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Rozprawy doktorskie na temat „GPCR”

Autor: Grafiati

Data publikacji: 4 czerwca 2021

Data aktualizacji: 25 lipca 2025

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1

Blankenship, Elise. "Conserved solvent networks in GPCR activation." Case Western Reserve University School of Graduate Studies / OhioLINK, 2016. http://rave.ohiolink.edu/etdc/view?acc_num=case1458221506.

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Poudel, Sagar. "GPCR-Directed Libraries for High Throughput Screening." Thesis, University of Skövde, School of Humanities and Informatics, 2006. http://urn.kb.se/resolve?urn=urn:nbn:se:his:diva-29.

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<p>Guanine nucleotide binding protein (G-protein) coupled receptors (GPCRs), the largest receptor family, is enormously important for the pharmaceutical industry as they are the target of 50-60% of all existing medicines. Discovery of many new GPCR receptors by the “human genome project”, open up new opportunities for developing novel therapeutics. High throughput screening (HTS) of chemical libraries is a well established method for finding new lead compounds in drug discovery. Despite some success this approach has suffered from the near absence of more focused and specific targeted librarie

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3

Majin, Wodu. "Mathematical modelling of GPCR-mediated calcium signalling." Thesis, University of Nottingham, 2012. http://eprints.nottingham.ac.uk/12451/.

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Ca2+ is an important messenger which mediates several physiological functions, including muscle contraction, fertilisation, heart regulation and gene transcription. One major way its cytosolic level is raised is via a G-protein coupled receptor (GPCR)- mediated release from intracellular stores. GPCR’s are the target of approximately 50% of all drugs in clinical use. Hence, understanding the underlying mechanisms of signalling in this pathway could lead to improved therapy in disease conditions associated with abnornmal Ca2+ signalling, and to the identification of new drug targets. To gain su

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Tang, Lisa Sarah. "GPCR expressions in Saccharomyces cerevisiae : engineering transductions." Thesis, University of Leeds, 2005. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.423190.

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Mishra, Satyakam. "Frequent Subgraph Mining Analysis of GPCR Activation." Case Western Reserve University School of Graduate Studies / OhioLINK, 2021. http://rave.ohiolink.edu/etdc/view?acc_num=case1613575702373053.

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6

Kiess, Alexandra. "Funktionelle Relevanz intrazellulärer Splicevarianten des Brain-specific Angiogenesis Inhibitor 2 (BAI2)." Doctoral thesis, Universitätsbibliothek Leipzig, 2014. http://nbn-resolving.de/urn:nbn:de:bsz:15-qucosa-156171.

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BAI2 gehört zu den Adhesion-G-Protein-gekoppelten Rezeptoren (aGPCR). Diese bisher wenig untersuchte Klasse von ca. 30 GPCR ist charakterisiert durch eine komplexe genomische Struktur, sehr große extrazelluläre Domänen und eine Vielzahl von Splicevarianten. Bisher ist bei den meisten aGPCR, wie auch bei BAI2, wenig über ihre Signaltransduktion und Funktion bekannt. Zum Verständnis der physiologischen Relevanz und zur Suche nach dem endogenen Agonist sind Kenntnisse über Proteinstruktur, Splicevarianten und Signaltransduktion essentiell. Ziel dieser Arbeit war es, mittels verschiedener in

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7

Sladek, Barbara. "Structural studies of integral membrane GPCR accessory proteins." Thesis, University of Oxford, 2013. http://ora.ox.ac.uk/objects/uuid:09bf7ada-8e58-49f4-a979-bcd0cec95e8b.

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GPCR accessory proteins regulate the strength, efficiency and specificity of signal transfer upon receptor activation. Due to the inherent difficulties of studying membrane proteins in vitro and in vivo, little is known about the structure and topology of these small accessory proteins. Two examples of GPCR accessory proteins are the Melanocortin-2 receptor accessory protein (MRAP) and the Receptor-activity-modifying protein (RAMP) family. MRAP and RAMP1 are the main focus of this thesis in which they are thoroughly characterised by solution-state NMR and further biophysical techniques. The si

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8

Richardson, Kathryn. "Mechanisms of GPCR signal regulation in fission yeast." Thesis, University of Warwick, 2014. http://wrap.warwick.ac.uk/63554/.

