Synthesis Of Novel Temozolomide-Fatty Acid Imide Hybrid Compounds For The Chemotherapeutic Treatment Of Glioblastoma Multiforme,
2020
Andrews University
Synthesis Of Novel Temozolomide-Fatty Acid Imide Hybrid Compounds For The Chemotherapeutic Treatment Of Glioblastoma Multiforme, Janice Pakkianathan
Honors Theses
Glioblastoma multiforme (GBM) is an aggressive form of brain cancer that originates from glial cells, which make up the supportive tissue surrounding neurons. Temozolomide (TMZ) is the current chemotherapeutic drug administered to treat GBM as it works to inhibit the growth of the cancer cells. This research study focused on developing a method for synthesizing novel hybrid compounds that combines TMZ with various fatty acids known to have anticancer properties, forming a series of imide compounds with potential chemotherapeutic effects. Before synthesizing the compounds, various methods for synthesizing an imide from a primary amide were tested to ensure that TMZ …
Fungicide Sensitivity Of Sclerotinia Sclerotiorum Isolates Selected From Five Different States That Use Different Fungicide Treatments,
2020
University of Nebraska-Lincoln
Fungicide Sensitivity Of Sclerotinia Sclerotiorum Isolates Selected From Five Different States That Use Different Fungicide Treatments, Cristian Wulkop Gil
UCARE: Research Products
Sclerotinia sclerotiorum is a plant pathogenic fungus that causes a disease called white mold that can infect more than 450 plant species including soybeans, dry beans, green beans, canola, and sunflower. This pathogen is capable of up to $252M in losses every year (U.S. Canola Association, 2014). Fungicides are widely used in developed agricultural systems to control disease. However, resistance to the most effective fungicides has emerged and spread in pathogen populations and there have been multiple reports of S. sclerotiorum isolates becoming resistant to certain fungicides. Since different fields in different states use different fungicide treatments on plants and …
Synthesis And Characterization Of Potential Pharmaceutical Analogs Of A Gvsu Lead Compound: An Investigation Of Antibiotic & Anti-Tumor Activity,
2020
Grand Valley State University
Synthesis And Characterization Of Potential Pharmaceutical Analogs Of A Gvsu Lead Compound: An Investigation Of Antibiotic & Anti-Tumor Activity, Nicole Horne
Student Scholars Day Posters
In support of ongoing anti-microbial & anti-tumor research, analogs of a GVSU lead compound, a derivative of the known telomerase inhibitor BIBR1532, were synthesized. These compounds were submitted for biological analysis to determine pharmacological activity toward the discovery of either an antibiotic that can resist bacterial enzymatic degradation or a chemotherapeutic molecule that can destroy tumor cells without increasing toxicity. The anti-microbial interest in these compounds was based on the fact that they are non-penicillin based antibiotics and display a broad range of efficacy against targeted bacteria, including C. diff & MRSA, with minimal toxicity. These compounds were made via …
Periodic Table Club,
2020
University of Nebraska - Lincoln
Periodic Table Club, Makayla Gill, Kailynn Jensen
Honors Program: Expanded Learning Clubs
This club is dedicated to teaching the generation of future scientists the periodic table. This is designed to be a unique take on a STEM club that uses the periodic table as a backbone for a solid foundation in chemistry.
A Broadly Distributed, Novel Class Of Diiron Enzymes Involved In Para-Aminobenzoate Synthesis,
2020
University of South Carolina - Columbia
A Broadly Distributed, Novel Class Of Diiron Enzymes Involved In Para-Aminobenzoate Synthesis, Joseph M. Zambelas
Senior Theses
The overall structure and ligand arrangement of diiron enzymes influence their function and catalytic potential, allowing for them to catalyze an expansive breadth of high energy transformations. The diiron enzyme CADD from Chlamydia trachomatis is involved in a novel biosynthetic pathway for p-aminobenzoic acid (pABA), a precursor for tetrahydrofolate. The unique ligand structure and reactivity of CADD and homolog NE1434 provide an intriguing means to contrast structure function relationships with other known diiron enzymes that activate dioxygen. In this work, studies of CADD and NE1434 orthologs and comparison to other diiron enzymes reveal several sequence motifs that are likely critical …
Toxicity Of Novel Platinum Compounds In Mammalian Cancer Cells,
2020
Western Kentucky University
Toxicity Of Novel Platinum Compounds In Mammalian Cancer Cells, Vanesa Veletanlic
Masters Theses & Specialist Projects
There are currently three FDA platinum compounds approved for use as chemotherapeutics, where each drug has variable efficacies for different cancer types depending on cancer’s tissue of origin. The approved compounds are platinum(II) complexes with four coordination sites on the platinum atom allowing two types of ligands to attach: leaving ligands, which are removed from the platinum atom in solution, and non-leaving ligands, which remain complexed to the platinum. Carboplatin, the preferred compound used to treat ovarian and small-cell lung cancers, has a characteristic cyclobutanedicarboxylic acid leaving ligand and two ammonia non-leaving ligands. A novel compound, 1,1-cyclobutanedicarboxylato(ethylenediamine)platinum (II), or Pt(en)CBDCA, …
Understanding How Human Lipoxygenases Bind Molecular Oxygen And Arachidonic Acid Substrate,
2020
Louisiana State University
Understanding How Human Lipoxygenases Bind Molecular Oxygen And Arachidonic Acid Substrate, Austin Paul Primeaux
Honors Capstones
No abstract provided.
