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 405 for “"G-Protein-Coupled"”.
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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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Elucidating the biology of G-protein coupled receptor 35
G-protein coupled receptor 35 (GPR35) is an orphan G-protein coupled receptor which has attracted attention as a coding variant is linked to primary sclerosing cholangitis (PSC) and ulcerative colitis (UC). GPR35 is also upregulated in numerous cancers. Multiple studies of GPR35 have so far fallen …
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Proton-sensing G protein-coupled receptor signalling in inflammation
… receptors including both ion channels and G protein-coupled receptors, many of which are expressed by immune cells and sensory neurones, the principal drivers of inflammation and nociception respectively. While proton-sensitive ion channels, such as the acid-sensing ion channel family have …
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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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Modelling fitness and stability of G protein-coupled receptor variants
G protein-coupled receptors (GPCRs) are the molecular targets of more than a third of approved drugs1 used in a wide variety of diseases2. Protein-altering genetic variants have complex effects on the biophysical and functional properties of GPCRs. Understanding the biophysical and functional …
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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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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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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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Computational and experimental investigation of G protein-coupled receptor signalling mechanisms
G Protein-Coupled Receptors (GPCRs) are 7-transmembrane domain proteins. These receptors translate extracellular stimuli into cellular responses through heterotrimeric G proteins and β-arrestin proteins. These receptors are of considerable therapeutic interest, targeted by over 500 drugs approved …
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Signal Transduction Mechanisms Mediating the Regulation of Vascular G Protein-Coupled Receptors
… 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 governing receptor signaling, desensitization, and re-sensitization. GPCR kinase 2 …
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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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G protein-coupled receptor regulation: The role of protein interactions and receptor trafficking
The superfamily of G protein-coupled receptors (GPCR) is the largest gene family in the human genome. GPCR-mediated signaling operates in every human cell, and about 50% of existing clinically useful drugs act through GPCR. Kinins are proinflammatory peptides that are rapidly produced …
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