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Dissertations / Theses on the topic 'Drug targets'

Author: Grafiati

Published: 4 June 2021

Last updated: 25 July 2025

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1

Kanzi, Aquillah Mumo. "Falcipains as malarial drug targets." Thesis, Rhodes University, 2013. http://hdl.handle.net/10962/d1003842.

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Malaria is an infectious disease caused by parasites of the Plasmodium genus with mortality rates of more than a million annually, hence a major global public health concern. Plasmodium falciparum (P. falciparum) accounts for over 90% of malaria incidence. Increased resistance to antimalarial drugs by the Plasmodium parasite, coupled with the lack of an effective malaria vaccine necessitates the urgent need for new research avenues to develop novel and more potent antimalarial drugs. This study focused on falcipains, a group of P. falciparum cysteine proteases that belong to the clan CA and pa

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2

Diaz, Saez Laura. "Assessment of potential antibacterial drug targets." Thesis, University of Dundee, 2016. https://discovery.dundee.ac.uk/en/studentTheses/4c3fe03b-5ddc-40c9-962c-8c38f811f6ea.

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The alarming increase in antibacterial drug resistance indicates an urgent need to develop new drugs. This project aimed to assess and select potential antibacterial targets and carry out initial biochemical characterisation concentrating on enzymes from biowarfare agents <i>Bacillus anthracis</i>, <i>Burkholderia pseudomallei</i>, <i>Francisella tularensis</i> and <i>Yersinia pestis</i>. The overall objective is to combine genetic and chemical studies to validate, or not, targets for early stage drug discovery. In collaboration with the Dstl (Defence Science and Technology Laboratory), a seri

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3

Uhlemann, Anne-Catrin. "Plasmodium falciparum transporters as antimalarial drug targets." Thesis, St George's, University of London, 2011. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.559278.

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Plasmodiumfalciparum malaria poses one of the most important disease problems in the world. Despite decades of effort to improve disease outcome, the emergence and rapid dissemination of multi-drug resistant parasites has led to a disturbing increase in malaria mortality and morbidity. A critical limitation in managing multi-drug resistant falciparum malaria has been the incomplete understanding of both the underlying molecular mechanisms of drug resistance and the mode of action of widely used drugs. This study aimed to characterise the molecular mechanisms underlying multi- drug resistant ma

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4

Moore, Thomas Oliver. "Synthetic strategies towards challenging PPI drug targets." Thesis, University of Sussex, 2016. http://sro.sussex.ac.uk/id/eprint/64915/.

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Protein-protein interactions (PPIs) present a challenging target for the development of inhibitors, due to the large size and lipophilicity of protein binding sites. Because of this, work that is able to increase our understanding of how PPI inhibitors can be better developed is of great value. In unusual cases, approved drug compounds are able to exhibit excellent pharmacological (PK) profiles despite having unfavourable physical properties. New methodology was developed whereby the solubilising side chains found in one such compound, daclatasvir, could be incorporated onto aryl-bromides usin

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5

Abdel-Ghany, Yasser S. "Osmotic processes as targets for drug design /." The Ohio State University, 1992. http://rave.ohiolink.edu/etdc/view?acc_num=osu1487779439847767.

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6

Mokoena, Fortunate. "Malarial drug targets cysteine proteases as hemoglobinases." Thesis, Rhodes University, 2012. http://hdl.handle.net/10962/d1004065.

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Malaria has consistently been rated as the worst parasitic disease in the world. This disease affects an estimated 5 billion households annually. Malaria has a high mortality rate leading to distorted socio-economic development of the world at large. The major challenge pertaining to malaria is its continuous and rapid spread together with the emergence of drug resistance in Plasmodium species (vector agent of the disease). For this reason, researchers throughout the world are following new leads for possible drug targets and therefore, investigating ways of curbing the spread of the disease.

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7

George, Sarah. "Chemotherapy and Drug Targets in Fasciola hepatica." Thesis, The University of Sydney, 2018. http://hdl.handle.net/2123/20335.