The Effects Of Transgenic Alterations Of Bicarbonate-Utilizing Enzymes In Escherichia Coli On The Activity Of Acetyl-Coa Carboxylase,
2020
Louisiana State University
The Effects Of Transgenic Alterations Of Bicarbonate-Utilizing Enzymes In Escherichia Coli On The Activity Of Acetyl-Coa Carboxylase, Aniko Alicia Nowakowski
Honors Capstones
No abstract provided.
Tip60 Regulation Of Δnp63Α Is Associated With Cisplatin Resistance,
2020
Wright State University - Main Campus
Tip60 Regulation Of Δnp63Α Is Associated With Cisplatin Resistance, Akshay Hira, Andrew Stacy, Jin Zhang, Michael P. Craig, Madhavi Kadakia
Celebration of Undergraduate & Graduate Research, Scholarship, and Creative Activities Materials
About 5.4 million basal and squamous cell skin cancers are diagnosed every year in the US. ΔNp63a, a member of the p53 transcription factor family, is overexpressed in non-melanoma skin cancer and regulates cell survival, migration and invasion. TIP60 is histone acetyltransferase (HAT) which mediates cellular processes such as transcription and the DNA damage response (DDR). Previous studies in our lab have shown that overexpression of TIP60 induces ΔNp63a protein stabilization in a catalytic-dependent manner. Since ΔNp63a is known to transcriptionally regulate several DDR genes and promote cisplatin resistance, its stabilization by TIP60 may contribute to the failure of platinum-based …
Optimization Of Methods For Cross-Species Infection Of Cell Cultures With Wolbachia,
2020
University of South Dakota
Optimization Of Methods For Cross-Species Infection Of Cell Cultures With Wolbachia, Sarah J. Lane
Honors Thesis
The common intracellular endosymbiont genus of bacteria called Wolbachia is of interest due to the promise it shows for playing a role in disease control. Wolbachia have a number of widely variable effects on its many species of host insects. In combination with these roles, Wolbachia largely affects reproduction and development of its host species. It can lead to feminization and cytoplasmic incompatibility (Werren et al. 2008). Furthermore, this species is vertically transmitted which means that it passes from mother to offspring (Caragata et al., 2016). In combination with its effects on reproduction, which can allow Wolbachia to propagate through …
Synthesis And Structure-Activity Relationship Study Of Novel Nitrodiphenylurea Antibiotics,
2020
Grand Valley State University
Synthesis And Structure-Activity Relationship Study Of Novel Nitrodiphenylurea Antibiotics, Helen Bahlbi
Student Scholars Day Posters
According to the World Health Organization, tuberculosis (TB) is the leading cause of death by infectious disease. Tuberculosis is caused by the bacteria Mycobacterium tuberculosis and occurs globally. Additionally, in 2017, TB was reported in all 50 states. Due to the scope of TB, strict observation of patients is required to ensure adherence to the current drug regimen. However, most reported cases are in developing countries where proper care is difficult. With the emergence of multidrug-resistant TB exhibiting resistance to current treatments, novel antibiotics are needed. Recently, our lab discovered a family of diphenyl ureas that exhibit antimicrobial activity against …
The Organic Synthesis Of Anthranilic Acid Derivatives As Potential Active Antibiotics,
2020
Grand Valley State University
The Organic Synthesis Of Anthranilic Acid Derivatives As Potential Active Antibiotics, Paul Chappell
Student Scholars Day Posters
The objective of this research project was to synthesize multiple derivatives of anthranilic acid. These derivatives will then be tested for antibiotic activity against Staphylococcus aureus and Escherichia coli (E. coli). As bacteria become more resistant to penicillin-based antibiotics, the exploration of anthranilic acid-based antibiotics could serve an important role for future medical use. This research project included data collection via 1H-NMR, 12C-NMR, TLC, MP, and IR to determine purity for biological testing.