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Cells communicate with each other and respond to environmental cues by sending and receiving signals. Many external signals (ligands) are detected through G protein-coupled receptors (GPCRs), a major class of transmembrane proteins. GPCRs transduce these external signals into appropriate intracellular responses, enabling the cell to adapt to its environment. Malfunctions in these signalling pathways can lead to a range of human diseases and hence GPCRs have become attractive candidates for pharmacological design. The activation of a single receptor has the ability to induce numerous intracellu

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9

Goddard, Alan David. "Functional analysis of GPCR signalling cascades in Schizosaccharomyces pombe." Thesis, University of Warwick, 2006. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.437696.

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10

Koyama, Hiroyuki. "Comprehensive Profiling of GPCR Expression in Ghrelin-producing Cells." Kyoto University, 2016. http://hdl.handle.net/2433/215953.

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11

Engemaier, Eva. "Die strukturelle und funktionelle Evolution des G-Protein-gekoppelten Rezeptors GPR34." Doctoral thesis, Universitätsbibliothek Leipzig, 2012. http://nbn-resolving.de/urn:nbn:de:bsz:15-qucosa-86270.

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Gegenstand der Arbeit ist eine umfassende Charakterisierung von Struktur und Funktion des G-Protein-gekoppelten Rezeptors GPR34 auf genomischer, mRNA und Proteinebene, die mögliche Rückschlüsse auf physiologische Funktionen oder den natürlichen Agonisten zulassen. Dazu wurde die genomische Organisation des GPR34 in Mensch, Maus und Ratte analysiert und festgestellt, dass neben der intronlosen kodierenden Sequenz auch der 5´-Bereich des GPR34 mit seiner nicht-kodierenden Intron-Exon-Struktur stark konserviert ist. Es wurden in der Ratte und der Maus mindestens zwei, beim Menschen ein putativer

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12

Thamm, Markus. "Charakterisierung der Serotonin-Rezeptoren der Honigbiene Apis mellifera : von den Genen zum Verhalten." Phd thesis, Universität Potsdam, 2009. http://opus.kobv.de/ubp/volltexte/2010/4073/.

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Das serotonerge System besitzt sowohl bei Invertebraten als auch bei Vertebraten eine große Bedeutung für die Kontrolle und Modulation vieler physiologischer Prozesse und Verhaltensleistungen. Bei der Honigbiene Apis mellifera spielt Serotonin (5-Hydroxytryptamin, 5-HT) eine wichtige Rolle bei der Arbeitsteilung und dem Lernen. Die 5-HT-Rezeptoren, die überwiegend zur Familie der G-Protein gekoppelten Rezeptoren (GPCRs) gehören, besitzen eine Schlüsselstellung für das Verständnis der molekularen Mechanismen der serotonergen Signalweiterleitung. Ziel dieser Arbeit war es, 5-HT-Rezeptoren der Ho

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13

Zhang, Boyang. "Functional and Structural Insights into the First and Second Intracellular Domains for D1-Class Dopaminergic Receptors." Thesis, Université d'Ottawa / University of Ottawa, 2017. http://hdl.handle.net/10393/35932.

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Previous studies have shown that the subtype-specific pharmacological properties of D1-class receptors (D1R and D5R) can be attributed to their third intracellular domain and C-terminal tail. However, the importance of their first and second intracellular domains (IC1 and IC2) has yet to be explored. Using mutagenesis and bioinformatics, we examine the functional and structural roles of Ser/Thr spanning IC1 and IC2—most of which are conserved not only among D1-class receptors but also among other GPCRs. Mutant receptors of human D1-class receptors (hD1R and hD5R) were constructed whereby all S

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14

Guerrero, Hernández Martina. "Targeting tumor microenvironment crosstalk through GPCR receptors and PI3K pathway." Doctoral thesis, Universitat de Barcelona, 2019. http://hdl.handle.net/10803/667975.

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The tumor microenvironment (TME) is gaining momentum due to its contribution to cancer progression and therapy resistance. This TME has a direct crosstalk with tumor cells that involves the activation of different pathways. Follicular lymphoma (FL) is the most common indolent non-Hodgkin lymphoma. Although FL is generally characterized by slow progression and high response rates to therapy, it is still considered incurable, because almost virtually all the patients relapse. FL is probably the NHL with the highest dependence on microenvironment. PI3K is a common denominator transducing the sig

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15

Gardner, Jacob Andrew. "GPCR Signaling in the Genesis and Progression of Pancreatic Cancer." Diss., Temple University Libraries, 2009. http://cdm16002.contentdm.oclc.org/cdm/ref/collection/p245801coll10/id/35453.