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Controlled multi-age infection studies demonstrated a lack of reliable detection within the first 6 weeks post-treatment using coproantigen (c)ELISA (Bio-X Diagnostics). A second cELISA is recommended for on-farm efficacy testing at 6 weeks in addition to an initial check at 1-2 weeks post-treatment. Field trials confirmed the utility of cELISA as an epidemiological monitoring tool, however results were inconclusive for the recommended field efficacy protocol and further studies are required. Fasciola hepatica burden in controlled studies correlated strongly with cELISA (R2=0.777) at necropsy,

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8

Foulkes, Broderick M. "Developing novel drug delivery methods for anti-leishmanial drugs." Thesis, Griffith University, 2020. http://hdl.handle.net/10072/393974.

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Background: Leishmaniasis is a DNDi listed disease caused by protozoan parasites of the kinetoplastida class. The disease currently spans over 80 countries, across the New World and Old World, potentially affecting 500 million people with 1 million new cases reported annually. Leishmaniasis is a vector-driven disease, utilizing two genus of sand fly, Phlebotomus sand fly is responsible for Old World transmission, whereas the Lutzomyia sand fly is responsible for New World transmission. The two main stages of leishmaniasis, are the diagnostic stage (promastigote in sand fly) and the infective s

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9

Gallagher, Cathal T. "NMR studies of nucleic acids as drug targets." Thesis, University of Nottingham, 2004. http://eprints.nottingham.ac.uk/10082/.

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Nogalamycin is a member of the anthracycline family of antitumour antibiotics. These are potent cytotoxic agents and are routinely used in cancer chemotherapy. Though nogalamycin is clinically insignificant, it does exhibit three distinct types of non-covalent binding to DNA. Since most other anthracyclines bind to DNA by only one or two of these mechanisms, nogalamycin is an excellent model with which to probe the interaction of this class of anti-tumour agents with DNA. Here, we investigate the binding orientation and stoichiometry of nogalamycin in adjacent TpG(CpA) (and CpG(CpG)) intercala

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10

Nichols, Charles E. "Structural studies of potential anti-microbial drug targets." Thesis, Open University, 2004. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.402253.

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11

Roberts, N. J. "Old and new targets in antimalarial drug discovery." Thesis, University of Liverpool, 2016. http://livrepository.liverpool.ac.uk/3007683/.

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The increasing emergence of resistance to commonly used therapies has placed a huge strain on the prevention and control of malaria; therefore, there is an urgent need to develop novel antimalarial agents. The aim of this research was to design and synthesise a library of potent antimalarial compounds, with desirable pharmacokinetic profiles, in order to identify a drug candidate suitable for preclinical development. This research was divided into two main sections: x The synthesis of compounds deigned to inhibit IspD, a novel target in antimalarial drug discovery x The late stage development

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12

Batey, Sibyl. "Drug targets in Mycobacterium tuberculosis α-glucan synthesis". Thesis, University of East Anglia, 2017. https://ueaeprints.uea.ac.uk/67832/.

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α-Glucans are important energy storage polysaccharides in bacteria, plants and animals. In Mycobacterium tuberculosis, α-glucan also functions as a virulence factor that is exported to the mycobacterial capsule and interacts with human immune receptors. In M. tuberculosis and other actinomycetes, α-glucan is synthesised from maltose-1-phosphate by the maltosyl transferase GlgE and the α-1,6-branching enzyme GlgB. These enzymes have been genetically validated as tuberculosis drug targets. The loss of the α-glucan virulence factor is exacerbated by the toxic accumulation of maltose-1-phosphate,

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13

Kumar, Hirdesh. "Identification of vaccine and drug targets against malaria." Thesis, IIT Delhi, 2016. http://localhost:8080/xmlui/handle/12345678/7008.

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14

Lin, Kuan-Hung. "Viral Proteases as Drug Targets and the Mechanisms of Drug Resistance: A Dissertation." eScholarship@UMMS, 2016. https://escholarship.umassmed.edu/gsbs_diss/841.

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Viral proteases have been shown to be effective targets of anti-viral therapies for human immunodeficiency virus (HIV) and hepatitis C virus (HCV). However, under the pressure of therapy including protease inhibitors, the virus evolves to select drug resistance mutations both in the protease and substrates. In my thesis study, I aimed to understand the mechanisms of how this protease−substrate co-evolution contributes to drug resistance. Currently, there are no approved drugs against dengue virus (DENV); I investigated substrate recognition by DENV protease and designed cyclic peptides as inhi

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Lin, Kuan-Hung. "Viral Proteases as Drug Targets and the Mechanisms of Drug Resistance: A Dissertation." eScholarship@UMMS, 2009. http://escholarship.umassmed.edu/gsbs_diss/841.

