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Dissertations / Theses on the topic 'Drug-receptor interaction'

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1

Lähdesmäki, Ilkka Johannes. "Flow injection methods for drug-receptor interaction studies, based on probing cell metabolism /." Thesis, Connect to this title online; UW restricted, 1999. http://hdl.handle.net/1773/8590.

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2

Zheng, Yujuan. "The role of aryl hydrocarbon receptor (AHR) in drug-drug interaction and the expression of AHR in Pichia Pastoris." Scholarly Commons, 2019. https://scholarlycommons.pacific.edu/uop_etds/3580.

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The aryl hydrocarbon receptor is a ligand-activated transcription factor that is involved in many important functions in the body. To study the role and function of AHR, an abundant amount of in vitro expressed and purified protein is needed. A baculovirus insect expression system is commonly employed to express AHR, however, there are several drawbacks with this method, such as mutation potential and high cost. A better in overexpression system is needed and we hypothesize that Pichia pastoris, a yeast expression system, could stably express AHR and ARNT (aryl hydrocarbon receptor nuclear tra
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3

AIROLDI, CRISTINA. "Development of new potential antitumor drugs based on Ras protein inhibition." Doctoral thesis, Università degli Studi di Milano-Bicocca, 2007. http://hdl.handle.net/10281/116562.

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Because of their role in oncogenesis, inhibition of Ras proteins, particularly of their tumorigenic variants, represents today one of the principal strategies finalized to the obtainment of new antitumoral therapies. Among the different possible approaches, one of the most innovative and less explored is represented by the inhibition of this protein activation, key event for the explication of their biological activity, but also for the Ras-induced tumoral cell transformation. Objective of this thesis has been the development of new small molecules able to inhibit, at least partially (total i
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4

Rimondini-Giorgini, Roberto. "Behavioural and biochemical pharmacology of adenosine/dopamine receptor/receptor interaction /." Stockholm, 1999. http://diss.kib.ki.se/1999/91-628-3617-X/.

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5

Mitchell, T. J. "Theoretical investigations into some drug-receptor interactions." Thesis, University of Surrey, 1988. http://epubs.surrey.ac.uk/847811/.

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This study investigates some interactions of agonists with the adrenergic receptor using theoretical and computational chemistry methods. In Chapter 1, the effect of ring fluorination of noradrenaline on the specificity for the a and B receptor is considered. Using a simple receptor model, a conformational difference is found which can explain the experimental observations. In Chapter 2, various theoretical methods are applied to clonidine and a series of similar compounds. The results of these calculations are compared with the differing affinity and activity of these compounds with the adren
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6

Saunders, Martin. "Some theoretical aspects of drug receptor interactions." Thesis, University of Surrey, 1986. http://epubs.surrey.ac.uk/847992/.

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This thesis describes some attempts to model the effect of environment on a molecule, in particular, the effect of solvent and of the receptor site on the properties of a drug molecule. Chapter 1 describes the basic principles of drug activity, the forces responsible for binding of a drug to a receptor, and some of the consequences for drug design. Chapter 2 briefly reviews some of the quantitative structure-activity data available for angiotensin converting enzyme, and describes the design of a postulated active site by drawing an analogy with other zinc peptidases with known crystal structur
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7

Kruger, Karen. "A critical appraisal of intrinsic activity, efficacy and intrinsic efficacy with reference to the development and the current meaning / Karen Krüger." Thesis, North-West University, 2006. http://hdl.handle.net/10394/1088.

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It has been observed that confusion exists in literature concerning the meaning and use of the term efficacy. Confusion is worsened by the use of the term as a general term describing agonist activity. The meaning of the terms intrinsic activity, efficacy and intrinsic efficacy as used in theoretical models of drug action was investigated. The classical occupation model, the two-state model, the ternary complex model (including conformational change and ideas surrounding G-proteins) and the operational model were studied in order to understand the historical and current usage of these terms. A
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8

Shearer, Jacqueline A. "The synthesis and biological evaluation of conformationally restricted analogues of octopamine." Thesis, University of Strathclyde, 1989. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.278492.