Visible-Light Photooxidation In Water By 1o2-Generating Supramolecular Hydrogels,
2020
CUNY Advanced Science Research Center
Visible-Light Photooxidation In Water By 1o2-Generating Supramolecular Hydrogels, Sankarsan Biswas, Mohit Kumar, Andrew Levine, Ian Jimenez, Rein V. Ulijn, Adam Braunschweig
Advanced Science Research Center
We report supramolecular photocatalytic hydrogels, produced by the enzymatically driven self-assembly of low molecular weight gelators (LMWGs). These LMWG precursors are composed of the organic chromophore diketopyrrolopyrrole (DPP), which is bi-functionalized with a series of amino acid (Phe, Tyr, Leu) methyl esters. In situ enzymatic hydrolysis of these photoactive precursors results in supramolecular hydrogels that provide a high density of photocatalytic sites. Under visible light irradiation these hydrophobic fibers recruit the reaction substrates and also produce 1O2, which is used here for the photooxidation of thioanisole (aromatic substrate) and cyclohexyl methyl sulfide (aliphatic substrate), with yields as …
Network Approaches To Elucidate The Determinants Of Protein Topology And Stability,
2020
Old Dominion University
Network Approaches To Elucidate The Determinants Of Protein Topology And Stability, Zeinab Haratipour
Chemistry & Biochemistry Theses & Dissertations
Predicting three-dimensional structures of proteins from sequence information alone, remains one of the most profoundly challenging and intensely studied problems in basic science. It has uniquely garnered the interdisciplinary efforts of biologists, biochemists, computer scientists, mathematicians and physicists. The advancement of computational methods to study fundamental features of proteins also enables insights that are either difficult to explore experimentally or complimentary to further interpret experimental data. In the present research and through the combined development and application of molecular dynamics and network science approaches we aimed to elucidate the role of geographically important amino acids and evolutionarily conserved long-range interactions …
Synthesis Of A Protected 2-Aminocyclobutanone As A Modular Transition State Synthon For Medicinal Chemistry,
2020
Loyola University Chicago
Synthesis Of A Protected 2-Aminocyclobutanone As A Modular Transition State Synthon For Medicinal Chemistry, Thahani S. Habeeb Mohammad, Cory T. Reidl, Matthias Zeller, Daniel P. Becker Ph.D.
Chemistry: Faculty Publications and Other Works
The hydrochloride salt of ɑ-aminocyclobutanone protected as its dimethyl acetal 2,2-dimethoxycyclobutan-1-aminium chloride (3) has been prepared as a modular synthon for convenient access to cyclobutanone-containing lead inhibitors of hydrolase enzymes including serine proteases and metalloproteases. Protected ɑ-aminocyclobutanone 3 was converted to representative amide and sulfonamide-functionalized 2-aminocyclobutanone derivatives. Reaction of the amino acetal 3 with phenyl isothiocyanate afforded the bicyclic urea 1-hydroxyl-2,4-diazabicyclo[3.2.0]heptane-3-thione (9) as confirmed by a single crystal X-ray structure.
