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Rozprawy doktorskie na temat „Inhibitor Activity”

Autor: Grafiati

Data publikacji: 6 września 2023

Data aktualizacji: 31 lipca 2025

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1

Stott, Holly Rosannah. "MMP-12 activity during vascular remodelling." Thesis, University of Edinburgh, 2017. http://hdl.handle.net/1842/23609.

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Matrix metalloproteinases (MMPs) are required for tissue remodelling processes, including angiogenesis. MMP activity is generally proangiogenic but MMP-12 is suggested to be antiangiogenic and its precise role is still unclear. The work in this thesis describes the synthesis of an MMP-12 inhibitor and activity probe to address the hypothesis that MMP-12 inhibits angiogenesis. An inhibitor, synthesised in-house, selectively inhibited MMP-12 in in vitro recombinant enzyme assays. An activity probe, also synthesised in-house, was selective for MMP-12 in in vitro recombinant enzyme assays. The fun

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Eckelman, Brendan P. "The regulation of caspase activity by the inhibitor of apoptosis proteins." Diss., Connect to a 24 p. preview or request complete full text in PDF format. Access restricted to UC IP addresses, 2007. http://wwwlib.umi.com/cr/ucsd/fullcit?p3288846.

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Thesis (Ph. D.)--University of California, San Diego, 2007.<br>Title from first page of PDF file (viewed June 2, 2008). Available via ProQuest Digital Dissertations. Vita. Includes bibliographical references (p. 188-214).

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3

Gora, Kasia G. (Kasia Gabriela). "SciP : a novel inhibitor of CtrA transcriptional activity in Caulobacter crescentus." Thesis, Massachusetts Institute of Technology, 2011. http://hdl.handle.net/1721.1/68426.

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Thesis (Ph. D.)--Massachusetts Institute of Technology, Dept. of Biology, September 2011.<br>Cataloged from PDF version of thesis. "August 8, 2011."<br>Includes bibliographical references.<br>Cells must sense changes in their environment and respond appropriately in order to survive. A common survival strategy is for cells to translate an environmental signal into the activity of a transcription factor they effects a change in gene expression. In this way, cells can express a gene just-in-time for its biological function. In addition, cells can coordinate the activity of many transcription fac

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4

Al-Yousuf, Karamallah. "Investigating the anti-melanoma activity of combinatorial paclitaxel and MEK inhibitor." Thesis, University of Dundee, 2018. https://discovery.dundee.ac.uk/en/studentTheses/1be821d2-2436-4c31-8485-e62b86d6d33b.

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Melanoma has increased considerably over the past forty years. Traditional and newly-developed anti-melanoma drugs do not produce a satisfactory therapeutic response for the treatment of late stage melanoma. Nanomedicine is a potent tool for clinicians to circumvent many of the existing shortcomings in cancer therapy. Combination of more than one drug may maximise the therapeutic response and minimise undesirable effects of the chemotherapeutic agents in cancer patients. I developed a novel combinatorial approach that can be loaded into targeted anti-melanoma nanocarriers. Our group have been

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5

Sancho, Elena. "Conformation and activity of plasminogen activator inhibitor type 1 (PAI-1)." Thesis, University of Aberdeen, 1994. http://digitool.abdn.ac.uk/R?func=search-advanced-go&find_code1=WSN&request1=AAIU552562.

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Plasminogen activator inhibitor type 1 (PAI-1) is a unique member of the serpins in that it can adopt various conformations. It is synthesized as an active inhibitor which rapidly converts to a latent form that is not inhibitory. Conformational studies on this protein have been made difficult by this property. The production of recombinant PAI-1 was studied. The expression of r-PAI-1 by the bacterial strain MSD 1005 accounted for some 15-20% of the total cell protein, although some was produced in the form of inclusion bodies. As an attempt to improve the yields of PAI-1 antigen and activity,

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6

Mawlankar, R. "Polyphasic systematics of marine bacteria and their alpha-glucosidase inhibitor activity." Thesis(Ph.D.), CSIR-National Chemical Laboratory, Pune, 2020. http://dspace.ncl.res.in:8080/xmlui/handle/20.500.12252/5847.