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Molecular Biology and Genetics<br>Ph.D.<br>Ductal adenocarcinomas of the pancreas are the 4th most common cause of cancer death. The 1 and 5 year survival rates for all stages combined are currently 26% and 5% respectively. Median survival is less than 6 months. Despite remarkable progress in the fields of genetics, cancer biology, and advances in surgical techniques as well as chemotherapeutics, our ability to recognize and treat patients with pancreatic cancer remains poor. GPCR signaling modules have been increasingly implicated in the genesis and progression of pancreatic cancers. Aberran

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16

Senarath, Kanishka D. "Interrogation of GPCR-G Protein Signaling using Novel Optogenetic Tools." University of Toledo / OhioLINK, 2019. http://rave.ohiolink.edu/etdc/view?acc_num=toledo155681039815937.

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17

Jha, Ankita. "Quantitative control of GPCR organization and signaling by endocytosis in epithelial morphogenesis." Thesis, Aix-Marseille, 2017. http://www.theses.fr/2017AIXM0393/document.

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Au cours de la gastrulation de l’embryon de Drosophile, l’activation apicale du cytosquelette d’acto-myosine orchestre la constriction apicale dans le mésoderme en invagination ainsi que l’intercalation cellulaire dans l’ectoderme en extension. Un contrôle quantitatif de l’activité des GPCRs et, par conséquent, de l’activation de Rho1 est à l’origine des différences de déformation des cellules du mésoderme et de l’ectoderme mais ces mécanismes demeurent incompris. L’activité du GPCR Smog se concentre respectivement en deux compartiments distincts à la surface de la membrane plasmique (PM) et d

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18

Cutolo, Pasquale. "Etude de l'interaction structurelle et fonctionnelle entre la chimiokine CXCL12 et ses récepteurs : CXCR4 et ACKR3/CXCR7." Thesis, Université Paris-Saclay (ComUE), 2016. http://www.theses.fr/2016SACLS550/document.

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L'axe formé par la chimiokine CXCL12 et son récepteur CXCR4 est conservé chez les vertébrés où il joue un rôle important dans l'embryogenèse et la vie adulte, régule de nombreux processus des réponses immunitaires grâce à ses fonctions dans la migration cellulaire, la survie et la prolifération.En outre, cet axe est impliqué dans les processus pathologiques tels que les cancers (croissance et métastase) et immunodéficiences ainsi que des dysfonctionnements (par exemple l'expression dérégulée, polymorphismes ou mutations) et est également détourné par certains agents pathogènes (par exemple le

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19

Adamson, Roslin Jane. "Probing GPCR-Gα interactions : a functional study by EM and SPR". Thesis, University of Oxford, 2014. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.669745.

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20

Mason, Vicki Louise. "Effects of different assay configurations on pharmacological profiling of GPCR targets." Thesis, University of Reading, 2007. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.494820.

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The effect of assay type and assay configuration on the pharmacological profile of a range of ligands acting at the D2 dopamine receptor was investigated in this thesis. The ligands explored have previously been shown to display a spectrum of efficacy at the D2 dopamine receptor. In competition ligand binding studies versus [³H]spiperone in HEK-293CREβlacD₂ˡ cell membranes, receptor-G protein coupling was increased in the absence of Na⁺, however the pK/ values for some agonists were higher in the presence of Na⁺, which suggested that different ligands are able to induce different receptor conf

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21

Santos, Geisa Aparecida dos. "Análise comparativa de perfis de sinalização do receptor AT1 ativado por agonistas seletivos para a via de -arrestinas." Universidade de São Paulo, 2013. http://www.teses.usp.br/teses/disponiveis/17/17131/tde-31102013-150124/.

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Os receptores acoplados à proteína G (GPCRs), também chamados de receptores 7TM, são conhecidos por regular virtualmente todos os processos fisiológicos em mamíferos e cerca de 40% de todas as drogas comerciais agem através destes receptores. A sinalização mediada por eles é classicamente atribuída à proteína G, que é ativada pela troca de GDP por GTP, promovendo a separação das subunidades G e G, e leva à produção de mensageiros secundários como cAMP, Ca2+ e DAG. Após a resposta os GPCRs são fosforilados pelas quinases de GPCRs (GRKs), sinalizando para recrutamento das -arrestinas citoplasmát

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22

Jaén, Cristina. "Differential coupling of RGS3s and RGS4 to GPCR-GIRK channel signaling complexes." [Tampa, Fla] : University of South Florida, 2006. http://purl.fcla.edu/usf/dc/et/SFE0001533.