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Viral proteases have been shown to be effective targets of anti-viral therapies for human immunodeficiency virus (HIV) and hepatitis C virus (HCV). However, under the pressure of therapy including protease inhibitors, the virus evolves to select drug resistance mutations both in the protease and substrates. In my thesis study, I aimed to understand the mechanisms of how this protease−substrate co-evolution contributes to drug resistance. Currently, there are no approved drugs against dengue virus (DENV); I investigated substrate recognition by DENV protease and designed cyclic peptides as inhi

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16

Jones, Nathaniel Gadsby. "Validating protein kinases of Trypanosoma brucei as drug targets." Thesis, University of Glasgow, 2013. http://theses.gla.ac.uk/4007/.

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Trypanosoma brucei spp. are protozoan parasites that cause Human African Sleeping Sickness and Nagana, a disease of cattle. The diseases have a very high mortality rate if untreated and the current drug treatments are inadequate due to toxicity and resistance. In order to develop new treatments, potential drug targets can be investigated in a candidate approach by genetic validation. In trypanosomes this can be performed by using RNA interference (RNAi) technology, which is well developed for this organism. One category of potential targets are protein kinases; members of this enzyme family ha

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17

Drought, L. G. "Investigations into phosphodieterases as targets for antimalarial drug discovery." Thesis, London School of Hygiene and Tropical Medicine (University of London), 2015. http://researchonline.lshtm.ac.uk/2305376/.

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Phosphodiesterases are key enzymes in cyclic-nucleotide signalling pathways, regulating the levels of cAMP and cGMP in the cell. Cyclic nucleotides play an important role in regulating progression of the complex parasite life cycle. There are four Plasmodium PDEs, PDEα-δ. PDEβ has proved refractory to deletion and is predicted to be essential in asexual blood stages. PDEs α, γ and δ have been successfully disrupted in previous studies, which revealed stage-specific roles for PDEγ and PDEδ in the mosquito. PDEβ is a promising drug target due to the proven ability to create specific inhibitors f

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18

Tran, Thanh Nguyen. "Plasmodium Falciparum Histone Deacetylases as Novel Antimalarial Drug Targets." Thesis, Griffith University, 2010. http://hdl.handle.net/10072/367456.

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Histone deacetylases (HDACs) are recognised as potential drug targets for many diseases including cancer, inflammatory diseases and some parasitic diseases including malaria. In eukaryotic cells, these enzymes play an important role in transcriptional regulation through modification of chromatin structure. Inhibitors of mammalian HDAC enzymes including trichostain A and apicidin are active against P. falciparum parasites, however these compounds are not selective for malaria parasites versus normal cell lines. The aims of this study were to examine the antimalarial potential of new hydroxamate

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Punchihewa, Chandanamalie. "DNA and DNA-Interacting Proteins as Anticancer Drug Targets." Diss., The University of Arizona, 2006. http://hdl.handle.net/10150/194379.

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DNA is both the oldest and newest of targets for cancer therapy. While it is already being targeted by many anticancer drugs in the clinic, the development of sequence-specific DNA binders has brought it back to the limelight as a valuable anticancer drug target.My studies on DNA interacting agents was initiated with the DNA intercalator campotothecin, and also included topoisomerase I enzyme. I have evaluated the structure of topoisomerase I C-terminal domain that consists of the active site tyrosine. My data indicate that this domain exists in a molten globule conformation with a fluctuating

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20

Bakheet, Tala M. Burhan. "Properties and Identification of Human and Bacterial Protein Drug Targets." Thesis, University of Manchester, 2009. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.518898.

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21

McKenzie, Neil Iain. "The immunophilins as drug targets : development of novel fluorescence assays." Thesis, University of Edinburgh, 2014. http://hdl.handle.net/1842/17961.

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The immunophilins are a superfamily of proteins comprising the cyclophilins, the FKBPs and the parvulin sub-families. Members are present ubiquitously in plant and animal cells, acting as both prolyl-isomerases and signalling proteins. Some also have chaperone activity. The prolyl isomerase function of the immunophilins has been identified as being central to progression of a large number of diseases, making them tempting drug targets. Whilst there are several assays which can be used to identify inhibitors of the prolyl isomerase function, they are hampered by one or more problems: multistep

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22

Edkins, Adrienne Lesley. "Hsp90 co-chaperones as drug targets in cancer: current perspectives." Springer International Publishing Switzerland, 2016. http://hdl.handle.net/10962/66347.