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Microbes are the most diverse group of organisms present on the earth. Microbial diversity is the variety and variability of an organism’s and the ecosystem in which they occur. Microbes have been adapted to global environmental changes as and when it happened on the earth.The enormous microbial diversity also gives rise to a largely untapped amount of genetic information, bioactive compounds and biomaterials which could deliver important beneficial traits and applications of societal interest, for example, to improve the medical treatments,fisheries and aquaculture applications, supply of ene

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7

Grundy, Martin. "Activity of the aurora kinase B inhibitor AZD1152 in acute myeloid leukaemia." Thesis, University of Nottingham, 2012. http://eprints.nottingham.ac.uk/12758/.

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Aurora kinases play an essential role in orchestrating chromosome alignment, segregation and cytokinesis during mitotic progression, with both aurora-A and B frequently over-expressed in a variety of human malignancies including those of leukaemic origin. Acute myeloid leukaemia (AML) is a heterogeneous clonal disorder of haematopoietic progenitor cells whose prognosis is particularly poor and where standard induction therapy has changed little over the past thirty years. This thesis evaluated the effects of AZD1152-hQPA (barasertib-hQPA), a highly selective inhibitor of aurora-B kinase, in AM

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8

Sampathkumar, Yamuna. "Thermal processing effects on total phenolic content, antioxidant activity, trypsin inhibitor activity and in-vitro protein digestibility of lentils." Thesis, McGill University, 2012. http://digitool.Library.McGill.CA:80/R/?func=dbin-jump-full&object_id=107918.

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Heat pre-treatment of nutrient-rich lentil seeds prior to their processing into flour may enhance its use by reducing processing and preparation times in value added products. In this study, changes in trypsin inhibitor content, total phenolic content, antioxidant activity, and in-vitro protein digestibility of flours prepared from hulled red lentils and unhulled green lentils were determined subsequent to various processing methods such as oven roasting (OR), boiling and microwave heating (MH). The increasing interest in the phenolic content of plant based food-stuffs made us to assess two d

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9

Ren, Zhongyuan. "Small molecules regulated bone resorption and enzyme activity in osseous cells." Thesis, Lyon 1, 2014. http://www.theses.fr/2014LYO10291/document.

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La Cathepsine K est parmi la plus efficace des collagénases de mammifère pour cliver la triple hélice de collagène de type-1. Nous avons développé une série d'azanitriles, (CKI-8 and CKI-13) inhibiteurs de cathepsine K. CKI-8 (un isomère de CKI-13) et CKI-13 ne sont pas toxiques sur les osteoblastes Saos-2 et les cellules RAW 264.7 jusqu' à une concentration de 1000 nM, tandis qu'ils ne le sont pas jusqu'à une concentration de 100 nM sur les osteoclastes. CKI-8 n'affecte pas l'activité de la phosphatase alkaline ainsi que la minéralisation induite par les Saos-2 et par les osteoblastes primair

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10

Mendis, Mihiri Marini. "Variability in Arabinoxylan, Xylanase Activity and Xylanase Inhibitor Levels in Hard Spring Wheat." Thesis, North Dakota State University, 2012. https://hdl.handle.net/10365/26806.

