Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 88 for “"Ligand- receptor"”.
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Ligand-receptor interactions of Gonadotropin-releasing hormone antagonists
… GnRH agonists and antagonists with the GnRH receptor were investigated using site directed mutagenesis and photoaffinity cross/inking of the receptor with a labelled GnRH analog. With the aim of identifying residues involved in ligand binding, the relative affinities of five peptide and one …
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Cytokine engineering through ligand/receptor dynamics : a study on granulocyte colony-simulating factor
… chemotherapy. GCSF binds to its specific receptor (GCSFR) on bone marrow precursor cells and generates intracellular signals that cause these cells to proliferate and differentiate into mature neutrophils. However, for such cytokines that act as agonists for cell-surface receptors, these …
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Analysis of trafficking dynamics and cellular response in the interleukin-2 ligand/receptor system
… interaction with one or more forms of the IL-2 receptor (IL- 2R). The overall goal of this thesis is to quantitatively characterize IL-2/IL-2R interactions toward the scientific end of advancing the understanding of the effects of molecular perturbations on cell function, and the technological …
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Exploring the molecular signatures of the ligand-receptor-Gi/o protein interactions of adenosine A1 and A3 receptors
Human adenosine A1 receptor (hA1R) and adenosine A3 receptors (hA3R) are two closely related class A Gi/o-coupled receptors. Both of them represented valuable therapeutic targets and various types of ligands have been developed for regulating their activities. hA1R has important implications in …
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INVESTIGATING PROTEIN - BILAYER COMPLEXES: A STUDY OF LIGAND - RECEPTOR INTERACTIONS AT MODEL MEMBRANE SURFACE BY USING ELECTRONIC ABSORPTION SPECTROSCOPY AND FLUORESCENCE RESONANCE ENERGY TRANSFER.
… chapter 6, we investigate interactions between receptors and ligands at bilayer surface of polydiacetylene (PDA) liposomal nanoparticles using changes in electronic absorption spectroscopy and fluorescence resonance energy transfer (FRET). We study the effect of mode of linkage (covalent versus …
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I. A Structure-Based Approach Toward the Development of a Ligand-Receptor System With Unique Specificity. II. Synthesis and Evaluation of Hexahydrochrysene and Tetrahydrobenzofluorene Derivatives as Selective Estrogen Receptor Modulators
… a large variety of steroidal and non-steroidal ligands, trying to mimick or antagonize estrogenic effects. Partial agonists, with a tissue selective agonist/antagonist profile, termed selective estrogen receptor modulators (SERMs), are better candidates for applications in the treatment of …
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Characterization of heparan sulfate proteoglycan receptor from a permanent rat liver cell line
… a heparan sulfate proteoglycan (HSPG) specific receptor on the cell surface of rat liver cell (RLC), and to characterize the specificity of the ligand-receptor interaction, the properties of the receptor, and the importance of the receptor in HSPG metabolism.
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Ligand-Directed Aavp to Deliver A Therapeutic Transgene to Neuroendocrine Tumors of The Pancreas
… do, however, consistently express somatostatin receptor type 2 (SSTR2) making them vulnerable to somatostatin analogs. Exploiting cell surface receptors overexpressed in tumors is a common avenue for ligand-directed delivery of imaging or therapeutic agents to tumors. In this regard, …
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A general method for studying autocrine signaling and its impact on cancer cell growth
… perturbing agents to inhibit the underlying ligand/receptor interactions. Recent studies reported the ability of drug-resistant cancer cells to acquire mitogenic signals from previously neglected autocrine loops, causing tumor recurrence. Methods that can evaluate autocrine-loop dependency in …
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Cancer Proliferation at the Brain Metastatic Site: A Proteomic Exploration of Inter-Cellular Cross-talk Sustained by Cell-membrane/Secretome Interactions
… secreted and cell membrane proteins, (2) mapping ligand-receptor interactions using an in-house ligand-receptor database, and (3) determining the functional roles of the interacting ligands and receptors. The analysis revealed a complex network of intercellular communications demonstrating how the …
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Understanding ligand binding, selectivity and functions on the G protein-coupled receptors: A molecular modeling approach
… increasing number of available G protein-coupled receptor crystal structures has enabled utilization of a varied number of computational approaches for understanding the ligand-receptor interactions, ligand selectivity and even receptor response upon ligand binding. The following dissertation …
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Investigating Ligand Induced Conformational Changes in the Estrogen Receptor
… calculations from EPR line-shape theory express receptor differences quantitatively as a spectrum of conformational change. Relative squared difference (RSD) analysis allows us to compare ligand receptor complexes to one another. Furthermore, a rigorous statistical analysis shows that these …
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Regulation of natriuretic peptide system activation:effects of spontaneous natriuretic peptide mutations and identification of novel natriuretic peptide receptor phosphorylation sites.
… and GC-B) are transmembrane guanylyl cyclase receptors that mediate the physiologic effects of natriuretic peptides, including reduction of blood pressure and blood volume, stimulation of long bone growth, and regulation of cardiac size. Atrial natriuretic peptide (ANP) and B-type natriuretic …
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Reengineering Estrogen Receptor Hormone Specificity Through Coordinated Changes at Key Contact Sites Between Estrogen Receptor and Estradiol
… from the specific interaction that a hormonal ligand has with its cognate receptor. This interaction is defined by steric and electronic complementarity at certain sites at which portions of the ligand contact specific residues in its receptor. In the nuclear hormone receptors, mutational …
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Dissecting combinatorial microenvironmental regulation of cell fate and function using a multi-modal arraying platform
… cues can include biochemical elements, as in ligand–receptor binding for cell–cell or cell–extracellular matrix (ECM) interactions, or responses to biophysical parameters, as in cell sensing of substrate material properties. One category of engineered system, high-throughput cell microarrays, …
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New Instrumentation and Methods for Analyzing Biological Compounds for Drug Discovery and Discovering Novel Disease Markers
Ligand-receptor interactions mitigate intracellular responses, with abnormal signaling corresponding to different disease states. G-protein coupled receptors currently compose 50% of drug targets, signifying their importance in the pharmaceutical industry. Therefore, monitoring the binding events …
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Light-activated gene expression
… developed. This method uses the Nuclear Hormone Receptor (NHR) family as a model system. This tool provided an opportunity to study the spatial and temporal control of genes by using small synthetic molecules and light. In the late 1990s, we first demonstrated this concept by using as a …
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Effects of cellular and tissue pharmacokinetics on control released growth factors
… CellularPharmacokinetics: The effect of ligand-receptor trafficking was examined on the potency of sustained release versus bolus administration of two growth factors that differed by intracellular trafficking kinetics. Sustained delivery potency was demonstrated to be dependent on both …
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Symmetric signaling by an asymmetric 1 erythropoietin : 2 erythropoietin receptor complex
… molecule binds asymmetrically to two identical receptor monomers via erythropoietin site 1 and site 2, although it is unclear how asymmetry affects receptor activation and signaling. Here we report the computational design and experimental validation of two mutant erythropoietin receptors: one …
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Computational and synthetic approaches in the design and development of chemical probes for estrogen receptor function
A member of the nuclear receptor superfamily, the estrogen receptor (ER) is a ligand-regulated transcription factor responsible for the regulation of hundreds of genes. Consequently, ERs are involved in numerous disease states, including cellular proliferation, post-menopausal symptoms, …
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