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Dissertations / Theses on the topic '"targeted activity"'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

Laporte, Aimée Nicole. "Targeted activity of histone deacetylase inhibition in synovial sarcoma." Thesis, University of British Columbia, 2017. http://hdl.handle.net/2429/62602.

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Synovial sarcoma is an aggressive soft tissue cancer affecting primarily adolescents and young adults and characterized by the known chimeric fusion oncoprotein SS18-SSX resulting from a t(X;18) translocation. Oncoprotein-mediated interactions with chromatin-modification proteins are known to influence transformation; however targeted therapies are not currently available. Patients remain at high-risk for local recurrence and metastasis and see a 10-year survival rate of approximately 50%. Accordingly, it was hypothesized that therapeutic compounds able to disrupt the SS18-SSX driving complex

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2

Franzman, Michael Ryan. "Targeted antimicrobial activity of SMAP28 conjugated to IgG antibody." Thesis, University of Iowa, 2007. http://ir.uiowa.edu/etd/140.

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3

Smith, Peter Gerard. "Potentiation of multi-targeted antifolate activity by novel dipyridamole analogues." Thesis, University of Newcastle Upon Tyne, 2000. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.311118.

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4

Morales, Kimberly. "RAD52 DNA Binding Activity Can Be Targeted to Eliminate CML Stem Cells." Diss., Temple University Libraries, 2012. http://cdm16002.contentdm.oclc.org/cdm/ref/collection/p245801coll10/id/190030.

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Biology<br>Ph.D.<br>BCR-ABL1 transforms hematopoietic stem cells into leukemia stem cells (LSCs) to induce chronic myeloid leukemia in chronic phase. Expression of BCR-ABL1 stimulates production of elevated levels of reactive oxygen species (ROS), which induce oxidative DNA damage. CML cells accumulate excessive amounts of ROS-induced DNA damage which can be converted to potentially lethal DNA double strand breaks (DSBs). BCR-ABL1 stimulates enhanced Rad51-mediated DSB repair by the homologous recombination repair (HRR) pathway. In these studies we show BCR-ABL1-transformed cells depend on Rad

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5

Jeldi, Artaban Johnson. "Physical activity following total hip replacement : measurement and enhancement using a targeted stepping intervention." Thesis, Glasgow Caledonian University, 2016. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.700995.

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6

Tanaka, Ruriko. "Activity of the multi-targeted kinase inhibitor, AT9283, in imatinib-resistant BCR-ABL positive leukemic cells." Kyoto University, 2011. http://hdl.handle.net/2433/142109.

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7

Sathanantham, Preethi. "Impact of Mutations of Targeted Serine, Histidine, and Glutamine Residues in Citrus paradisi Flavonol Specific Glucosyltransferase Activity." Digital Commons @ East Tennessee State University, 2015. https://dc.etsu.edu/etd/2560.

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A flavonol specific glucosyltransferase cloned from Citrus paradisi has strict substrate and regio-specificity (Cp3OGT). The amino acid sequence of Cp3OGT was aligned with sequences of an anthocyanidin UDP- dependant glucosyltransferase (UGT) from Clitorea ternatea and a UGT from Vitis vinifera that can glucosylate both flavonols and anthocyanidins. Using homology modeling to identify candidate regions followed by site directed mutagenesis, three double mutations were constructed and biochemically characterized. S20G+T21S mutant protein retained activity with flavonols similar to the wildtype

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8

GIACOBINI, GIANLUCA. "Identification of immune correlates of clinical activity and/or disease outcome in melanoma patients undergoing targeted therapy." Doctoral thesis, Università di Siena, 2018. http://hdl.handle.net/11365/1051713.