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Arabinoxylans (AX), xylanase, and xylanase inhibitors have an important role in many cereal food processing applications. The effect of growing location (L), genotype (G), and their interactions (L ×G) on AX, apparent xylanase and apparent xylanase inhibition activities of <italic>Triticum aestivum</italic> xylanase inhibitor (TAXI) and xylanases inhibiting protein (XIP) of wheat was studied using six hard red spring wheat and six hard white spring wheat genotypes. Total AX content was largely dependent on L×G. In bran, xylanase activity, 25% of the variability could be attributed

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11

Zwahlen, Hugo. "Effects of low-dose "Factor VIII Inhibitor Bypassing Activity (FEIBA)" in resistant heamophilia /." [S.l : s.n.], 1986. http://www.ub.unibe.ch/content/bibliotheken_sammlungen/sondersammlungen/dissen_bestellformular/index_ger.html.

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12

Subedi, Yagya P. "Cost-Effective Synthesis, Bioactivity and Cellular Uptake Study of Aminoglycosides with Antimicrobial and Connexin Hemichannel Inhibitory Activity." DigitalCommons@USU, 2019. https://digitalcommons.usu.edu/etd/7699.

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Amphiphilic kanamycin is one of the promising class of compounds for the treatment of fungal infections in plants and animal. Factor that lead to the restricting of compounds for commercialization includes, the higher cost of production and poor stability of the compound. However, the new lead, identified from the synthesis and biological testing, can be synthesized on a large scale with a cost comparable to commercial antifungals. The newly reported lead is stable at the acidic and basic conditions. Additionally, this compound has an excellent activity towards Candida auris, a multidrug-resis

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13

Lau, Rosanna. "cIAP2 Negatively Regulates Proliferation and Tumourigenesis by Repressing IKK Activity and Maintaining p53 Function." Thèse, Université d'Ottawa / University of Ottawa, 2012. http://hdl.handle.net/10393/22845.

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The cellular inhibitor of apoptosis protein (cIAP)-2 plays an important role in the protection against apoptosis by inhibiting the endogenous IAP inhibitor Smac, thus allowing other members of the IAP family, such as XIAP to block caspases. Additionally, cIAP2 functions as a ubiquitin ligase and mediates survival/proliferative signaling through NF-κB. cIAP2 is overexpressed in many human cancers and is believed to play an oncogenic role. This led to the development of small molecule IAP antagonists aimed at eliciting apoptosis in cancer cells. However, the loss of cIAP2 is also associated with

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14

Bosc, Damien. "Synthèse et évaluation biologique d’hétérocycles à cinq chaînons, inhibiteurs de la protéine farnésyltransférase." Thesis, Paris 11, 2011. http://www.theses.fr/2011PA112200/document.

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La protéine farnésyltransférase (FTase) est une métalloenzyme à zinc catalysant le transfert d’une chaîne farnésyle provenant du pyrophosphate de farnésyle (FPP) sur le résidu cystéine de certaines protéines possédant un motif CaaX C-terminal où C est la cystéine farnésylée, a est un acide aminé aliphatique et X est Ser, Ala, Gln ou Met. Une fois additionné, le groupement farnésyle fait office de point d’ancrage rendant possible la fixation des protéines à la membrane cellulaire et de guide moléculaire facilitant la liaison de ces protéines prénylées à d’autres protéines. D’abord étudiée en on

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15

Posarac, Vesna. "Characterization and anti-HIV activity of the proprotein convertase-directed serine protease inhibitor, Spn4A." Thesis, University of British Columbia, 2008. http://hdl.handle.net/2429/3434.

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HIV/AIDS is a global health problem of immense magnitude, with 33 million people living with HIV and 2 million AIDS-related deaths per year. As the development of drug resistance undermines treatment efficacy, the long-term success of anti-retroviral therapy depends upon the introduction of novel drugs aimed at additional targets essential for the viral life cycle. With a critical role in many viral diseases including the proteolytic maturation of the HIV-1 envelope glycoprotein gp160, the secretory pathway proprotein convertases (PCs) represent a potential anti-viral target. Our laboratory ha

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16

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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17

Couto, Jason. "Biologic Activity of the Novel Small Molecule STAT3 Inhibitor Against Canine Osteosarcoma Cell Lines." The Ohio State University, 2013. http://rave.ohiolink.edu/etdc/view?acc_num=osu1373986927.

