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 170 for “"GPCRs"”.
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Adhesion-GPCRs in cancer progression and metastasis
Adhesion-GPCRs, a novel family of G protein-coupled receptors (GPCRs), are characterized by an extended extracellular region linked to a seven-pass transmembrane moiety via GPCR proteolytic site (GPS)-containing stalk region known as GAIN domain. The name adhesion refers to the presence of …
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Drug discovery at class A and class B GPCRs
G protein-coupled receptors (GPCRs) are a big family of membrane receptors encoded by more than 800 genes in humans. The vast number and diversity of GPCRs enables them to interact with an equally great number of ligands enabling them to regulate many physiological functions such as senses, …
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Defects in protein trafficking affect expression of GPCRs in C. elegans
In the nematode C. elegans, the bilaterally symmetric PVQ neurons are located in the tail and each extends an axon along the ventral nerve cord to the head. Several G protein coupled receptors (EGL-47, SRA-6) are terminally expressed in PVQ as well as a limited number of other neurons. Mutations in …
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Studies on the optimization of expression and purification & Functional characterization of Class C – GPCRs
G-protein coupled receptor (GPCRs) is a multigene family consisting of more than 1000 genes. They are the most abundant membrane proteins found on a cell surface and are involved in several signaling pathways. In a cell, the signal is transduced by diverse activating endogenous ligands binding on …
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Identification of A Conserved Cluster In The Rh Domain of Grk Critical For Activation By Gpcrs
… critical aspects of G Protein Coupled Receptors (GPCRs) regulation is their rapid and acute desensitization following agonist stimulation. Phosphorylation of these receptors by GPCR kinases (GRK) is a major mechanism of desensitization. Considerable evidence from studies of rhodopsin kinase and …
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Cryo-EM studies of class A GPCRs: the thyroid-stimulating hormone receptor and the β1-adrenoceptor
G protein-coupled receptors (GPCRs) are integral membrane proteins with seven transmembrane domains. They are essential in intercellular communication in human physiology and represent important drug targets in human disease. While methodological advances, particularly in cryogenic electron …
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Chemogenomic approaches to drug design : docking-based virtual screening of nematode GPCRs for potential anthelmintic agents
… G-Protein Coupled Receptor are available. GPCRs play a significant role as targets for therapeutics and are responsible for signal transduction in cells. Thus, nematode GPCRs offer an alternative target to design new anthelmintics. Unfortunately, very little information exists about these …
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Identification of Previously Unknown Interactions Between G Protein-Coupled Receptors and Receptor Activity-Modifying Proteins
<p>G protein-coupled receptors (GPCRs) are known to interact with several other classes of integral membrane proteins. However, the extent of these interactions and their role in regulating GPCR-mediated transmembrane signaling is not well understood. For example, receptor activity-modifying …
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Enhancing the fight against malaria : from genome to structure and activity of a G-protein coupled receptor from the mosquito, Anopheles Gambiae
G-proton coupled receptors (GPCRs) are excellent drug targets that occupy a central position in the physiology of insects and are involved in transmission of signal from the extracellular to the intracellular side of the cell. Adipokinetic hormone receptors (AKHRs) are GPCRs that mediate …
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Investigating G-protein coupled receptors as novel biomarkers for diagnosis, prognosis, and targeted therapy in ovarian cancer
… platform driven by the identification of GPCRs as tumour specific biomarkers. It can be very well imagined that an array of frequently overexpressed GPCRs – matched to ovarian tumour heterogeneity – will in a first step be implemented as a diagnostic tool. In a second step targeted drug …
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Proton-sensing G protein-coupled receptor signalling in inflammation
… proton-sensing G protein-coupled receptors (PS-GPCRs) is less clear. The overarching aim of this work was to further basic pharmacological understanding of the PS-GPCR family and assess their role in inflammatory processes and nociception. The pain associated with chronic inflammation is …
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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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Activation mechanisms of non-class A G protein-coupled receptors
… While the majority of the recent literature on GPCRs focuses on Class A GPCRs, the structural and dynamic insights underlying the activation mechanism of non-Class A GPCRs are lacking. This thesis addresses this gap by investigating activation mechanisms of Class F receptor Smoothened (SMO), six …
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Characterization of Gf a Drosophila trimeric G protein alpha subunit
… of such signals. G-protein coupled receptors (GPCRs) are the largest class of cell surface receptors that respond to an enormous diversity of extracellular stimuli, and are critical mediators of cellular signal transduction in eukaryotic organisms. Signaling through GPCRs has been well …
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Development of Novel Chemical Biology Tools for Probing Structure-Function Relationships in G Protein-Coupled Receptors
<p>G protein-coupled receptors (GPCRs) constitute a large family of transmembrane receptors that transduce extracellular signals into intracellular biochemical responses. Understanding with chemical precision how GPCRs function in cellular membranes is an active area of biological research, but …
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Studies of G Protein-Coupled Receptor Stability and Dimerization Using Novel Fluorescence and Crosslinking Approaches
<p>G protein-coupled receptors (GPCRs) comprise a large family of related seventransmembrane- helical membrane proteins that bind to specific extracellular ligands, such as hormones or neuromodulators. The active receptor-ligand complex then engages with a heterotrimeric G protein on the …
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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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Application of Genetically-Encoded Photoactivatable Crosslinkers to Map Ligand-Binding Sites on G Protein-Coupled Receptors
<p>G protein-coupled receptors (GPCRs) are dynamic membrane proteins that bind extracellular molecules to transduce biological signals. Although GPCRs represent the largest class of targets for therapeutic agents, ligand-binding sites have been precisely defined for only a small percentage of the …
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A mutational analysis of the roles of cytoplasmic domains of the gonadotropin-releasing hormone receptor in coupling and internalization
… of homologous proteins in the human genome. GPCRs are of prime physiological and medical importance as the actions of a wide range of hormones and drugs are mediated by these receptors. The gonadotropin-releasing hormone (GnRH) receptor is a member of the GPCR family, and plays a central role …
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Differential modulation of T-type voltage gated calcium channels by G-protein coupled receptors.
… 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 currents generated by the three …
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