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23

Altosaar, Katrin. "Dimer-dependent allosteric modulation within GPCR signalling complexes can influence signalling diversity." Thesis, McGill University, 2013. http://digitool.Library.McGill.CA:80/R/?func=dbin-jump-full&object_id=114353.

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G protein-coupled receptors (GPCRs) comprise the largest group of cell surface receptors, translating environmental signals into cellular responses via cognate G protein partners. Contrary to our initial understanding, most GPCRs do not function in living cells as monomers, but most likely dimers, or even larger arrays of receptors. Standard drug design approaches rely on the notion that drugs binding the two receptors in a given dimer likely function independently of one another. However, this view has been challenged by recent work showing that ligand binding at both receptors can modulate d

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24

Hall, Caroline Jane. "The effect of GPCR crosstalk on intracellular Ca2+ responses and downstream signalling." Thesis, University of Leicester, 2011. http://hdl.handle.net/2381/9528.

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Jaén, Cristina. "Differential coupling of RGS3s and RGS4 to GPCR-GIRK channel signaling complexes." Scholar Commons, 2006. http://scholarcommons.usf.edu/etd/2571.

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'Regulators of G protein signaling' (RGS proteins) modulate the G proteincycle by enhancing the GTPase activity of Ga subunits. These changesaccelerate the kinetics of ion channel modulation by Gai/o-coupled receptors(GPCRs) such as the G protein-gated inward rectifier K+ (GIRK/Kir3) channel. Myexperiments indicate that a single cerebellar granule (CG) neuron, a cell type thatendogenously expresses GIRK channels is able to express a wide variety ofRGS proteins. I selected two of them, which are widely expressed andtranscriptionally regulated during pathophysiologic conditions, to compare their

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Ranganathan, Anirudh. "The impact of GPCR structures on understanding receptor function and ligand binding." Doctoral thesis, Stockholms universitet, Institutionen för biokemi och biofysik, 2016. http://urn.kb.se/resolve?urn=urn:nbn:se:su:diva-129879.

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G protein-coupled receptors (GPCRs) form the largest superfamily of eukaryotic membrane proteins and are responsible for the action of nearly 30% of all marketed drugs. For a long period, efforts to study these receptors were limited by the paucity of atomic-resolution structural information. Numerous receptors spread across the GPCR superfamily have recently been crystallized, revealing crucial clues about receptor function and ligand recognition. The work in this thesis has primarily focused on using computational techniques to capitalize on this increasing amount of structural information.

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Bahena, Silvia. "Computational Methods for the structural and dynamical understanding of GPCR-RAMP interactions." Thesis, Uppsala universitet, Institutionen för biologisk grundutbildning, 2020. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-416790.

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Protein-protein interaction dominates all major biology processes in living cells. Recent studies suggestthat the surface expression and activity of G protein-coupled receptors (GPCRs), which are the largestfamily of receptors in human cells, can be modulated by receptor activity–modifying proteins (RAMPs). Computational tools are essential to complement experimental approaches for the understanding ofmolecular activity of living cells and molecular dynamics simulations are well suited to providemolecular details of proteins function and structure. The classical atom-level molecular modeling o

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28

Scarlin, Hugh. "Studies on the synthesis of novel PP2A inhibitors and a GPCR detergent." Thesis, University of Glasgow, 2016. http://theses.gla.ac.uk/7370/.

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Chapter 1 While targeting kinases in oncology research has been explored extensively, targeting protein phosphatases is currently in its infancy. However, a number of pharmaceutical companies are currently looking to expand their research efforts in this area. PP2A has been shown to down-regulate ERK5, a mitogen-activated protein kinase (MAPK) that has been shown to be important in driving the invasive phenotype of prostate cancer. Fostriecin and its related structural analogues PD 113,270 and 113,271 have been shown to inhibit a mitotic entry checkpoint in cell growth through the potent and s

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29

Elenko, Eric. "Localization and fate of GAIP following G[alpha]i̳ linked GPCR stimulation /." Diss., Connect to a 24 p. preview or request complete full text in PDF format. Access restricted to UC campuses, 2001. http://wwwlib.umi.com/cr/ucsd/fullcit?p3026385.

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Heuninck, Joyce. "Analysis of CXCR4 and ACKR3 oligomerisation." Thesis, Montpellier, 2019. http://www.theses.fr/2019MONTT018.