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BRAF inhibitors (BRAFi) have been shown to modulate the immune responses in metastatic melanoma (MM) patients treated with this agent. In this study, Peripheral Blood Mononuclear Cells (PBMCs) were collected from 34 MM patients, selected on the basis of HLA-A typing, at baseline and at three different time points post-BRAFi treatment (week 4 - 12 - 18). The recognition by circulating T cells of tumor cell lines and tumor associated antigens (TAAs; NY-ESO-1, MAGE-A1, A2 or A3, Gp100, MART-1, TYR, H-TERT, SVV-1, SOX-2) was evaluated by IFN-γ release assay. The correlation between antigen-specifi

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9

Kadir, Mohammad Abdul. "Inspiring Patients with Overweight and Obesity to Participate in a Walking Program: A Comprehensive Formative Research Study." Thesis, Griffith University, 2016. http://hdl.handle.net/10072/366595.

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Understanding the target audience and targeted behaviour through comprehensive formative research is essential for designing an effective behaviour change intervention. Formative research is an essential benchmark criterion of Social Marketing framework (Andreasen, 2002). This thesis responds to calls for broader formative research approaches to be undertaken (Rundle-Thiele, Russell-Bennett, Leo, & Dietrich, 2013) employing a narrative literature review, a qualitative inquiry and finally a quantitative study in the form of an online survey to generate consumer insights that could be used in in

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10

Mercatali, Laura <1977&gt. "Evaluation of Antitumoral activity of bone targeted drugs/conventional chemotherapies and identification of biomarkers for the selection of patients with breast cancer for the bone targeted therapy in adjuvant setting." Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2014. http://amsdottorato.unibo.it/6394/1/Mercatali_Laura_tesi.pdf.

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Bone metastases are responsible for different clinical complications defined as skeletal-related events (SREs) such as pathologic fractures, spinal cord compression, hypercalcaemia, bone marrow infiltration and severe bone pain requiring palliative radiotherapy. The general aim of these three years research period was to improve the management of patients with bone metastases through two different approaches of translational research. Firstly in vitro preclinical tests were conducted on breast cancer cells and on indirect co-colture of cancer cells and osteoclasts to evaluate bone targeted the

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Mercatali, Laura <1977&gt. "Evaluation of Antitumoral activity of bone targeted drugs/conventional chemotherapies and identification of biomarkers for the selection of patients with breast cancer for the bone targeted therapy in adjuvant setting." Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2014. http://amsdottorato.unibo.it/6394/.

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Bone metastases are responsible for different clinical complications defined as skeletal-related events (SREs) such as pathologic fractures, spinal cord compression, hypercalcaemia, bone marrow infiltration and severe bone pain requiring palliative radiotherapy. The general aim of these three years research period was to improve the management of patients with bone metastases through two different approaches of translational research. Firstly in vitro preclinical tests were conducted on breast cancer cells and on indirect co-colture of cancer cells and osteoclasts to evaluate bone targeted the

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12

Bruno, Samantha <1989&gt. "Exploring novel targeted therapeutic strategies against Acute Myeloid Leukemia cells based on inhibition of bromodomain proteins and CDC20 activity." Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2020. http://amsdottorato.unibo.it/9351/1/PhD%20Thesis%20Bruno%20S..pdf.

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Acute myeloid leukemia (AML) is a haematological malignancies arising from the accumulation of undifferentiated myeloid progenitors with an uncontrolled proliferation. The genomic landscape of AML revealed that the disease is characterized by high level of heterogeneity and is subjected to clonal evolution driven by selective pressure of chemotherapy. In this study, we investigated the therapeutic effects of the inhibition of BRD4 and CDC20 in vitro and ex vivo. We demonstrated that inhibition of BRD4 with GSK1215101A in AML cell lines was effective under hypoxia. It induced the activation o

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13

Bapat, Aditi Ajit. "Inhibition of Ape1's DNA repair activity as a target in cancer identification of novel small molecules that have translational potential for molecularly targeted cancer therapy /." Connect to resource online, 2009. http://hdl.handle.net/1805/2062.