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18

Hewitt, Laura. "Using a novel small molecule inhibitor to investigate the role of Mps1 kinase activity." Thesis, University of Manchester, 2011. https://www.research.manchester.ac.uk/portal/en/theses/using-a-novel-small-molecule-inhibitor-to-investigate-the-role-of-mps1-kinase-activity(fcacfefc-90d9-4e92-9af4-a57897737329).html.

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During mitosis, accurate chromosome segregation is essential: gain or loss of genetic information can be detrimental to cell viability, or promote tumourigenesis. The mitotic checkpoint (also known as the spindle assembly checkpoint or SAC) ensures accurate chromosome segregation by delaying cell cycle progression until accuracy can be guaranteed. Mps1 is a protein kinase that is crucial for mitotic checkpoint signalling and also for proper chromosome alignment at metaphase. However, the precise role of Mps1’s catalytic activity is still unclear. Here, I present AZ3146, a novel small molecule

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19

Watanabe, Koji. "Pterin-6-aldehyde, an Inhibitor of Xanthine Oxidase, Has Superoxide Anion Radical Scavenging Activity." Kyoto University, 2000. http://hdl.handle.net/2433/151411.

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20

Li, Hao. "Design, Synthesis, and Structure-Activity Relationship Investigation of Selective Sphingosine Kinase Inhibitors." Diss., Virginia Tech, 2019. http://hdl.handle.net/10919/100741.

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Sphingosine kinase 1 (SphK1) is the key enzyme catalyzing the formation of sphingosine-1-phosphate (S1P), which is an important signaling molecule that regulates multiple biological process including inflammatory responses. Elevated SphK1 activity as well as upregulated S1P levels is linked to various diseases such as cancer, fibrosis and sickle cell disease. Therefore, there is a growing interest in studying SphK1 as a potential target for these diseases. Through high-throughput screening, various SphK1 inhibitors have been discovered, among which PF-543 is the most potent and selective inhib

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21

Baker, Amanda F., Neale T. Hanke, Barbara J. Sands, Liliana Carbajal, Janet L. Anderl, and Linda L. Garland. "Carfilzomib demonstrates broad anti-tumor activity in pre-clinical non-small cell and small cell lung cancer models." BioMed Central, 2014. http://hdl.handle.net/10150/610318.

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BACKGROUND: Carfilzomib (CFZ) is a proteasome inhibitor that selectively and irreversibly binds to its target and has been approved in the US for treatment of relapsed and refractory multiple myeloma. Phase 1B studies of CFZ reported signals of clinical activity in solid tumors, including small cell lung cancer (SCLC). The aim of this study was to investigate the activity of CFZ in lung cancer models. METHODS: A diverse panel of human lung cancer cell lines and a SHP77 small cell lung cancer xenograft model were used to investigate the anti-tumor activity of CFZ. RESULTS: CFZ treatment inhibit

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22

Chandrasekar, Balakumaran [Verfasser]. "From glycosidase activity profiling to inhibitor discovery in the plant pathogen Pseudomonas syringae / Balakumaran Chandrasekar." Bonn : Universitäts- und Landesbibliothek Bonn, 2018. http://d-nb.info/1161462309/34.

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23

Yunus, Madiha. "Investigating the Effect of Regorafenib on the Expression and Activity of the Angiogenesis-Modulating Receptor Tyrosine Kinases." Thesis, The University of Sydney, 2022. https://hdl.handle.net/2123/29860.

