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Dissertations / Theses on the topic 'Drug discovery; natural products; proteomics'

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1

Demers, Danielle H. "Chemical Investigations of Fungal Natural Products for Drug Discovery." Scholar Commons, 2017. http://scholarcommons.usf.edu/etd/6825.

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Natural products have, historically, played an important role in drug discovery. Nevertheless, drug resistance, pathogen evolution, and global climate change threaten human health and nearly all current anti-infective treatments on the market today. It is undeniable that new drug discovery efforts are needed with increasing urgency. Bolstered by a rich history of discovering treatments in the world around us, natural products chemists continue to look to the environment with increasing understanding and emerging technologies that allow efficient, effective isolation of new chemical entities. T
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2

Dinarvand, Mojdeh. "Discovery and development of novel antibacterials from natural products." Thesis, The University of Sydney, 2017. http://hdl.handle.net/2123/18569.

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Methicillin-resistant Staphylococcus aureus (MRSA) is a major human pathogen associated with a variety of moderate to severe infections. The multi-drug resistant nature of this pathogen makes treatment difficult. The main aim of this study was to screen a library of marine samples for novel compounds with antibacterial activity. A high-throughput assay was developed to identify active extracts, followed by determination of minimum inhibitory concentrations (MICs) for hits. The toxicity of marine samples was measured against different cells lines. Crude extracts were purified using column chrom
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3

Larsson, Sonny. "Mistletoes and Thionins : as Selection Models in Natural Products Drug Discovery." Doctoral thesis, Uppsala : Acta Universitatis Upsaliensis, 2007. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-7705.

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4

Hatherley, Rowan. "Structural bioinformatics studies and tool development related to drug discovery." Thesis, Rhodes University, 2016. http://hdl.handle.net/10962/d1020021.

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This thesis is divided into two distinct sections which can be combined under the broad umbrella of structural bioinformatics studies related to drug discovery. The first section involves the establishment of an online South African natural products database. Natural products (NPs) are chemical entities synthesised in nature and are unrivalled in their structural complexity, chemical diversity, and biological specificity, which has long made them crucial to the drug discovery process. South Africa is rich in both plant and marine biodiversity and a great deal of research has gone into isolatin
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5

Huffman, Olivia G. "Drug Discovery: identification of Anticancer Properties of Podophyllotoxin Analogues." Youngstown State University / OhioLINK, 2020. http://rave.ohiolink.edu/etdc/view?acc_num=ysu1588874335556129.

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6

Hagos, Selam. "Chemical Investigation of Bioactive Marine Extracts." Scholar Commons, 2018. https://scholarcommons.usf.edu/etd/7301.

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Natural products have been a fundamental source of medicinal scaffolds for decades; with sixty percent of marketed drugs. Many synthetic chemists are focused on synthesizing potent and nontoxic compounds for pharmaceutical targets, however, nature is still proving to be a source of new bioactive compounds. Produced by the host organism for defense, reproduction and communication, secondary metabolites also demonstrate promising bioactivity against human pathogens. Hence, natural product chemists continue their quest for new leads. As a continuation
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7

Voser, Tanja M. "Marine Biodiscovery - An Exploration of Chemical Diversity, Antibiotic Discovery, and Invertebrate Natural Product Chemistry." Thesis, Griffith University, 2022. http://hdl.handle.net/10072/414294.

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This thesis covers a wide range of research on marine natural products with a focus on their role in drug discovery. Chapter 1 starts with a general introduction to marine natural product chemistry, describing current trends and problems. It gives an insight into the importance of the discovery of new antibiotics in this pressing time where multidrug-resistant bacteria are on the rise. Chapter 2 is a meta-analysis of current trends in marine microbial natural product research and an analysis of how much of their chemistry overlaps with the chemistry of terrestrial microbial natural products. O
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8

Turbyville, Thomas Jefferson. "Using Phylogenetically Conserved Stress Responses to Discover Natural Products with Anticancer Activity." Diss., Tucson, Arizona : University of Arizona, 2005. http://etd.library.arizona.edu/etd/GetFileServlet?file=file:///data1/pdf/etd/azu%5Fetd%5F1078%5F1%5Fm.pdf&type=application/pdf.

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9

Holland, Darren C. "Marine Natural Products Biodiscovery and Meta-analysis of their Bioactivities to Improve their Potential for Drug Discovery." Thesis, Griffith University, 2022. http://hdl.handle.net/10072/416310.

