following unlabeled uses: Cushing's disease, carcinoid syndrome, vascular headaches, and as an appetite stimulant.


A Nmr Experiment For Simultaneous Correlations Of Valine And Leucine/Isoleucine Methyls With Carbonyl Chemical Shifts In Proteins, Vitali Tugarinov, Vincenzo Venditti, G. Marius Clore 2014 National Institutes of Health

A Nmr Experiment For Simultaneous Correlations Of Valine And Leucine/Isoleucine Methyls With Carbonyl Chemical Shifts In Proteins, Vitali Tugarinov, Vincenzo Venditti, G. Marius Clore

Vincenzo Venditti

A methyl-detected ‘out-and-back’ NMR experiment for obtaining simultaneous correlations of methyl resonances of valine and isoleucine/leucine residues with backbone carbonyl chemical shifts, SIM-HMCM(CGCBCA)CO, is described. The developed pulse-scheme serves the purpose of convenience in recording a single data set for all Ileδ1, Leuδ and Valγ (ILV) methyl positions instead of acquiring two separate spectra selective for valine or leucine/isoleucine residues. The SIM-HMCM(CGCBCA)CO experiment can be used for ILV methyl assignments in moderately sized protein systems (up to ~100 kDa) where the backbone chemical shifts of 13Cα, 13Cβ and 13CO are known from prior NMR ...


Iterative Assembly Of Two Separate Polyketide Chains By The Same Single-Module Bacterial Polyketide Synthase In The Biosynthesis Of Hsaf, Yaoyao Li, Haotong Chen, Yanjiao Ding, Yunxuan Xie, Haoxin Wang, Ronald Cerny, Yuemao Shen, Liangcheng Du 2014 Shandong University

Iterative Assembly Of Two Separate Polyketide Chains By The Same Single-Module Bacterial Polyketide Synthase In The Biosynthesis Of Hsaf, Yaoyao Li, Haotong Chen, Yanjiao Ding, Yunxuan Xie, Haoxin Wang, Ronald Cerny, Yuemao Shen, Liangcheng Du

Ronald Cerny Publications

HSAF (1) was isolated from the biocontrol agent Lysobacter enzymogenes (Figure 1).[1-4]

This bacterial metabolite belongs to polycyclic tetramate macrolactams (PTM) that are

emerging as a new class of natural products with distinct structural features. [5, 6] HSAF

exhibits a potent antifungal activity and shows a novel mode of action.[1-4] The HSAF

biosynthetic gene cluster contains only a single-module hybrid polyketide synthasenonribosomal

peptide synthetase (PKS-NRPS), although the PTM scaffold is apparently

derived from two separate hexaketide chains and an ornithine residue.[1-4] This suggests that

the same PKS module would act not only iteratively, but also separately, in ...


Proton Pump Inhibitors: Omeprazole, Paulina N. Ongkowijoyo 2014 Parkland College

Proton Pump Inhibitors: Omeprazole, Paulina N. Ongkowijoyo

A with Honors Projects

Characteristics and uses of proton pump inhibitors are discussed, specifically, the drug omeprazole, a type of proton pump inhibitor, is discussed, including the chemistry, it's uses and side effects.


Glyco-Modification Of Protein With O-Cyanate Chain-End Functionalized Glycopolymer Via Isourea Bond Formation, Valentinas Gruzdys, Hailong Zhang, Xue-Long Sun 2014 Cleveland State University

Glyco-Modification Of Protein With O-Cyanate Chain-End Functionalized Glycopolymer Via Isourea Bond Formation, Valentinas Gruzdys, Hailong Zhang, Xue-Long Sun

Chemistry Faculty Publications

Glycoengineering aimed at addition of carbohydrates to proteins is an attractive approach to alter pharmacokinetic properties of proteins such as enhancing stability and prolonging the duration of action. We report a novel protein glyco-modification of BSA and recombinant thrombomodulin with O-cyanate chain-end functionalized glycopolymer via isourea bond formation. The protein glycoconjugates were confirmed by SDS-PAGE, western blot, and MALDI-TOF Mass Spectrometry. Protein C activation activity of the glyco-modified recombinant thrombomodulin was confirmed, proving no interference to activity from the glycopolymer modification. The isourea bond formation under mild conditions was demonstrated as an alternative method for protein modification with polymers.