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publisher version<br>Hsp90 is a molecular chaperone that regulates the function of numerous oncogenic transcription factors and signalling intermediates in the cell. Inhibition of Hsp90 is sufficient to induce the proteosomal degradation of many of these proteins, and as such, the Hsp90 chaperone has been regarded as a promising drug target. The appropriate functioning of the Hsp90 chaperone is dependent on its ATPase activity and interactions with a cohort of non-substrate accessory proteins known as co-chaperones. Co-chaperones associate with Hsp90 at all stages of the chaperone cycle and re

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23

Torretta, Archimede <1993&gt. "E-cadherin and Choline Kinase: two challenging drug discovery targets." Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2022. http://amsdottorato.unibo.it/10030/1/PhD%20Thesis%20of%20Archimede%20Torretta.pdf.

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The data presented in this thesis was generated using molecular biology, protein chemistry and X-ray crystallography techniques. However, while the methodologies employed are essentially the same, the research work presented here refers to two different proteins, which are part of different research projects in the laboratory. For this reason, the content of this thesis is divided in two independent parts, each provided with an introduction and a general overview of the research topic and state-ofthe- art, a materials and methods section discussing the techniques used and the protocols fo

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24

Giommarelli, C. "APPROACHES OF MODULATION OF THERAPEUTIC TARGETS RELEVANT TO DRUG RESISTANCE." Doctoral thesis, Università degli Studi di Milano, 2011. http://hdl.handle.net/2434/150271.

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An emerging anticancer strategy is to identify molecular targets that when inhibited pharmacologically, result in pleiotropic downstream effects on pathways relevant to the malignant phenotype, with particular reference to the development of resistance. In recent years, the molecular chaperone Hsp90 has emerged as leading example of such a target-specific therapy. Heat-shock proteins are found at increased levels in many solid tumors and haematological malignancies. Their expression may account for the ability of malignant cells to maintain protein homeostasis even in the hostile hypoxic micro

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Harris, Michelle J. "Characterization of Drug Resistance in Mycobacterium Tuberculosis via Saturating Mutagenesis of Drug Targets: A Master’s Thesis." eScholarship@UMMS, 2012. https://escholarship.umassmed.edu/gsbs_diss/605.

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Mycobacterium tuberculosis isolates from multiple drug resistant or extensively drug resistant patients show a particular set of mutations in drug targets conferring resistance. However, the selection of drug-resistant strains in vitro yields an alternative set of mutations, thought to result from the cost-benefit associated with drug resistance. Mutations allowing for survival under antibiotic may not be beneficial when presented with the host environment or with a drug-free environment. These fitness effects drive the natural evolution of this bacterium. Using recombineering a large cohor

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Moilanen, A. M. (Anne-Mari). "Identification of novel drug targets for the treatment of heart failure." Doctoral thesis, Oulun yliopisto, 2012. http://urn.fi/urn:isbn:9789514299131.

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Abstract Heart failure (HF) is a complex pathological state, involving simultaneous alterations in several signalling pathways and changes in gene programming. In HF, activation of the neurohumoral factors and renin-angiotensin-aldosterone (RAA) system occurs as a compensatory mechanism to combat the abnormal ventricular function. Developments in cardiac gene delivery methods have exerted a significant impact to treat HF and to discover the novel molecular mechanisms associated with HF and other cardiac diseases. This study demonstrated that adenovirus–mediated gene delivery of B-type natriure

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Mageed, Sarmad Nagemaldeen. "Toxoplasma gondii metabolic enzymes and their evaluation as antiparasitic drug targets." Thesis, University of Leeds, 2013. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.598037.

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Toxoplasma gondii is an ubiquitous obligate intracellular protozoan parasite that causes permanent infections in 10-30% of humans worldwide. It plays a role as an opportunistic parasite in AIDS patients and can cause eye diseases. T. gondii has veterinary importance and has an important role in abortion and mortality in economic animals like sheep, goats and pigs in all parts of the world. It is also a major cause of foetal abortion in human and other mammals and is associated with some behavioural and neurological effects. Two metabolic enzymes; pantothenate synthase producing the precursor t

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Hermawan, Adam. "Molecular evolution assays reveal novel targets and mechanisms of drug resistance." Diss., Ludwig-Maximilians-Universität München, 2015. http://nbn-resolving.de/urn:nbn:de:bvb:19-184920.