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The past two decades have been vital for developing cancer treatments. Even though traditional chemotherapy remains the primary choice for most oral treatment regimens, the cancer treatment paradigm is shifting towards more personalised, mechanism-based and selective therapeutic strategies. Tremendous advances have been made in understanding the aberrant signal transduction pathways in cancer, and a myriad of oncogenic drivers have been identified as promising candidates for molecule-targeted therapies. By using small low-molecular-weight compounds, specific alterations in oncogenic molecules

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24

Wang, Haiyao. "Antiplasmin the main plasmin inhibitor in blood plasma : studies on structure-function relationships /." Stockholm : Department of Surgical Sciences, Division of Clincal Chemistry and Blood Coagulation, Karolinska University, 2005. http://diss.kib.ki.se/2005/91-7140-278-0/.

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Fernández, Cecilia A. 1969. "Functional and structural uncoupling of the angiogenic and enzymatic inhibitory activity of TIMPs : loop 6 of TIMP-2 is a novel inhibitor of angiogenesis." Thesis, Massachusetts Institute of Technology, 2004. http://hdl.handle.net/1721.1/31110.

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Thesis (Ph. D. in Applied Biosciences)--Massachusetts Institute of Technology, Biological Engineering Division, 2004.<br>Includes bibliographical references (leaves 119-130).<br>Tissue inhibitors of metalloproteinases (TIMPs) regulate tumor growth, progression and angiogenesis in a variety of experimental cancer models and in human malignancies. However, numerous studies have revealed important differences between TIMP family members in their ability to inhibit angiogenic processes in vitro and angiogenesis in vivo despite their universal ability to inhibit matrix metalloproteinase (MMP) activ

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26

Natarajan, M. "Effects of amylase inhibitor albumin from wheat on the alpha-amylase activity in carp and tilapia." Thesis, University of Stirling, 1988. http://hdl.handle.net/1893/1919.

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The amylolytic activities of alpha-amylase extracted from Mirror carp (Cyprinus carpio) and Nile tilapia (Oreochromis niloticus) were significantly reduced by purified amylase inhibitor albumin of wheat when tested under in vitro conditions. The action of this inhibitor was rapid and maximum levels of inhibition were attained within 20 minutes. For both carp and tilapia, the enzyme residual activities after inhibition were found to be related inversely to inhibitor concentration and positively to the initial enzyme activity levels. The curvilinear relationships between these parameters were ex

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27

Glas, Carina [Verfasser], and Franz [Akademischer Betreuer] Bracher. "Structure-activity relationship analysis of the subtype-selective Sirt5 inhibitor balsalazide / Carina Glas ; Betreuer: Franz Bracher." München : Universitätsbibliothek der Ludwig-Maximilians-Universität, 2021. http://d-nb.info/1228270929/34.

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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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29

Batman, Angela. "MODULATION OF COCAINE-LIKE BEHAVIOURAL ACTIVITY BY SEROTONIN UPTAKE INHIBITION RELATIVE TO THE EFFECTS OF THE NOVEL AND SELECTIVE DOPAMINE TRANSPORTER INHIBITOR, D-84." VCU Scholars Compass, 2010. http://scholarscompass.vcu.edu/etd/2181.

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Cocaine dependence is a major health concern worldwide, but despite this high rate of abuse there are currently no approved therapies for cocaine dependence. Replacement pharmacotherapies are one possible approach for treating cocaine dependence, and identification of such therapeutics for cocaine abuse is the long-term goal of this research. Cocaine binds to, and inhibits uptake at the dopamine (DAT), serotonergic (SERT) and noradrenaline (NET) uptake transporters, but studies have shown that cocaine produces its strong behavioural and positive reinforcing effects through inhibition of the D

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30

Debord, Jean. "Relation structure chimique-activité biologique pour quelques phosphoramides et benzamides." Poitiers, 1988. http://www.theses.fr/1988POIT2331.

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Les constantes d'inhibition reversible de la butylcholinesterase par une serie de 16 phosphoramides aliphatiques ont ete determinees par spectrophotometrie et par microcalorimetrie. L'activite des substituants amines augmente avec la lipophilie. L'inhibition irreversible de la butylcholinesterase par le thio-tepa et le methyl-parathion a ete etudiee en suivant l'hydrolyse d'une faible concentration de substrat en presence de l'inhibiteur

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Ren, Huan. "Biological activity of the 2-phenylaminopyrimidine class receptor tyrosine kinase inhibitor imatinib mesylate (STI571) in malignant glioma." Thesis, University of Liverpool, 2005. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.419008.