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Mon travail de thèse s’est focalisé sur l’étude des récepteurs CXCR4 et ACKR3, deux récepteurs aux chimiokines. Ceux-ci jouent des rôles majeurs dans différentes fonctions physiologiques notamment le chimiotactisme des cellules immunitaires. Le dérèglement de leur activité est souvent associé à différents pathologies, notamment des cancers. Outre le fait que ces récepteurs lient tous les deux la même chimiokine, CXCL12, il a été montré qu’ils étaient capables d’exercer l’un sur l’autre des régulations croisées. Les mécanismes sous-tendant celles-ci sont très mal connus. Ils pourraient être lié

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Brewer, Cynthia. "Use of PC12 cells to characterize PAFR-GPCR-mediated activity in neural precursors." Thesis, University of Ottawa (Canada), 2001. http://hdl.handle.net/10393/9170.

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Platelet activating factor (PAF: 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine) is a biologically active phospholipid mediator produced by neurons and glial cells. In adult central nervous system (CNS), physiological concentrations of PAF have been shown to mediate long-term potentiation, the purported cellular basis of mammalian learning and memory. Elevated levels of PAF are implicated in the pathophysiology of a number of neurodegenerative diseases, ischemia-reperfusion injury, human immunodeficiency virus-1 (HIV-1) associated dementia, and the developmental brain disorder Miller-Dieker Sy

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Jackson, Verity. "Mechanistic studies of the adhesion-GPCR latrophilin and its interactions in neural guidance." Thesis, University of Oxford, 2017. http://ora.ox.ac.uk/objects/uuid:ecc6187a-3e20-4753-ada6-dc009ad7f6e2.

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The adhesion GPCRs are a poorly understood and evolutionarily ancient family of cell surface receptors, several of which have emerging functions in the development of the nervous system. aGPCRs comprise a large extracellular domain, providing binding sites for a variety of ligands, alongside a seven transmembrane domain characteristic of GPCRs. It has been proposed that aGPCRs may function as "context-recognisers", using their large ectodomains to bind different combinations of ligands depending on the molecular make-up of the environment. However there is a lack of direct evidence for this at

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Bucco, Olgatina, and olgatina@gmail com. "Preparing, measuring and capturing G-protein coupled receptor (GPCR) signalling complexes for future development of cell-free assay technologies." Flinders University. medicine, 2006. http://catalogue.flinders.edu.au./local/adt/public/adt-SFU20060703.114912.

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G-protein coupled receptors (GPCRs) are integral membrane proteins which represent primary cellular targets for intracellular signalling. Many of these receptors are altered in disease states and hence are the target for over 50% of marketed drugs. Despite their physiological importance, high-throughput, cell-free assays which measure functional or signalling activity are only recently being investigated. The current approach by the pharmaceutical industry to initially screen compounds for functionality is to use heterologous cell-based assay formats. The aim of this work was to reconstitute a

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Peyrassol, Xavier. "Développement et caractérisation d’anticorps de camélidés dirigés contre des récepteurs couplés aux protéines G et leur utilisation dans des approches structurales." Doctoral thesis, Universite Libre de Bruxelles, 2018. http://hdl.handle.net/2013/ULB-DIPOT:oai:dipot.ulb.ac.be:2013/270870.

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Les camélidés possèdent une caractéristique immunologique particulière parmi les mammifères. En plus des anticorps conventionnels tétramériques composés de 2 chaînes lourdes et de 2 chaînes légères, on retrouve dans des proportions variant de 25 à 50% des anticorps dépourvus de chaînes légères. Le paratope de ces anticorps est dès lors constitué de la partie variable monomérique des chaînes lourdes. Ce domaine d’environ 15 kDa représente le plus petit fragment capable de lier un antigène et est communément appelé nanobody de par sa petite taille. Les nanobodies possèdent des propriétés uniques

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do, Nascimento Júnior Francisco. "Classificação de Proteínas usando Máquinas de Aprendizagem e Descoberta de Padrões." Universidade Federal de Pernambuco, 2008. https://repositorio.ufpe.br/handle/123456789/1596.

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Made available in DSpace on 2014-06-12T15:51:20Z (GMT). No. of bitstreams: 1 license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) Previous issue date: 2008<br>Máquinas de aprendizagem têm sido aplicadas em diferentes problemas em Bioinformática. Similarmente, algoritmos de descoberta de padrões também têm sido usados para descobrir motifs em seqüências de proteínas, contribuindo na definição de assinaturas (tais como impressões digitais) que caracterizam classes funcionais de proteínas. Como por exemplo, a classe de receptores acoplados a proteína-G (GPCR) que repres

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Garcia, De Las Bayonas Alain. "Spatio-temporal and quantitative control of Rho1 activity by GPCR signaling during tissue morphogenesis." Thesis, Aix-Marseille, 2018. http://www.theses.fr/2018AIXM0548/document.