Comparative Analysis Of The Human Serine Hydrolase Ovca2 To The Model Serine Hydrolase Homolog Fsh1 From S. Cerevisiae,
2020
Butler University
Comparative Analysis Of The Human Serine Hydrolase Ovca2 To The Model Serine Hydrolase Homolog Fsh1 From S. Cerevisiae, Jessica S. Bun, Michael D. Slack, Daniel E. Schemenauer, R. Jeremy Johnson
Scholarship and Professional Work - LAS
Over 100 metabolic serine hydrolases are present in humans with confirmed functions in metabolism, immune response, and neurotransmission. Among potentially clinically relevant but uncharacterized human serine hydrolases is OVCA2, a serine hydrolase that has been linked with a variety of cancer-related processes. Herein, we developed a heterologous expression system for OVCA2 and determined the comprehensive substrate specificity of OVCA2 against two ester substrate libraries. Based on this analysis, OVCA2 was confirmed as a serine hydrolase with a strong preference for long-chain alkyl ester substrates (>10-carbons) and high selectivity against a variety of short, branched, and substituted esters. Substitutional analysis …
Evaluating The Anti-Cancer Efficacy Of A Synthetic Curcumin Analog On Human Melanoma Cells And Its Interaction With Standard Chemotherapeutics,
2020
Wayne State University
Evaluating The Anti-Cancer Efficacy Of A Synthetic Curcumin Analog On Human Melanoma Cells And Its Interaction With Standard Chemotherapeutics, Krishan Parashar, Siddhartha Sood, Ali Mehaidli, Colin Curran, Caleb Vegh, Christopher Nguyen, Christopher Pignanelli, Jianzhang Wu, Guang Liang, Yi Wang, Siyaram Pandey
Medical Student Research Symposium
Melanoma is the leading cause of skin-cancer related deaths in North America. Metastatic melanoma is difficult to treat and chemotherapies have limited success. Furthermore, chemotherapies lead to toxic side effects due to nonselective targeting of normal cells. Curcumin is a natural product of Curcuma longa (turmeric) and has been shown to possess anti-cancer activity. However, due to its poor bioavailability and stability, natural curcumin is not an effective cancer treatment. We tested synthetic analogs of curcumin that are more stable. One of these derivatives, Compound A, has shown significant anti-cancer efficacy in colon, leukemia, and triple-negative inflammatory breast cancer cells. …
Development And Implementation Of A Biochemistry Argumentation Task To Promote Scientific Literacy Among Undergraduate Students,
2020
University of Nebraska - Lincoln
Development And Implementation Of A Biochemistry Argumentation Task To Promote Scientific Literacy Among Undergraduate Students, Lukas Hall
Honors Program: Senior Projects (Public)
Science education reform efforts at the postsecondary level have been lacking regardless of meaningful reform at the K-12 level. Of these reforms, the Next Generation Science Standards (NGSS) serve to reframe effective science teaching and learning as three-dimensional (3D). That is, 3D instruction integrates core disciplinary ideas, cross-cutting concepts, and science practices to support students’ science learning. There have been calls to extend this 3D model to the postsecondary level. The purpose of this study was to design, implement, and evaluate a 3D task in a university-level biochemistry course. The task was implemented as a homework assignment to 107 students …
The Role Of Apkcs And Apkc Inhibitors In Cell Proliferation And Invasion In Breast And Ovarian Cancer,
2020
University of South Florida
The Role Of Apkcs And Apkc Inhibitors In Cell Proliferation And Invasion In Breast And Ovarian Cancer, Tracess B. Smalley
USF Tampa Graduate Theses and Dissertations
Research has demonstrated that the atypical protein kinase C-zeta (PKC-ζ) is a component of many dysregulated pathways in breast and ovarian cancer, including cellular proliferation, survival, and cell cycle upregulation. Breast and ovarian cancers affect women every day and are second and fifth leading cause of cancer death. Women who seek treatments are commonly met with invasive surgeries or chemotherapy. Protein kinase C (PKC) is a family of serine and threonine phosphorylating kinases that have been shown to modulate and transduce signaling cascades that play roles in the development and survival of cancers. Atypical PKC (aPKC), have been heavily suggested …
Functions Of Cdk/Cyclin Complexes In Endoreplication Regulation By The Cdk Inhibitor Siamese,
2020
Louisiana State University and Agricultural and Mechanical College
Functions Of Cdk/Cyclin Complexes In Endoreplication Regulation By The Cdk Inhibitor Siamese, Kai Wang
LSU Doctoral Dissertations
Arabidopsis trichome (leaf hair) is a specialized single cell extended from epidermal cell on the leaves, which is a typical endoreplication and is also known as endoreduplication. Several D-type cyclins were tested to check the cell division in trichome, and the trichome expressing either CYCB1;2 or CDKB2;2 cannot trigger cell division, even if simultaneous expression of CYCB1;2 and CDKB2;2 failed to produce mitosis in trichome. Only CYCD3;1 specifically promotes multicellular trichome. cdkb1;1cdbk1;2 double mutants and sim cdkb1;1cdkb1;2 triple mutants exhibit the phenotype similar to the wild type and very limited cell division respectively. Overexpression of a CDKB1;1 dominant-negative construct that …