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Ogunwobi, Olorunseun Olatunji. "Aetiological factors and potential drug targets in colonic and oesophageal adenocarcinoma." Thesis, University of East Anglia, 2007. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.435983.

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30

Grover, Shipra. "Molecular and biochemical characterisation of mycobacterial cell wall drug targets - Lipoarabinomannan." Thesis, University of Birmingham, 2014. http://etheses.bham.ac.uk//id/eprint/5098/.

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A recent surge in emergence of drug resistant strains of Mycobacterium tuberculosis, the etiological agent of tuberculosis has highlighted the importance of developing new therapeutics and devising novel strategies for effective management of this disease. The cell wall of M. tuberculosis is a major determinant of high level drug resistance demonstrated by this pathogen. Therefore pathways for the synthesis of its components and their regulation have remained an attractive drug target. In this study, the pathway for decaprenyl phosphate recycling emerges as a new target and illustrates a possi

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Taylor, Rebecca Clare. "Mycobacterial fatty acid metabolism : identification of novel drug targets and chemotherapeutics." Thesis, University of Birmingham, 2011. http://etheses.bham.ac.uk//id/eprint/3192/.

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Tuberculosis has been a deadly human pathogen for thousands of years and is as prevalent and lethal now as it was in the pre-antimicrobials era. With new challenges continually being presented in the form of multidrug resistant strains evolving and the implications of the HIV epidemic, it is imperative that every effort is made to understand the causative agent, Mycobacterium tuberculosis, and develop new effective and affordable drugs to treat the disease. With this in mind, the first part of this project tests novel drugs that have been identified using different approaches. The desired targ

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Kanvatirth, Panchali. "Deconvolution of Mycobacterium tuberculosis drug targets using high throughput screening approaches." Thesis, University of Birmingham, 2018. http://etheses.bham.ac.uk//id/eprint/8294/.

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Tuberculosis (TB) is an infectious bacterial disease mainly infecting the pulmonary system of the human body. It affects around 1.5 million people every year, most of whom live in developing countries. The incidence of TB has increased in line with the rise in incidences of Human Immunodeficiency Virus (HIV) infections and Acquired immune deficiency syndrome (AIDS). Due to the pressing concerns of TB, the World Health Organisation (WHO) came up with the Direct Observed Treatment (DOTS) programme. Unfortunately, the development of several resistant strains against first-line drugs and consequen

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Kinkead, James Robert H. "Study of the molecular regulation of trypanosomatid phosphofructokinases as drug targets." Thesis, University of Edinburgh, 2018. http://hdl.handle.net/1842/31144.

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The trypanosomatid parasites T. brucei, T. cruzi and Leishmania spp. are responsible for the ‘neglected diseases’ Human African Trypanosomiasis, Chagas disease and Leishmaniasis respectively. In their human infective form in the bloodstream all three trypanosomatid parasites rely heavily on glycolysis for ATP production. Phosphofructokinase (PFK) catalyses the third step of the glycolytic pathway in all organisms using aerobic respiration. It facilitates the phospho transfer from ATP to fructose 6-phosphate (F6P) to make the products fructose 1,6- bisphosphate (F16BP) and ADP. RNAi knockout of

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MARTINS, Tiago Miguel Lopes. "Identification of proteases as diagnostic and drug targets in bovine babesiosis." Doctoral thesis, Instituto de Higiene e Medicina Tropical, 2009. http://hdl.handle.net/10362/62521.

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A babesiose bovina é uma doença transmitida por carraças, que causa elevada morbidade e mortalidade, e provoca consideráveis perdas económicas devido aos esforços para controlar esta doença. As medidas de controlo da babesiose bovina incluem a erradicação ou redução de carraças, correcto diagnóstico, assim como tratamento e vacinação apropriados. Este trabalho tem como objectivo contribuir para um melhor diagnóstico da infecção e a consequente melhoria de algumas das medidas de controlo, bem como identificar e caracterizar genes de proteases utilizados para o desenvolvimento de um método de di

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Ranjbarian, Farahnaz. "Targets and strategies for drug development against human African sleeping sickness." Doctoral thesis, Umeå universitet, Institutionen för medicinsk kemi och biofysik, 2017. http://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-131074.