Structural Dynamics Of A Single-Stranded Rna–Helix Junction Using Nmr, Catherine D. Eichhorn, Hashim M. Al-Hashimi 2014 The University Of Michigan

Structural Dynamics Of A Single-Stranded Rna–Helix Junction Using Nmr, Catherine D. Eichhorn, Hashim M. Al-Hashimi

Faculty Publications -- Chemistry Department

Many regulatory RNAs contain long single strands (ssRNA) that adjoin secondary structural elements. Here, we use NMR spectroscopy to study the dynamic properties of a 12-nucleotide (nt) ssRNA tail derived from the prequeuosine riboswitch linked to the 3′ end of a 48-nt hairpin. Analysis of chemical shifts, NOE connectivity, 13C spin relaxation, and residual dipolar coupling data suggests that the first two residues (A25 and U26) in the ssRNA tail stack onto the adjacent helix and assume an ordered conformation. The following U26-A27 step marks the beginning of an A6-tract and forms an acute pivot point for ...


Structure And Function Of Preq1 Riboswitches, Catherine D. Eichhorn, Mijeong Kang, Juli Feigon 2014 University of California, Los Angeles

Structure And Function Of Preq1 Riboswitches, Catherine D. Eichhorn, Mijeong Kang, Juli Feigon

Faculty Publications -- Chemistry Department

PreQ1 riboswitches help regulate the biosynthesis and transport of PreQ1 (7-aminomethyl-7- deazaguanine), a precursor of the hypermodified guanine nucleotide queuosine (Q), in a number of Firmicutes, Proteobacteria, and Fusobacteria. Queuosine is almost universally found at the wobble position of the anticodon in asparaginyl, tyrosyl, histidyl and aspartyl tRNAs, where it contributes to translational fidelity. Two classes of PreQ1 riboswitches have been identified (PreQ1-I and PreQ1-II), and structures of examples from both classes have been determined. Both classes form H-type pseudoknots upon PreQ1 binding, each of which has distinct unusual features and modes ...


Metallurgical And Corrosion Assessment Of Submerged Tanker S.S. Montebello, Dana Medlin, James D. Carr, Donald L. Johnson, David L. Conlin 2014 Engineering Systems, Inc.

Metallurgical And Corrosion Assessment Of Submerged Tanker S.S. Montebello, Dana Medlin, James D. Carr, Donald L. Johnson, David L. Conlin

Faculty Publications -- Chemistry Department

The Union Oil Tanker S.S. Montebello was torpedoed and sunk six miles (9.7 km) off the coast of Cambria, California by a Japanese submarine on December 23, 1941, two weeks after the attack on Pearl Harbor. With close proximity to the National Monterey Bay Marine Sanctuary, concern about possible crude oil contamination led to the most recent expedition to the site in October 2011. Assessment of the shell plate found that the average corrosion rate was very low and the structure will remain stable for many decades.


Advances In Chemical And Structural Characterization Of Concretion With Implications For Modeling Marine Corrosion, Donald L. Johnson, Robert J. Deangelis, Dana J. Medlin, James D. Carr, David L. Conlin 2014 National Park Service Submerged Resources Center

Advances In Chemical And Structural Characterization Of Concretion With Implications For Modeling Marine Corrosion, Donald L. Johnson, Robert J. Deangelis, Dana J. Medlin, James D. Carr, David L. Conlin

Faculty Publications -- Chemistry Department

The Weinsnumber model and concretion equivalent corrosion rate methodology were developed as potential minimum-impact, cost-effective techniques to determine corrosion damage on submerged steel structures. To apply the full potential of these technologies, a detailed chemical and structural characterization of the concretion (hard biofouling) that transforms into iron bearing minerals is required. The fractions of existing compounds and the quantitative chemistries are difficult to determine from x-ray diffraction. Environmental scanning electron microscopy was used to present chemical compositions by means of energy-dispersive spectroscopy (EDS). EDS demonstrates the chemical data in mapping format or in point or selected area chemistries. Selectedarea EDS ...


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