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Thesis (Ph.D.)--Indiana University, 2009.<br>Title from screen (viewed on February 2, 2010). Department of Biochemistry and Molecular Biology, Indiana University-Purdue University Indianapolis (IUPUI). Advisor(s): Mark R. Kelley, Millie M. Georgiadis, John J. Turchi, Martin L. Smith. Includes vitae. Includes bibliographical references (leaves 114-133).

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14

LA, MONICA Gabriele. "Correlation between cell line chemosensitivity and protein expression pattern as new approach for the design of targeted anticancer small molecules." Doctoral thesis, Università degli Studi di Palermo, 2022. https://hdl.handle.net/10447/573085.

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BACKGROUND AND RATIONALE: Over the past few decades, several databases with a significant amount of biological data related to cancer cells and anticancer agents (e.g.: National Cancer Institute database, NCI; Cancer Cell Line Encyclopedia, CCLE; Genomic and Drug Sensitivity in Cancer portal, GDSC) have been developed. The huge amount of heterogeneous biological data extractable from these databanks (among all, drug response and protein expression) provides a real foundation for predictive cancer chemogenomics, which aims to investigate the relationships between genomic traits and the response

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15

Köster, Stephan David [Verfasser], Nils [Gutachter] Metzler-Nolte, and Ingo [Gutachter] Ott. "Towards mitochondria-targeted organometallic peptide bioconjugates : synthesis, biological activity and mode of action / Stephan David Köster ; Gutachter: Nils Metzler-Nolte, Ingo Ott ; Fakultät für Chemie und Biochemie." Bochum : Ruhr-Universität Bochum, 2012. http://d-nb.info/1230628576/34.

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16

Pestel, Galina Farina. "Synthese und biologische Evaluation neuartiger Duocarmycin-Analoga für eine selektive Krebstherapie." Doctoral thesis, Niedersächsische Staats- und Universitätsbibliothek Göttingen, 2012. http://hdl.handle.net/11858/00-1735-0000-001D-BF65-4.

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Herkömmliche Zytostatika greifen vornehmlich in den Zellzyklus ein und somit werden Zellen mit hoher Proliferationsrate geschädigt. Allerdings fallen hierunter nicht ausschließlich Krebszellen, sondern auch gesunde, schnell proliferierende Gewebearten. Auf Grund dessen verursacht eine klassische Chemotherapie schwerwiegende Nebenwirkungen. Neuere Therapieansätze greifen daher geno- sowie phänotypischer Unterschiede zwischen malignen und gesunden Zellpopulationen auf und können selektiv den zytotoxischen Wirkstoff in die Tumorpopulation einbringen. Dazu werden sogenannte Prodrug-Konzepte verfol

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17

Stigsson, Marie, and Johanna Jaran. "Riktade hälsosamtal i Skåne: Analys av samtidig validitet hos frågor om självskattad fysisk aktivitet samt kartläggning av stillasittande." Thesis, Högskolan Dalarna, Institutionen för hälsa och välfärd, 2021. http://urn.kb.se/resolve?urn=urn:nbn:se:du-38068.

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Background: “Targeted health dialogues” is a preventive method that aims to reduce the risk of cardiovascular disease and type 2 diabetes. It includes a health-survey containing physical activity (PA)-questions. Health region Skåne introduced the method 2020 and decided to add additional questions about PA and sedentary behavior (SB). With the wish to replace current validated PA-questions with new validated questions and describe SB. Aim: Analyze concurrent validity between the answers of the original PA-questions (kcal/week) in the method and new answers (activity-minutes/last 7-days) and de

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18

Marie, Solène. "Imagerie translationnelle pour la mise en évidence des répercussions pharmacocinétiques des transporteurs de médicaments Imaging Probes and Modalities for the Study of Solute Carrier O (SLCO)-Transport Function In Vivo Validation of Pharmacological Protocols for Targeted Inhibition of Canalicular MRP2 Activity in Hepatocytes Using [99mTc]mebrofenin Imaging in Rats." Thesis, université Paris-Saclay, 2020. http://www.theses.fr/2020UPASQ004.

