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 214 for “"G protein-coupled receptors"”.
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The methuselah family of g protein coupled receptors
<p>G protein-coupled receptors (GPCRs) are one of the largest class of transmembrane signaling proteins that regulate essential developmental and physiological processes in a cell. GPCR success is illustrated by their abundance across both invertebrate and vertebrate genomes. Phylogenetic analyses …
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Constitutive activity in orphan G protein coupled receptors
… constitutive signaling among orphan class-A G protein coupled receptors (GPCRs). These receptors translate extracellular signals via conformational change into intracellular activation of different G proteins and subsequent second messenger synthesis. These small molecules regulate cellular …
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G-Protein Coupled Receptors Modulating Incretin Hormone Secretion
… with altered enteroendocrine profiles. G-protein coupled receptors (GPCR)s are considered attractive targets to modulate incretin secretion. The aim of this dissertation was to investigate the contributions of GPCRs to incretin secretion. Receptors of interest were identified based on …
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Structure, Function and Dynamics of G-Protein coupled Receptors
Understanding the function of membrane proteins is crucial to elucidate the molecular mechanisms by which transmembrane signaling based physiological processes,i. e., the interactions of extracellular ligands with membrane-bound receptors, are regulated. In this work, synthetic transmembrane …
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Insight into G Protein-Coupled Receptors through Molecular Dynamics Simulations
… significantly to the understanding of protein-drug recognition, providing detailed information on structural flexibility and conformational changes, the supervised molecular dynamics(SuMD) allows to understand the (un)binding paths differences, and metadynamics (MetaD) enhances the …
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Activation mechanisms of non-class A G protein-coupled receptors
G protein-coupled receptors are central to mediating homeostasis across a plethora of biochemical signaling pathways across the entire body and are one of the most important classes of drug targets. While the majority of the recent literature on GPCRs focuses on Class A GPCRs, the structural and …
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Induced Degradation of G-Protein-Coupled Receptors Through Proteolysis Targeting Chimeras
<p>G protein-coupled receptors (GPCRs) are a family of heptahelical transmembrane proteins that can modulate various cellular signaling pathways and therefore are attractive drug targets. Despite high mutational rates of GPCRs in cancer there are few oncology FDA-approved anti-GPCR drugs, leaving a …
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Bioorthogonal Tethering of Drug Fragments to Engineered G Protein-Coupled Receptors
<p>G protein-coupled receptors (GPCRs) modulate diverse cellular signaling pathways and are important drug targets. Despite the availability of high-resolution structures for nearly 100 discrete GPCRs in complex with various ligands, discovering allosteric drugs that can modulate receptor signaling …
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Engineering spores to display g protein-coupled receptors for directed evolution
… of deleterious substances from the outside. G protein-coupled receptors (GPCRs) are the membrane proteins, which transmit signals across the cell membrane. GPCRs are involved in almost every physiological process, and irregular control leads to pathological conditions. Therefore, they are major …
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Signal Transduction Mechanisms Mediating the Regulation of Vascular G Protein-Coupled Receptors
… signaling mechanisms. Among the broad network of receptors and signaling molecules regulating blood vessel reactivity, members of the G protein-coupled receptor (GPCR) family are known to play a central role. GPCR activity represents a delicate, but coordinated balance between molecular mechanisms …
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Novel hypothalamic G protein-coupled receptors involved in the control of reproduction
In the hypothalamus, various G-protein coupled receptors (GPCRs) form part of the regulatory pathways of the hypothalamus-pituitary-gonadal (HPG) axis. The master hormone regulator of the HPG axis is the gonadotropin-releasing hormone (GnRH). Defects in GnRH neuron activity are associated with …
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Towards an accurate alignment of G-protein-coupled receptors from different classes.
G-protein coupled receptors (GPCRs) are a large and diverse family of cell surface receptors involved in signal transduction. They share a general structure of a seven transmembrane domain, an extracellular N-terminus and an intracellular C-terminus domain responsible for coupling to the G-protein. …
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Investigating the molecular pharmacology of class A and B G protein-coupled receptors
G protein-coupled receptors (GPCRs) possess an inherent ability to bind to an extremely diverse range of ligands and activate multiple downstream signalling pathways. It is becomingly increasingly evident, however, that for many GPCRs, the exact downstream signalling cascade(s), and the extent of …
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Differential modulation of T-type voltage gated calcium channels by G-protein coupled receptors.
… to which T-type Ca2+ channels are modulated by G-protein coupled receptors (GPCRs) remains largely unexplored. Investigations into T-type modulation within native neuronal systems have been complicated by the presence of multiple GPCR subtypes and a lack of pharmacological tools to separate …
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Studies of G-Protein Coupled Receptors Incorporated Into a Novel, Nanoscale, Membrane-Mimetic System
<p>From first principles of phospholipid — apolipoprotein A-I (apo A-I) interactions, we hypothesized that the amino acid sequence of apo A-I derived from a different species may exhibit improved properties compared to human apo A-I for the purpose of incorporation of G protein-coupled receptors …
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Advances in structure and small molecule docking predictions for crystallized G-Protein coupled receptors
This dissertation discusses two main aspects of protein-ligand interaction for G-Protein coupled receptors: structure predictions of the flexible loop domains and docking into these receptors. The prediction of loop structure has been long worked on in the context of native, globular proteins. In …
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CGRP family of G protein-coupled receptors and their signalling in human cardiovascular cells
… properties of a unique family of cell surface receptors known as G protein-coupled receptors (GPCRs), and one of their subclasses: The CGRP receptor family. These receptors are crucial for transducing information from the extracellular to intracellular space. While much pharmacological research …
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