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Marine natural products biodiscovery continues to evolve into an increasingly more sophisticated and multidisciplinary field. Since the first reported marine compound in the 1970’s, there have been more than 33,000 marine natural products reported in the literature with seventeen marine-derived drugs currently approved for therapeutic use worldwide. Despite this, how much do we really know about marine natural product chemical space with respect to biological activity, and are we examining these precious resources against suitable disease targets that aim to maximise their potentials for drug
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10

Wang, Tao Verfasser], and Jeroen S. [Akademischer Betreuer] [Dickschat. "Discovery of antifungal and antibacterial volatile natural products and synthetic drug analogs / Tao Wang ; Betreuer: Jeroen S. Dickschat." Braunschweig : Technische Universität Braunschweig, 2018. http://d-nb.info/1175815454/34.

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11

Wiley, Jessica Delia. "Investigating the role of the Apicoplast in Plasmodium falciparum Gametocyte Stages." Diss., Virginia Tech, 2014. http://hdl.handle.net/10919/64150.

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Malaria continues to be a global health burden that affects millions of people worldwide each year. Increasing demand for malaria control and eradication has led research to focus on sexual development of the malaria parasite. Sexual development is initiated when pre-destined intraerythrocytic ring stage parasites leave asexual reproduction and develop into gametocytes. A mosquito vector will ingest mature gametocytes during a blood meal. Sexual reproduction will occur in the midgut, leading to the production of sporozoites that will migrate to the salivary gland. The sporozoites will be injec
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12

Strand, Mårten. "The discovery of antiviral compounds targeting adenovirus and herpes simplex virus : assessment of synthetic compounds and natural products." Doctoral thesis, Umeå universitet, Virologi, 2014. http://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-88186.

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There is a need for new antiviral drugs. Especially for the treatment of adenovirus infections, since no approved anti-adenoviral drugs are available. Adenovirus infections in healthy persons are most often associated with respiratory disease, diarrhea and infections of the eye. These infections can be severe, but are most often self-limiting. However, in immunocompromised patients, adenovirus infections are associated with morbidity and high mortality rates. These patients are mainly stem cell or bone marrow transplantation recipients, however solid organ transplantation recipients or AIDS pa
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13

Fries, Jacqueline Lee. "Chemical Investigation of Antarctic Marine Organisms & Their Role in Modern Drug Discovery." Scholar Commons, 2016. http://scholarcommons.usf.edu/etd/6084.

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The chemicals produced by biological systems, whether proteins, peptides, or terpenes, will always provide an intriguing topic for researchers. Invisibly controlling every aspect of nature, these molecules are responsible for life, evolution, and death. Specifically, here is described the secondary metabolites produced by Antarctic marine organisms as well as others, and how they are used to defend or attract other animals while potentially providing health benefits to mankind. This is done through collection, extraction, and separation of individual specimens. The respective mixtures of compo
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14

Kumar, Rohitesh. "Design and Synthesis of Natural Product-Based Screening Libraries." Thesis, Griffith University, 2017. http://hdl.handle.net/10072/366694.

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Natural products (NPs) continue to have significant impact in the area of drug discovery and development. More than 50% of the approved drugs between 1981 and 2014 were either unaltered NPs, NP derivatives or synthetic drugs inspired by NP pharmacophores. NPs have also served as lead molecules in drug development programs; noteworthy example include the semi-synthetic antifungal drugs caspofungin, anidulafungin, and micafungin that were based on NP lead compounds isolated from the fermentation products of various fungus. Other notable examples include the sponge metabolite halichondrin B that
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15

Knestrick, Matthew A. "From Florida to Antarctica: Dereplication Strategies and Chemical Investigations of Marine Organisms." Scholar Commons, 2018. https://scholarcommons.usf.edu/etd/7635.

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In the fight against disease and illness, nature has provided mankind some of our best therapeutics in the form of secondary metabolites. The plant, fungi and animal phyla inhabiting the Earth produce diverse and unique chemistry that can be used in our fight against disease. In the growing threat of drug resistance and pathogen evolution, the field of natural products chemistry strives to explore new biological and chemical diversity sources, and develop innovative methodology to identify and isolate new chemistry faster than ever. The dissertation herein presented is one such effort to find
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16

Faraone, Immacolata. "Pharmacological potential and phytochemical profile of three unexplored medicinal plants." Doctoral thesis, Universita degli studi di Salerno, 2019. http://elea.unisa.it:8080/xmlui/handle/10556/4256.