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La distribution des médicaments du sang vers les tissus, où ils exercent leurs effets pharmacologiques et/ou toxiques, implique souvent des transporteurs qui régulent leur passage membranaire. Les transporteurs Organic Anion-Transporting Polypeptide (OATP), avec d’autres systèmes de transporteurs hépatocytaires, participent à l’élimination hépatique de nombreux médicaments. Certains OATPs ont été retrouvés dans d’autres organes où leurs répercussions pharmacocinétiques restent mal connues.L’objectif de ce travail a été de développer des approches d’imagerie originales permettant de mesurer sél

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19

Zhang, Chunyi. "The Ppz protein phosphatase as a potential novel antifungal target." Doctoral thesis, Universitat Autònoma de Barcelona, 2019. http://hdl.handle.net/10803/667263.

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Las infecciones fúngicas invasivas son una amenaza enorme, pero actualmente solo hay un limitado número de medicamentos antifúngicos disponibles. El aumento de la incidencia de infecciones fúngicas ha agravado la necesidad de nuevos enfoques para las terapias antifúngicas. Nuestro laboratorio descubrió en S. cerevisiae la proteína fosfatasa (PPasa) Ppz1, que participa en múltiples procesos celulares y es importante en la regulación de la homeostasis de los cationes monovalentes. En la levadura, Ppz1 está inhibida por dos proteínas reguladoras, Hal3 y Vhs3. Estas dos proteínas tienen propiedade

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20

Andrews, Timothy John. "The role of targets and growth factors in neuronal ageing." Thesis, University College London (University of London), 1993. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.307442.

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21

ZANCHETTA, MELANIA EVA. "BRAF35 as target of MID1/TRIM18 E3 ligase activity." Doctoral thesis, Università degli Studi di Trieste, 2016. http://hdl.handle.net/11368/2908069.

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TRIM proteins are a family of ubiquitin E3 ligase enzymes characterized by the presence of a conserved N-terminus, the tripartite motif, which consists of a RING finger domain, two B-box motifs and an alpha-helical Coiled-coil region (RBCC). We focused our attention on TRIM18/MID1, the gene responsible for the X-linked form of Opitz G/BBB syndrome, a congenital disease characterized by defects in midline development and mental retardation. More recently, MID1 has also been found as overexpressed in some aggressive prostate cancers. The role of MID1 within the cell and the target(s) of its E3 u

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22

ZHAO, CHEN. "DECIPHERING TRANSCRIPTIONAL ACTIVITY OF DROSOPHILA BICOID MORPHOGEN: SELECTIVITY AND REGULATION." University of Cincinnati / OhioLINK, 2001. http://rave.ohiolink.edu/etdc/view?acc_num=ucin1006196849.

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23

Wang, Qing. "Target payment and the UK NHS general practitioners service activity." Thesis, University of York, 2006. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.441059.

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24

Myles, Kimberly. "Activity-Based Target Acquisition Methods for Use in Urban Environments." Diss., Virginia Tech, 2009. http://hdl.handle.net/10919/28422.

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Many military conflicts are fought in urban environments that subject the U.S. soldier to a number of challenges not otherwise found in traditional battle. In the urban environment, the soldier is subject to threatening attacks not only from the organized army but also from civilians who harbor hostility. U.S. enemies use the civilian crowd as an unconventional tactic to blend in and look like civilians, and in response to this growing trend, soldiers must detect and identify civilians as a threat or non-threat. To identify a civilian as a threat, soldiers must familiarize themselves with b

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25

Dy, Diane Jazmin. "S. aureus bacteria a new target of serum calcification activity /." Diss., [La Jolla] : University of California, San Diego, 2009. http://wwwlib.umi.com/cr/ucsd/fullcit?p1465072.