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Zyryanova, Alisa. "A molecule-inhibitor of the integrated stress response regulates activity of mammalian eukaryotic translation initiation factor 2B." Thesis, University of Cambridge, 2018. https://www.repository.cam.ac.uk/handle/1810/284208.

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The Integrated Stress Response (ISR) is a conserved eukaryotic translational and transcriptional program implicated in mammalian metabolism, memory and immunity. Although mainly considered to be a protective mechanism, prolonged and severe ISR can result in cell death. The ISR is activated by diverse stress pathways converged on phosphorylation of the alpha subunit of eukaryotic translation initiation factor 2 (eIF2) that inhibits the guanine nucleotide exchange activity of its partner eIF2B and attenuates overall rates of protein synthesis. Numerous mutations in eIF2B are linked to a fatal ne

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33

Harrington, Bonnie K. "Activity of the Second Generation BTK Inhibitor Acalabrutinib in Canine and Human B-cell Non-Hodgkin Lymphoma." The Ohio State University, 2018. http://rave.ohiolink.edu/etdc/view?acc_num=osu1531911818180297.

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Garrido, Christian M. "Avicin is a potent sphingomyelinase inhibitor that blocks K-Ras plasma membrane interaction and its oncogenic activity." Wright State University / OhioLINK, 2018. http://rave.ohiolink.edu/etdc/view?acc_num=wright1545974237243977.

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Khanwalkar, Harshal. "In vitro and in vivo analysis of anti-tumour activity of UVI5008, a novel chromatin enzyme inhibitor." Strasbourg, 2010. http://www.theses.fr/2010STRA6266.

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De plus en plus de données indiquent que le cancer n’est pas uniquement la conséquence d’altérations génétiques, mais résulte également en partie d’altérations épigénétiques. De façon intéressante, cette dérégulation épigénétique est réversible, faisant des enzymes responsables des cibles thérapeutiques potentielles. En effet, les enzymes de modification de la chromatine et en particulier les Histones Déacétylases (HDACs) et les ADN Méthyltransférases (DNMTs), ont récemment émergé comme de nouvelles cibles prometteuses appelées « drogues épigénétiques » pour le traitement des cancers. Le but d

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ARNO', BARBARA. "Investigation of human topoisomerase 1b activity through a domain substitution and interaction with a new synthetic inhibitor." Doctoral thesis, Università degli Studi di Roma "Tor Vergata", 2013. http://hdl.handle.net/2108/210054.

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Il Plasmodium falciparum è l’agente eziologico della malaria umana. La diffusione di ceppi multi- resistenti ai farmaci ha reso necessaria l’identificazione di nuovi bersagli molecolari per la terapia antimalarica. Le DNA topoisomerasi, responsabili della regolazione della topologia del DNA durante fondamentali processi biologici, possono essere considerate possibili candidati. La DNA topoisomerasi 1 (Top1) risolve i superavvolgimenti accumulati dalla doppia elica del DNA catalizzando il processamento di uno dei due filamenti, la rotazione e la risaldatura. La Top1 umana (hTop1) ha una struttu

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Boisson, Julien. "Synthèse de nouveaux iminosucres et évaluation de leur activité inhibitrice de glycosidases." Thesis, Grenoble, 2014. http://www.theses.fr/2014GRENV027/document.