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Trypanosoma brucei is a causative agent of African sleeping sickness. It is an extracellular parasite which circulates in the blood, lymph and eventually invades the central nervous system. There is a great need for new medicines against the disease and specific properties of nucleoside kinases in the pathogen can be exploited as targets for chemotherapy. T. brucei contains a gene where two thymidine kinase sequences are fused into a single open reading frame. These types of tandem thymidine kinases were found only in different types of parasites, which made us to believe that it might be ben

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Lovitt, Carrie Jade. "Exploring Breast Cancer Drug Targets in the Third Dimension with Imaging." Thesis, Griffith University, 2014. http://hdl.handle.net/10072/367232.

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This project utilises innovative methodology to evaluate the suitability of novel three-dimensional (3D) cell culture models for investigating anti-cancer drug activity. 3D cell culture methodology was utilised as this in vitro approach is considered to recapitulate the in vivo conditions more accurately than two-dimensional (2D) monolayer cell culture. Two separate 3D cell culture model formats were developed which are amenable to automated liquid handling systems, and a variety of instruments for total well fluorescence and confocal imaging. The first 3D cell culture assay developed was in a

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Gironda, Martínez Adrián. "DNA-ENCODED CHEMICAL LIBRARIES: ADVANCES AND APPLICATIONS TO DRUG DIFFICULT TARGETS." Doctoral thesis, Università di Siena, 2022. http://hdl.handle.net/11365/1194175.

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The discovery of small organic ligands or biologics capable of modulating biological processes remains one of the biggest challenges in developing new medicines. Different technologies have been implemented over the last decades to ease this process and make it more efficient. In this regard, encoded display technologies have played a major role in the discovery of new antibodies, peptides, and proteins. However, the efficient exploitation of automated high-throughput screening to discover small organic ligands has mainly been limited to big pharmaceutical companies. DNA-Encoded Chemical Libra

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Clapham, John Christopher. "Characterisation and structural studies on dog heart cyclic nucleotide phosphodiesterase." Thesis, Birkbeck (University of London), 1997. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.267913.

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Fulton, Joel. "Selective interactions of nuclear receptors and cofactors: novel targets for drug discovery." Thesis, University of Nottingham, 2012. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.602958.

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Nuclear receptors (NRs) are biomedically important transcription factors that regulate gene expression by recruitment of coactivators and corepressors (cofactors) to target gene promoters. Humans express 48 different NRs.and their isoforms, approximately half of which are orphans that have no recognised ligand. NRs can interact with more than 350 known cofactor proteins, many of which are chromatin modifying enzymes. Binding of ligand induces a conformational change in the NR that stimulates or prevents the docking of cofactors. These interactions are mediated by signature motifs (LXXLL in coa

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Rana, Amrita Kaur. "Investigating novel drug targets and the biosynthetic pathways of lipids in mycobacteria." Thesis, University of Birmingham, 2014. http://etheses.bham.ac.uk//id/eprint/4850/.

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The spread of the tuberculosis (TB) has been further accelerated by the emergence of multi- and extensively-drug resistant Mycobacterium tuberculosis strains, thereby further increasing the need to characterise novel drug targets and develop anti-TB agents. The cell wall of M. tuberculosis plays a key role in survival of the pathogen in the host cell, making it an attractive drug target. The findings in this thesis present three different studies that contribute to the discovery of novel drug targets. Using a whole-cell screening approach and the generation of spontaneous drug-resistant mutant

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Rao, Vincenzo A. "Structure of T6SS components and assessment of potential Gram-ve drug targets." Thesis, University of Dundee, 2012. https://discovery.dundee.ac.uk/en/studentTheses/ec37df62-b65a-4f10-ba48-e8edde10e454.

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The structure and potential function of two components of the type VI secretion system in Serratia marcescens have been investigated by X-ray crystallography. Chapters 1 and 2 describe the background of the type VI secretion system and experimental methods respectively. In chapter 3, the solution of the structure of S. marcescens Lip is presented. This is an essential outer membrane lipoprotein that is conserved among bacterial species. It is part of a membrane-spanning sub-assembly that is thought to anchor the remaining components to the cell envelope. The crystal structure of SmLip was dete

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Kumari, Vandana. "Structure-Based Computer Aided Drug Design and Analysis for Different Disease Targets." The Ohio State University, 2011. http://rave.ohiolink.edu/etdc/view?acc_num=osu1311612599.