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Thesis (M.S.)--University of California, San Diego, 2009.<br>Title from first page of PDF file (viewed June 19, 2009). Available via ProQuest Digital Dissertations. Includes bibliographical references (p. 35-37).

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26

Arnold, Kevin. "Chitinolytic activity in nematodes and other parasites : a possible chemotherapeutic target." Thesis, University of Aberdeen, 1991. http://digitool.abdn.ac.uk/R?func=search-advanced-go&find_code1=WSN&request1=AAIU546293.

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Chitin is present in the eggshells of <i>Heligmosomoides polygyrus </i>(5% of dry egg weight) and <i>Caenorhabditis elegans</i>. The chitinolytic activities from a number of parasite sources were examined by the use of a range of fluorometric substrates based on methylumbelliferyl glycosides. The chitinase inhibitor, allosamidin had varied effects on chitinolytic activities dependent on parasite source and substrate used. Nematode chitinases were the most sensitive with an IC<SUB>50</SUB> of 2.2 nM for <i>H. polygyrus</i> eggs. Treatment with allosamidin slowed but did not prevent hatching of

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27

Russo, Alessandra. "Design, synthesis and biological activity of new target selective antitumoral agents." Doctoral thesis, Universita degli studi di Salerno, 2018. http://hdl.handle.net/10556/3037.

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2016 - 2017<br>Cancer development is a complex pathological process that exploits a variety of biological actors. The identification of new molecular entities able to interfere with new biological targets, involved in tumorigenesis, is strongly needed, both for the development of new promising drug candidates, and, as chemical probes useful to further investigate less understood biological aspects. Two main targets, involved at different levels, in cancer development, have been thoroughly investigated: Macrodomain proteins, MacroD1 and MacroD2, and the Bcl-2 associated athanogene 3, BAG3 prote

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Canon, Louise. "Mechanistic and structural basis for tuning of myosin activity." Electronic Thesis or Diss., Université Paris sciences et lettres, 2022. http://www.theses.fr/2022UPSLS064.

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Les nanomoteurs des cellules Eucaryotes leur permettent d'accomplir de nombreuses tâches mécaniques complexes, nécessaires à la génération de tensions dans des emplacements cellulaires précis. Le transport ou la fixation de vésicules dans des voies d'endocytose et de sécrétion peuvent par exemple en résulter. Parmi ces moteurs, les myosines sont capables, à partir de l’hydrolyse de l’ATP, de générer de la force en association avec des filaments d'actine. Les myosines se divisent en plusieurs classes impliquées dans un large panel de fonctions et de pathologies. Leur dysfonctionnement peut entr

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29

Zacharias, Eric. "Activist Investor Impact on CEO Compensation of Investment Targets." Scholarship @ Claremont, 2010. http://scholarship.claremont.edu/cmc_theses/2.

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This paper examines the “activist effect” on the levels and structures of CEO compensation when a company is targeted by a sample of activist groups. Activist investors are focused funds that use their resources to influence management of target investments in an effort to increase shareholder value. Due to their efforts to impose return enhancing agendas on the management of targets, activists have developed a reputation as “raiders” and are commonly feared by management. In this paper, the nature of activist investing is discussed, including a review of previous research on activism, and an

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30

Sjögren, Martin. "Bioactive compounds from the marine sponge Geodia barretti : characterization, antifouling activity and molecular targets /." Uppsala : Acta Universitatis Upsaliensis : Universitetsbiblioteket [distributör], 2006. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-6797.

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31

LOBO, Lis Tavares Coelho. "Study of antimalarial activity of new endoperoxides: potential parasite targets and mechanisms of action." Doctoral thesis, Instituto de Higiene e Medicina Tropical, 2019. http://hdl.handle.net/10362/77868.