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9

Plummer, Christopher John. "Studies of dopamine receptor and monoamine concentrations in the rat central nervous system." Thesis, University of Bristol, 1989. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.232929.

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10

Lewis, Richard Alan. "Molecular recognition and the development of an expert system for the design of novel drug molecules at specified binding sites." Thesis, University of Cambridge, 1987. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.253802.

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11

Lybrand, Terry Paul. "Computer Simulation of ligand-biomacromolecule interactions : theory and application for drug-receptor interactions /." Ann Arbor : Univ. Microfilms Intenational, 1985. http://www.gbv.de/dms/bs/toc/016435745.pdf.

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12

Sachdeva, Karuna. "Regulation of cytochrome P450-3A (CYP3A) and pregnane X receptor (PXR) : implications to drug-drug interactions /." View online ; access limited to URI, 2005. http://0-wwwlib.umi.com.helin.uri.edu/dissertations/dlnow/3186919.

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13

Tso, Cynthia K. W. "A reassessment of the interaction between complement C3d and complement receptor CD21 SCR1-2." Thesis, University of Oxford, 2012. http://ora.ox.ac.uk/objects/uuid:29114281-a320-459d-88a6-9b5fad7c3f7f.

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Biophysical characterisation of protein – ligand interactions can provide vital information to dissect complex biochemical binding mechanisms. C3d has been shown to interact with a number of different protein ligands, namely CD21 SCR1-2, S. aureus Efb-C, S. aureus Ehp, S. aureus Sbi and complement regulatory protein factor H. Although much is known about the relationship of C3d and CD21 in the induction of humoral immunity, the structural aspects of this interaction remained controversial until very recently. The aim of this thesis was to gain a detailed understanding of the C3d/CD21 SCR1-2 in
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14

Leach, Katie. "Pharmacological analysis of the CC chemokine receptors, CCR4 and CCR5 signalling properties and receptor-drug interactions." Thesis, University of Reading, 2005. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.427859.

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15

SHROFF, PURVI B. "AN ASSESSMENT OF THE POTENTIAL INFLUENCE OF BEXAROTENE, A NOVEL RETINOID X RECEPTOR AGONIST, ON THE HEPATIC METABOLISM OF BEXAROTENE." University of Cincinnati / OhioLINK, 2005. http://rave.ohiolink.edu/etdc/view?acc_num=ucin1123813553.

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16

Seeger, Christian. "Revealing Secrets of Synaptic Protein Interactions : A Biosensor based Strategy." Doctoral thesis, Uppsala universitet, Biokemi, 2014. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-220879.

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Protein interactions are the basis of synaptic function, and studying these interactions on a molecular level is crucial for understanding basic brain function, as well as mechanisms underlying neurological disorders. In this thesis, kinetic and mechanistic characterization of synaptic protein interactions was performed by using surface plasmon resonance biosensor technology. Fragment library screening against the reverse transcriptase of HIV was included, as it served as an outlook for future drug discovery against ligand-gated ion channels. The protein-protein interaction studies of postsyna
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17

López, Muñoz Laura. "Homology modeling and structural analysis of the antipsychotic drugs receptorome." Doctoral thesis, Universitat Pompeu Fabra, 2010. http://hdl.handle.net/10803/7228.

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Classically it was assumed that the compounds with therapeutic effect exert their action interacting with a single receptor. Nowadays it is widely recognized that the pharmacological effect of most drugs is more complex and involves a set of receptors, some associated to their positive effects and some others to the side effects and toxicity. Antipsychotic drugs are an example of effective compounds characterized by a complex pharmacological profile binding to several receptors (mainly G protein-coupled-receptors, GPCR). In this work we will present a detailed study of known antipsychotic drug
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18

Sahai, Michelle Asha. "Computational studies of ligand-water mediated interactions in ionotropic glutamate receptors." Thesis, University of Oxford, 2011. http://ora.ox.ac.uk/objects/uuid:b86d2f5a-3554-44c0-b985-5693241369ec.