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Le travail présenté dans ce manuscrit concerne la synthèse et une évaluation biologique de 10 nouveaux iminosucres. Les iminosucres sont une classe importante d'inhibiteurs de glycosidases (enzymes catalysant l'hydrolyse d'oligosaccharides), et l'activité inhibitrice de nos produits a été évaluée vis-à-vis d'un panel de 7 glycosidases différentes.Notre laboratoire a récemment décrit la préparation de cétonitrones cycliques polyalcoxylées à partir de cétoses tels que le D-fructose ou le L-sorbose (des sucres naturels abondants). Nous avons imaginé utiliser ces cétonitrones comme intermédiaires

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Kutlesa, Nicole J. "The insecticidal activity of a herbicidal inhibitor of glutamine synthetase tested on larvae of Calpodes ethlius (Lepidoptera: hersperiidae)." Thesis, National Library of Canada = Bibliothèque nationale du Canada, 1999. http://www.collectionscanada.ca/obj/s4/f2/dsk2/ftp01/MQ42166.pdf.

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Henderson, Sally E. "Translating the Anti-Tumor/Anti-Cachectic Activity of AR-42, a Novel HDAC Inhibitor, into Pancreatic Cancer Therapy." The Ohio State University, 2017. http://rave.ohiolink.edu/etdc/view?acc_num=osu1495801301660324.

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Christadore, Lisa M. "Discovery of a small molecule dihydroquinolinone inhibitor with potent antiproliferative and antitumor activity results in catastrophic cell division." Thesis, Boston University, 2013. https://hdl.handle.net/2144/12733.

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Thesis (Ph.D.)--Boston University PLEASE NOTE: Boston University Libraries did not receive an Authorization To Manage form for this thesis or dissertation. It is therefore not openly accessible, though it may be available by request. If you are the author or principal advisor of this work and would like to request open access for it, please contact us at open-help@bu.edu. Thank you.<br>A family of dihydroquinolinones that inhibited the proliferation of a number of cancer cell lines and targeted the oncogenic activities of the late simian virus 40 factor (LSF) was discovered. The lead quinolin

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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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Bou-Rouphaël, Johnny. "A new role for Barhl1 in a cerebellar germinative zone as inhibitor of T-cell factors transcriptional activity." Electronic Thesis or Diss., Sorbonne université, 2023. http://www.theses.fr/2023SORUS009.

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Le cervelet humain contient plus de 50 % des neurones cérébraux. Les neurones granulaires cérébelleux représentent la population neuronale majeure. Les progéniteurs des neurones granulaires (GNP), définis par l’expression de Atoh1, émergent à partir de la lèvre rhombique supérieure (URL), une zone germinative située dans le territoire cérébelleux. Au cours du développement, les GNP prolifèrent, migrent et se différencient. Chacun de ces processus est régulé par un certain nombre de facteurs de transcription et de voies de signalisation. Les « T-Cell Factors » (Tcf/Lef) » sont des effecteurs tr

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Crosby, Brendan. "Exercise as an adjunct therapy in melanoma patients undergoing checkpoint inhibitor therapy." Thesis, Edith Cowan University, Research Online, Perth, Western Australia, 2022. https://ro.ecu.edu.au/theses/2569.

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Extensive research has shown that exercise can improve physical, functional, and psychosocial outcomes during cancer treatment. Despite the prevalence of melanoma, exercise as a therapy in the management of this disease remains understudied and underrepresented in current exercise oncology guidelines. Our systematic literature review identified six studies (882 patients) reporting the effects of physical activity and exercise on objectively-measured and patient-reported outcomes among patients with melanoma. Studies presented heterogeneity of design with two cross-sectional surveys, two retros

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Souza, Pedro Filho Noronha de. "Purification, biochemical characterization and antimicrobial activity of a novel 2s albumin from castor bean(ricinus cmmunis L.) cake displaying trypsin inhibitory activity." Universidade Federal do CearÃ, 2012. http://www.teses.ufc.br/tde_busca/arquivo.php?codArquivo=8867.