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A malária é uma das doenças parasitárias mais prevalentes no mundo, causando um grande impacto no desenvolvimento socioeconómico dos países afetados. Esta doença afeta principalmente a África Subsaariana, mas continua presente em 87 países de regiões tropicais e subtropicais da América do Sul e Sudeste da Ásia. O surgimento e propagação de resistências do Plasmodium falciparum à terapia combinada à base de artemisinina (ACT) no sudeste da Ásia acentuou a necessidade de desenvolver novos antimaláricos e/ou medicamentos baseados no farmacóforo endoperóxido. Neste contexto, uma biblioteca quimi

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32

Sanusi, Junedah Bt. "The possible role of afferent activity in motoneurone survival after neonatal target-deprivation." Thesis, University College London (University of London), 1996. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.244770.

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Noori, Mahboubeh Sadat. "Aberrant Biomolecular Expression and Activity as a Target for Novel Diagnostics and Therapeutics." Ohio University / OhioLINK, 2019. http://rave.ohiolink.edu/etdc/view?acc_num=ohiou1572277204077271.

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34

Dumas, Guillaume. "La gestion des résultats des entreprises innovantes." Thesis, Toulouse 1, 2014. http://www.theses.fr/2014TOU10039/document.

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Cette thèse s’intéresse à la gestion des résultats dans le cadre des entreprises innovantes. Elle est constituée de trois articles. Dans le premier, il s’agit d’examiner si les résultats des entreprises innovantes sont gérés et si le stade de développement des innovations influence cette gestion des résultats. Il apparaît que les résultats des entreprises innovantes sont gérés à la hausse. Cette gestion ne semble intervenir qu’au cours de l’activité d’innovation (c’est-à-dire lorsque les entreprises investissent en R&D) ; l’achèvement des innovations n’incitant pas les dirigeants à gérer l

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35

Hedner, Erik. "Bioactive Compounds in the Chemical Defence of Marine Sponges : Structure-Activity Relationships and Pharmacological Targets." Doctoral thesis, Uppsala University, Division of Pharmacognosy, 2007. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-8218.

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<p>Marine invertebrates, in particular sponges, represent a source of a wide range of secondary metabolites, many of which have been attributed various defensive capabilities against environmental stress factors. In this thesis sponge-derived low-molecular peptide-like compounds and associated analogs are investigated for bioactivity and pharmacological targets. </p><p>The compound bromobenzisoxazolone barettin (cyclo[(6-bromo-8-(6-bromo-benzioxazol -3(1H)-one)-8-hydroxy)tryptophan)]arginine) was isolated from the sponge <i>Geodia barretti</i> and its ability to inhibit larval settlement of th

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Watson, Anna Frances. "Structure-activity studies for inhibitors of two cancer targets : Tip60 histone acetyltransferase and MDM2- p53." Thesis, University of Newcastle Upon Tyne, 2010. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.610978.

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Dunaway, Adam Blake. "Characterization of the binding activity of immobilized DNA aptamers for nucleotide and non-nucleotide targets." Thesis, Georgia Institute of Technology, 2014. http://hdl.handle.net/1853/54310.

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Deoxyribonucleic acid (DNA) aptamers are oligonucleotides with high specificity and affinity for non-nucleotide targets ranging from molecular species to cellular proteins. Their high affinity, rapid synthesis, and the ease with which they can be chemically modified to include convenient chemical groups (e.g. amine group on 5’ end) make them excellent adaptable ligands for use in colloidal drug delivery vehicles for both uptake and release of therapeutic agents. This work uses pre-identified aptamers for vascular endothelial growth factor (VEGF) to investigate the design of one such vehicle fo

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Standard, Joseph Tabb. "Mechanistic targets of weight loss-induced cancer prevention by dietary calorie restriction and physical activity." Thesis, Kansas State University, 2013. http://hdl.handle.net/2097/15937.