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2017 - 2018<br>Nature is a wide source of biologically active compounds investigated with the purpose to be used as drugs due to their biological activity and also useful in pharmaceutical discovery and drug design. Nowadays, medicinal plants play a major role in primary health care as therapeutic remedies in many developing countries. The aim of my PhD project was the phytochemical and biological investigation of three plant species, used in Bolivian traditional medicine, but few scientific studies were reported, such as: Azorella glabra Wedd., Minthostachys diffusa Epl. and Senecio cli
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17

Jones, Michael David. "Studies investigating sub-2 μm particle stationary phase supercritical fluid chromatography and application to profiling of natural products and drug discovery research". Thesis, King's College London (University of London), 2017. https://kclpure.kcl.ac.uk/portal/en/theses/studies-investigating-sub2-m-particle-stationary-phase-supercritical-fluid-chromatography-and-application-to-profiling-of-natural-products-and-drug-discovery-research(744340dd-0d8e-4a7d-aaaf-707f89aabec5).html.

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The aim of this thesis was to investigate a novel prototype supercritical fluid chromatography instrumentation optimized to exploit the theoretical benefits of sub-2 μm particle stationary phases and determine the benefits of its applied use towards the discovery and early drug development of new chemical entities found in natural products. The protoype supercritical instrument was designed to reduce the system and extra-column volumes in order to reach the theoretical efficiencies of a sub-2 μm particle stationary phase. The system was also designed to decrease baseline noise and drift via de
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18

Saunders-Mattingly, Meredith A. "DISCOVERY OF NATURAL PRODUCT ANALOGS AGAINST ETHANOL-INDUCED CYTOTOXICITY IN HIPPOCAMPAL SLICE CULTURES." UKnowledge, 2018. https://uknowledge.uky.edu/psychology_etds/142.

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An estimated 13.9% of Americans currently meet criteria for an alcohol (ethanol; EtOH) use disorder (AUD). While there are 4 medications approved by the Food and Drug Administration (FDA) to treat AUD, these treatments have demonstrated poor clinical efficacy. Our ongoing research program encompasses a multi-tiered screening of a natural product library and validation process to provide novel information about the mechanisms underlying EtOH-induced changes in neurobiology and to identify novel chemical scaffolds to be exploited in the development of pharmacological treatments for AUD in a rode
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19

Heilmann, Geronimo [Verfasser], and Markus [Akademischer Betreuer] Kaiser. "The use of mass-spectrometry-based chemical proteomics approaches in bioactivity annotation of natural products and biocatalyst discovery : Applications to the natural product Zelkovamycin and fungi / Geronimo Heilmann ; Betreuer: Markus Kaiser." Duisburg, 2020. http://d-nb.info/1221960318/34.

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20

Mazraati, Tajabadi Fatemeh. "Identification of 3D Scaffolds Embedded in Natural Products and Synthesis of Focused Libraries." Thesis, Griffith University, 2017. http://hdl.handle.net/10072/365575.

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The ever-increasing demand for new drugs drives the need to explore new areas of biologically-relevant chemical space. Drug targets, largely the active sites of proteins, have three-dimensional shape. However, chiefly for reasons of synthetic tractability, the screening libraries that are extensively used for high throughput screening (HTS) drug discovery are mostly composed of flat aromatic and heteroaromatic compounds.1 This has resulted in a trend towards flatness in drug candidates, limiting the possibilities in the navigation of three-dimensional biological space. A variety of approaches,
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21

Manwill, Preston Kim. "Discovery and Development of Natural Products from Plant and Microbial Sources: Drimane Sesquiterpenes and Abyssomicins as Mosquito Control and Antimicrobial Agents." The Ohio State University, 2020. http://rave.ohiolink.edu/etdc/view?acc_num=osu1591285556969447.

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22

Lane, Amy L. "Marine natural products as antimicrobial chemical defenses and sources of potential drugs." Diss., Atlanta, Ga. : Georgia Institute of Technology, 2008. http://hdl.handle.net/1853/26556.