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Careful treatment of water molecules in ligand-protein interactions is required in many cases if the correct binding pose is to be identified for molecular docking. Water can form complex bridging networks and can play a critical role in dictating the binding mode of ligands. A particularly striking example of this can be found in the ionotropic glutamate receptors (iGluRs), a family of ligand gated ion channels that are responsible for a majority of the fast synaptic neurotransmission in the central nervous system that are thought to be essential in memory and learning. Thus, pharmacological
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19

Jarvius, Malin. "Visualization of Protein Activity Status in situ Using Proximity Ligation Assays." Doctoral thesis, Uppsala universitet, Molekylära verktyg, 2010. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-131934.

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In 2001 the human proteome organization (HUPO) was created with the ambition to identify and characterize all proteins encoded in the human genome according to several criteria; their expression levels in different tissues and under different conditions; the sub-cellular localization; post-translational modifications; interactions, and if possible also the relationship between their structure and function.When the knowledge of different proteins and their potential interactions increases, so does the need for methods able to unravel the nature of molecular processes in cells and organized tiss
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20

Vallon, Gary. "Synthèse d'inhibiteurs de l'interaction entre la protéine à domaine PDZ, PSD-95 et le récepteur de la sérotoninte 5-HT2A pour le traitement des douleurs neuropathiques." Thesis, Clermont-Ferrand 2, 2016. http://www.theses.fr/2016CLF22664.

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Les protéines à domaines PDZ sont impliquées dans des interactions protéine-protéine (IPP) et participent aux transports de signaux impliqués dans de nombreuses pathologies (cancer, mucoviscidose, douleur,…). L’interruption de l’interaction entre la protéine à domaine PDZ, PSD-95, et le récepteur de la sérotonine, 5-HT2A, réduit l’hyperalgie mécanique sur un modèle expérimental de douleur neuropathique chez les rats. Afin de concevoir de nouveaux inhibiteurs de cette interaction, antalgiques potentiels, trois stratégies ont été développées au cours de ces travaux. Une première stratégie a cons
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21

Cashin, Amanda Leigh. "Chemical Scale Investigations of Drug-Receptor Interactions at the Nicotinic Acetylcholine Receptor." Thesis, 2006. https://thesis.library.caltech.edu/839/2/Cashin_Ch1_2006.pdf.

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<p>Biological signaling pathways employ a vast array of integral membrane proteins that process and interpret the chemical, electrical, and mechanical signals that are delivered to cells. Among these proteins, ligand gated ion channels (LGIC) are therapeutic targets for Alzheimer’s disease, Schizophrenia, drug addiction, and learning and memory. High-resolution structural data on neuroreceptors are only just becoming available, yet the functional importance of particular structural features can be challenging.</p> <p>The primary focus of the present work is to gain a chemical scale un
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22

Limapichat, Walrati. "Probing the Roles of Receptor Structure, Drug-Receptor Interactions, and Receptor Crosstalk in Ligand-Gated Ion Channel Function." Thesis, 2013. https://thesis.library.caltech.edu/7255/2/0_Title_1106.pdf.

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<p>Ligand-gated ion channels are multi-subunit transmembrane proteins that play crucial roles in synaptic transmission in the nervous system. These include the Cys-loop receptor superfamily, the ionotropic glutamate receptor (iGluR) family, and the purinergic P2X receptor family. Binding of specific neurotransmitters at the ligand-binding site triggers a series of conformational changes that ultimately leads to ion channel opening. This dissertation describes three molecular-scale functional studies on these receptors.</p> <p>The first project (Chapter 2) describes structure-function st
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23

Nekardová, Michaela. "Výpočetní studie interakcí malých molekul s jejich biologickými cíly." Doctoral thesis, 2020. http://www.nusl.cz/ntk/nusl-411413.

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The thesis specializes in the computational description of pharmaceutically important compounds. A substantial number of pharmaceutical drugs are small molecules that are bound to an active site of an enzyme by the "lock (binding site) and key (drug)" model through non-covalent interactions. The association of enzymes with drugs cause an increase or decrease in the activity of enzymes. The main topic is focused on the computational elucidation of the structural basis for the interactions of the purine-like compounds with the enzyme cyclin- dependent kinase 2 that belongs to the protein-kinase
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