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Master of Science<br>Department of Human Nutrition<br>Weiqun Wang<br>Weight control through either dietary calorie restriction (DCR) or exercise is associated with cancer prevention in animal models. However, the underlying mechanisms are not fully defined. Bioinformatics approaches using genomics, proteomics, and lipidomics were employed to elucidate the profiling changes of genes, proteins, and phospholipids in response to weight loss by DCR or exercise in a mouse skin cancer model. SENCAR mice were randomly assigned into 4 groups for 10 weeks: ad lib-fed sedentary control, ad lib-fed exerci

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Baldo, Fatima Magdi Hamza. "Integrating chemical, biological and phylogenetic spaces of African natural products to understand their therapeutic activity." Thesis, University of Cambridge, 2019. https://www.repository.cam.ac.uk/handle/1810/289714.

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This research aims to utilise ligand-based target prediction to (i) understand the mechanism of action of African natural products (ANPs), (ii) help identify patterns of phylogenetic use in African traditional medicine and (iii) elucidate the mechanism of action of phenotypically active small molecules and natural products with anti-trypanosomal activity. In Chapter 2 the objective was to utilise ligand-based target prediction to understand the mechanism of action of natural products (NPs) from African medicinal plants used against cancer. The Random Forest classifier used in this work compare

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Bosne, Stéphanie. "Characterization of Plasmodium falciparum membrane transporters as potential antimalarial targets." Thesis, Paris 11, 2014. http://www.theses.fr/2014PA11T052/document.

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La découverte de nouveaux agents antipaludiques est primordiale. A travers le monde, les chercheurs se sont focalisés sur plusieurs stratégies. Les plus développées sont : soit les tests de molécules issues de bibliothèques chimiques dans une recherche phénotypique (comme le test direct d’agents sur des cultures de parasites in vitro), soit la recherche de nouvelles molécules agissant sur l’activité d’une cible ou d’une voie spécifique et essentielle. Cette thèse est centrée sur le second type d’approche. Nous nous sommes intéressés aux transporteurs membranaires de P. falciparum. Pour cela, n

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Ordway, Gregory A., W. D. Gill, J. B. Coleman, Hui Wang-Heaton, and Russell W. Brown. "Anti-Inflammatory PARP Inhibitor Demonstrates Antidepressant Activity in Animal Model of Treatment Resistant Depression." Digital Commons @ East Tennessee State University, 2019. https://dc.etsu.edu/etsu-works/8643.

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Background: Major depressive disorder is associated with elevated levels of DNA oxidation, DNA damage, and gene expression of DNA repair enzymes including poly (ADP-ribose) polymerase-1 (PARP1). Elevated PARP1 activity is directly linked to neuroinflammation and PARP inhibitors are anti-inflammatory and neuroprotective. We previously showed that PARP inhibitors produce antidepressant-like effects equivalent to fluoxetine in rodent models. Here, we examined whether the PARP inhibitor 3-aminobenzamide (3AB) is effective in a rat model of treatment-resistant depression. Methods: Treatment-resis

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Sjögren, Martin. "Bioactive Compounds from the Marine Sponge Geodia barretti : Characterization, Antifouling Activity and Molecular Targets." Doctoral thesis, Uppsala universitet, Institutionen för läkemedelskemi, 2006. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-6797.

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The marine sponge Geodia barretti produces a range of secondary metabolites. Two of these compounds were isolated and elucidated guided by their ability to inhibit settlement of cypris larvae of the barnacle Balanus improvisus. The compounds barettin (cyclo-[(6-bromo-8-en-tryptophan)-arginine]) as E/Z mixture and 8,9-dihydrobarettin (cyclo-[6-bromo-tryptophan)-arginine]) were determined by using mass spectrometry, nuclear magnetic resonance and quantitative amino acid analysis.The bioactivity of these brominated dipeptides is in the range of antifouling substances used today: EC50 values of 0.

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Elkovich, Andrea J. "The DNA methyltransferase inhibitor, guadecitabine, targets tumor-induced myelopoiesis and recovers T cell activity to slow tumor growth." VCU Scholars Compass, 2019. https://scholarscompass.vcu.edu/etd/5792.