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CoordenaÃÃo de AperfeiÃoamento de Pessoal de NÃvel Superior<br>Conselho Nacional de Desenvolvimento CientÃfico e TecnolÃgico<br>FundaÃÃo Cearense de Apoio ao Desenvolvimento Cientifico e TecnolÃgico<br>Castor bean (Ricinus communis L.) is an important crop for the Northeast of Brazil, which recently has been used to produce biodiesel. Around 90% of the castor bean production in Brazil is concentrated at Northeast region and the state of CearÃ is the second largest producer. During the oil extraction process from the castor bean seeds, a resulting residue, called castor cake, is underutilized.

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Byberg, Liisa. "Plasminogen Activator Inhibitor-1 and the Insulin Resistance Syndrome." Doctoral thesis, Uppsala : Acta Universitatis Upsaliensis : Univ.-bibl. [distributör], 2002. http://publications.uu.se/theses/91-554-5307-4/.

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Böhm, Miriam [Verfasser]. "Targeting the Final Step of Blood Coagulation : Structure-Activity-Relationship Studies on the Factor XIIIa Inhibitor Tridegin / Miriam Böhm." Bonn : Universitäts- und Landesbibliothek Bonn, 2015. http://d-nb.info/1077290438/34.

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Shimura, Kazuya. "Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137)." Kyoto University, 2008. http://hdl.handle.net/2433/135828.

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Blanco, Aparicio Carmen. "El Inhibidor de carboxipeptidasa de patata (PCI): un antagonista del EGF con actividad antitumoral." Doctoral thesis, Universitat de Girona, 1998. http://hdl.handle.net/10803/96759.

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In this work we report that potato carboxypeptidase inhibitor suppresses the growth of several human and mouse pancreatic adenocarcinoma cell lines. The inhibitor also reduces the growth of solid tumors obtained by subcutaneous injection of human adenocarcinoma cell line in nude mice and the appearance of metastasis in mice injected intraesplenically with B16H10 melanoma cells. A transgenic line has been characterized, mice develop choroid plexus carcicomas and insulinomas. Lifespan of animals immunized with PCI I s significantly higher than control mice. To further characterize the effects of

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GALBIATI, ANDREA. "DESIGN AND SYNTHESIS OF NOVEL ENZYME INHIBITORS AS ANTIPROLIFERATIVE COMPOUNDS WITH ANTIPROTOZOAL AND ANTICANCER ACTIVITY." Doctoral thesis, Università degli Studi di Milano, 2021. http://hdl.handle.net/2434/827428.

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This dissertation describes the research carried out as part of a PhD program in Chemistry from the 1st October 2017 until 30th November 2020. The PhD project investigated the development of inhibitors of enzymes involved in important metabolic pathways, with the final aim to produce an antiproliferative effect. The present thesis combines the works performed at the University of Milan and Vrije Universiteit of Amsterdam. Part A describes the research performed in Amsterdam, NL during my period abroad from January to September 2019 in the research group of Professor Rob Leurs, at the Di

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Dias, Lucas Pinheiro. "PurificaÃÃo e caracterizaÃÃo de um inibidor de tripsina das flores de Cassia fistula Linn. com atividade antimicrobiana." Universidade Federal do CearÃ, 2012. http://www.teses.ufc.br/tde_busca/arquivo.php?codArquivo=16457.

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CoordenaÃÃo de AperfeiÃoamento de Pessoal de NÃvel Superior<br>As plantas sintetizam proteÃnas que possuem propriedades antimicrobianas, podendo ser utilizadas em substituiÃÃo aos defensivos quÃmicos no campo e como fonte de novas drogas para o controle de infecÃÃes bacterianas em humanos. Dentre as diversas estruturas vegetais, ÃrgÃos reprodutivos como as flores parecem ser uma fonte promissora de tais molÃculas ativas contra patÃgenos, particularmente se considerado o seu relevante papel fisiolÃgico, o qual deve ser preservado. Nesse contexto, a presente pesquisa experimental teve como obje

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