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Thesis (Ph. D.)--Chemistry and Biochemistry, Georgia Institute of Technology, 2009.<br>Committee Chair: Kubanek, Julia; Committee Member: Fernandez, Facundo M.; Committee Member: Harvey, Stephen C.; Committee Member: Hay, Mark E.; Committee Member: Hud, Nicholas V. Part of the SMARTech Electronic Thesis and Dissertation Collection.
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23

Cockroft, Nicholas T. "Applications of Cheminformatics for the Analysis of Proteolysis Targeting Chimeras and the Development of Natural Product Computational Target Fishing Models." The Ohio State University, 2019. http://rave.ohiolink.edu/etdc/view?acc_num=osu156596730476322.

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24

Bovio, Elena. "Champignons marins d'éponges marines : biodiversité, chimiodiversité et applications biotechnologiques." Thesis, Université Côte d'Azur (ComUE), 2019. http://theses.univ-cotedazur.fr/2019AZUR4009.

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L'environnement marin est doté d’une diversité fongique encore trop faiblement explorée puisqu’on estime qu’environ 10% des champignons marins ont fait l’objet d’une étude. Dans ce contexte, le projet de thèse décrit dans ce manuscrit est focalisé sur le potentiel biotechnologique des champignons marins isolés d’éponges marines. Ces champignons sont caractérisés par une importante biodiversité et chimiodiversité susceptible de conduire à de nouvelles molécules bioactives. Il s’agit d’un projet pluridisciplinaire qui joint la mycologie, la chimie, la biochimie et les biotechnologies. Il couvre
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25

Alsherbiny, Muhammad A. "Adventures in natural products drug discovery : metabolomic, proteomic, synergy and deep learning studies." Thesis, 2021. http://hdl.handle.net/1959.7/uws:67234.

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In the present project, integrated untargeted metabolomic profiling and antiproliferative assays were implemented for smart identification of the antiproliferative metabolites of Australian propolis against MCF7 breast cancer cells. The synergistic chemotherapeutic combinations of the Australian propolis or cannabinoids such as cannabidiol were investigated and validated against different synergy quantitation models and designs. Moreover, label-free quantification proteomics studies were employed to elucidate the potential mechanism of action and biological targets of the mono treatment or the
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26

Del, Gaudio Chiara. "From natural products chemistry to HTS by NMR: different approaches in drug discovery." Tesi di dottorato, 2015. http://www.fedoa.unina.it/10393/1/C_Del%20Gaudio_Phd%20Thesis.pdf.

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The process of drug discovery, by which new potential medicines are discovered, is a long and intricate path that can be approached with many different strategies. For a long time, drugs have been discovered by studying secondary metabolites produced by plants and other organisms mainly as defense or as a way to interact with competitors and mutualists. During recent years, high-throughput screening (HTS) of large compounds libraries has become very popular since it promised to drastically fasten the process of hit identification though requiring consistent initial investments. However, despit
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27

D'Aniello, Filomena. "Characterization of new bioactive natural products from marine sources as pharmaceutical tools and lead compounds in drug discovery processes." Tesi di dottorato, 2014. http://www.fedoa.unina.it/9845/1/d%27aniello%20filomena.pdf.

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Natural products have historically been a rich source of “lead compounds” in drug discovery. The investigation of terrestrial plants and marine organisms aimed at searching new biologically active compounds is a central issue of this kind of studies, trough structure elucidation combined with biological tests. My research activity has been mainly devoted to the discovery and to the chemical and pharmacological investigation of new bioactive natural products as “lead compounds” in the area of antitumor, anti inflammatory and antimalarial activities. My research work, described in this PhD thesi
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28

Rodrigues, Ana Rita Miradouro. "Produtos naturais na descoberta de fármacos." Master's thesis, 2018. http://hdl.handle.net/10284/6660.

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Desde sempre que os produtos naturais têm sido uma fonte rica para a descoberta de compostos bioativos a serem utilizados no desenvolvimento de medicamentos. Para isso muito contribui a grande diversidade de recursos naturais, quer terrestes quer marinhos. A Organização Mundial de Saúde (OMS) alertou para a importância da biodiversidade, a qual seria capaz de fornecer soluções terapêuticas acessíveis para a maioria da população mundial. A presente dissertação baseia-se numa revisão bibliográfica do uso de produtos naturais na descoberta de fármacos. Após uma contextualização histórica do tema,
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