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Myeloid Derived Suppressor Cells (MDSC) represent a significant hurdle to cancer immunotherapy because they dampen anti-tumor cytotoxic T cell responses. Previous studies have reported on the myelo-depletive effects of certain chemotherapies. Using guadecitabine, a next-generation DNA methyltransferase inhibitor (DNMTi), we observed significantly reduced tumor burden in the 4T1 murine mammary carcinoma model. Guadecitabine treatment prevents excessive tumor-induced myeloid proliferation and systemic accumulation, and skews remaining MDSCs toward a beneficial antigen-presenting phenotype. Toget

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Barton, Victoria. "Design and synthesis of activity based probes to investigate the biological target(s) of the endoperoxide antimalarials." Thesis, University of Liverpool, 2009. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.511090.

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Troutman, Jerry. "ISOPRENOID ANALOGS AS CHEMICAL GENETIC TOOLS TO PROVIDE INSIGHTS INTO FARNESYL TRANSFERASE TARGET SELECTION AND CELLULAR ACTIVITY." UKnowledge, 2006. http://uknowledge.uky.edu/gradschool_diss/212.

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Protein farnesylation is an essential post-translational modification required for the function of numerous cellular proteins including the oncoprotein Ras. The farnesyl transferase (FTase) catalyzed reaction is unique because farnesyl diphosphate (FPP), the farnesyl group donor for the reaction, forms a significant portion of a target protein binding site. The major goal of this research was to exploit this unique property of the FTase reaction and determine if changing the structure of the farnesyl donor group would affect FTase protein targeting. A small library of structural analogues of F

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Arendsen, Laura Janine. "A multi-method approach to understanding pain experience using non-pharmacological interventions that target alpha brain activity." Thesis, University of Leeds, 2017. http://etheses.whiterose.ac.uk/19837/.

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This thesis aimed to examine the relationship between pre-stimulus somatosensory alpha activity and pain experience. Four studies were included to assess: 1) if, and how pre-stimulus somatosensory alpha activity might affect pain experience; and 2) if the relationship between pre-stimulus somatosensory alpha activity and pain experience is influenced by uncertainty about pain intensity, fear of pain and pain catastrophising. Study 1 was designed to replicate the negative correlation between pre-stimulus somatosensory alpha activity and pain. Studies 2-4 each investigated the potential of a dif

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Strong, Kathryn A. "Weight Gain Prevention: Identifying Targets for Health Behavior Change in Young Adults Atttending College." Thesis, Virginia Tech, 2007. http://hdl.handle.net/10919/44026.

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The increasing prevalence of overweight and obesity suggests that current policies and interventions have been inadequate to counteract the driving forces. Young adults attending college gain weight at a faster rate than the general population, without evidence of compensatory weight loss. Therefore, college may be an important stage for the primary prevention of obesity. We sought to identify weight gain mediators in college underclassmen using the social cognitive model for health behavior change. Eligible students living on-campus to underwent assessments of height, weight, waist circumfere

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Radhakrishnan, Suresh. "Enhancement of anti-tumour activity by combination of cytotoxic drugs and replication-selective adenoviruses to target prostate cancer." Thesis, Queen Mary, University of London, 2007. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.498525.

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Tetteh, John. "Enhanced target factor analysis and radial basis function neural networks for analytical spectroscopy and quantitative structure activity relationships." Thesis, University of Greenwich, 1997. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.363872.

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Xiao, Qian. "Neuronal class-specific patterns of calcium activity and target dependence of neurotransmitter expression in the developing spinal cord." Diss., [La Jolla] : University of California, San Diego, 2009. http://wwwlib.umi.com/cr/ucsd/fullcit?p3369149.

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Thesis (Ph. D.)--University of California, San Diego, 2009.<br>Title from first page of PDF file (viewed September 15, 2009). Available via ProQuest Digital Dissertations. Vita. Includes bibliographical references.

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