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Plotkowski, Megan Lynn. "Characterization and modulation of transmembrane domain interactions in membrane protein drug-targets." Diss., Restricted to subscribing institutions, 2008. http://proquest.umi.com/pqdweb?did=1666392021&sid=2&Fmt=2&clientId=1564&RQT=309&VName=PQD.

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Pesce, Eva-Rachele, G. L. Blatch, and Adrienne Lesley Edkins. "Hsp40 Co-chaperones as drug targets: towards the development of specific inhibitors." Springer International Publishing Switzerland, 2016. http://hdl.handle.net/10962/66335.

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publisher version<br>The heat shock protein 40 (Hsp40/DNAJ) family of co-chaperones modulates the activity of the major molecular chaperone heat shock protein 70 (Hsp70) protein group. Hsp40 stimulates the basal ATPase activity of Hsp70 and hence regulates the affinity of Hsp70 for substrate proteins. The number of Hsp40 genes in most organisms is substantially greater than the number of Hsp70 genes. Therefore, different Hsp40 family members may regulate different activities of the same Hsp70. This fact, along with increasing knowledge of the function of Hsp40 in diseases, has led to certain H

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Trezza, Alfonso. "A novel computational way to unlock drug targets deep and transient secretes." Doctoral thesis, Università di Siena, 2019. http://hdl.handle.net/11365/1072788.

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Dutton-Regester, Ken. "The identification of therapeutic targets in metastatic melanoma." Thesis, Queensland University of Technology, 2012. https://eprints.qut.edu.au/53305/1/Ken_Dutton-Regester_Thesis_Final.pdf.

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Metastatic melanoma, a cancer historically refractory to chemotherapeutic strategies, has a poor prognosis and accounts for the majority of skin cancer related mortality. Although the recent approval of two new drugs combating this disease, Ipilimumab and Vemurafenib (PLX4032), has demonstrated for the first time in decades an improvement in overall survival; the clinical efficacy of these drugs has been marred by severe adverse immune reactions and acquired drug resistance in patients, respectively. Thus, understanding the etiology of metastatic melanoma will contribute to the improvement of

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Bolick, Sophia C. E. "Regulation of transcription and analysis of drug targets in lymphoma and myeloma cells." [Tampa, Fla] : University of South Florida, 2006. http://purl.fcla.edu/usf/dc/et/SFE0001750.

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Groome, Nigel Mark. "Invention of novel catalytic cascade reactions and their application to anticancer drug targets." Thesis, University of Leeds, 2011. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.612558.

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The main body of this thesis comprises four chapters: Chapter One serves as an introduction. The first two thirds deals with cell signalling cascades, focusing particularly upon protein kinases and the roles that their dysfunction play in cancerous processes and upon the methods employed to inhibit them in a bid to counter these processes. Kinase inhibition by small molecules is a very active area of research and notable clinical successes have been achieved. The last portion of the chapter addresses some of the issues surrounding .drug discovery, and ends by stating the author's intention to

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Apps, John Richard. "Molecular characterisation of childhood craniopharyngioma and identification and testing of novel drug targets." Thesis, University College London (University of London), 2018. http://discovery.ucl.ac.uk/10044242/.

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BACKGROUND: Adamantinomatous Craniopharyngiomas (ACPs) are clinically challenging sellar region tumours, known to be characterised by mutations in CTNNB1. ACPs are often histologically complex, with different morphological cell types and surrounded by a florid glial reaction. Murine models have been generated through activating β-catenin and support a critical role for nucleo-cytoplasmic accumulating β-catenin cell clusters (‘clusters’) in driving tumorigenesis. AIMS: To phenotype in detail the 3D growth patterns of human and murine ACP; To characterise the genomic and transcriptomic landscape

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Oloko, Olayinka Azeez. "The identification and validation of drug targets for prostate cancer using integrated approaches." Thesis, University of Essex, 2014. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.654477.

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Prostate cancer is a very complex disease, which we still do not fully understand. It is the second most common cause of cancer- related death in men and therefore, it is very important to investigate the mechanisms of prostate tumorigenesis and drug development. Membrane proteins represent a valuable source of potential drug targets due to their intimate involvement in a wide variety of disease states including but not limited to cancer. In our study, we identified five drug targets, namely; EpCAM, TACSTD2, FAM3C, NCEHl and TMEM109 abundantly present in the membrane fraction of prostate cance

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