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La constriction apicale des cellules du mésoderme et l'intercalation des cellules de l'ectoderme sont contrôlées par des réseaux contractiles d'acto-myosine dans l'embryon de Drosophile. Le niveau d'activation et la polarisation du cytosquelette d'acto-myosine détermine la nature des déformations cellulaires observées. Nous montrons que le GPCR Smog et les protéines G (Gα,Gβγ) en aval, activent la signalisation Rho1 et donc la Myosine-II dans les deux tissus. Dans l'ectoderme, Gα12/13 active Rho1 à la membrane apicale (aussi appelé compartiment médio-apical) tandis que les sous-unités Gβ13F-Gγ

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Sheng, Yinglun. "G protein signaling and G protein coupled receptor (GPCR) pathway in Xenopus oocyte maturation." Thesis, University of Ottawa (Canada), 2005. http://hdl.handle.net/10393/29262.

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Xenopus laevis oocytes are physiologically arrested at the first meiotic prophase. Progesterone reinitiates meiosis (maturation) through inhibition of an oocyte adenylyl cyclase (AC) and reduction of intracellular cAMP. However, the mechanism by which progesterone regulates AC activity and cAMP level still remains unclear. In this thesis, I summarize work I conducted that collectively helps elucidate how high levels of cAMP might be achieved in G2 arrested oocytes. In Chapter 2, I describe our finding that inhibiting endogenous G-protein betagamma subunits, through the use of two structurally

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Liebscher, Ines. "Die Physiologische Relevanz des G-Protein-gekoppelten Rezeptors GPR34." Doctoral thesis, Universitätsbibliothek Leipzig, 2011. http://nbn-resolving.de/urn:nbn:de:bsz:15-qucosa-64305.

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Die Familie der G-Protein-gekoppelten Rezeptoren (GPCRs) bildet die größte Gruppe von Membranrezeptoren im menschlichen Organismus. Für viele GPCRs sind bisher die physiologischen Funktionen nicht bekannt. Das biologische Verständnis der Funktionen im menschlichen Organismus dieser sogenannten „orphan“ GPCRs (oGPCRs) hat, aufgrund möglicher kausaler Beteiligung an der Pathogenese von Erkrankungen sowie deren therapeutische Beeinflussbarkeit, hohe medizinische Relevanz. Die GPCRs der P2Y12-ähnliche Rezeptorgruppe besitzen eine große physiologische Bedeutung bei der Thrombozytenaggregation und

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Akkuzu, Selin. "The Functional Assessment Of Fluorecently Tagged Adenosine A2a And Dopamine D2 Receptors And Qualitative Analysis Of Dimerization Of Adenosine A2a And Dopamine D2 Receptor By Using Fret." Master's thesis, METU, 2013. http://etd.lib.metu.edu.tr/upload/12615474/index.pdf.

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Recently, several studies have demonstrated that G protein coupled receptors exist as homo/heterodimers or oligomers. Adenosine A2A receptors and dopamine D2 receptors are present as both homo- and heterodimer. In the GABAergic striatopallidal neurons A2AR are co- localized with D2 receptors (D2R), and establish functional A2AR-D2R heteromers, which modulates dopaminergic activity. Due to be involved in physiological processes, these receptors bear critical roles. Dopamine receptors play critical role in dopaminergic pathways in regulation of memory, food intake and psychomotor activity, etc.

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Ellaithy, Amr. "Metabotropic Glutamate Receptor 2 Activation: Computational Predictions and Experimental Validation." VCU Scholars Compass, 2018. https://scholarscompass.vcu.edu/etd/5319.

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G protein-coupled receptors (GPCRs) are the largest family of signaling proteins in animals and represent the largest family of druggable targets in the human genome. Therefore, it is of no surprise that the molecular mechanisms of GPCR activation and signal transduction have attracted close attention for the past few decades. Several stabilizing interactions within the GPCR transmembrane (TM) domain helices regulate receptor activation. An example is a salt bridge between 2 highly conserved amino acids at the bottom of TM3 and TM6 that has been characterized for a large number of GPCRs. Throu

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MOLTENI, LAURA. "PHARMACOLOGICAL CHARACTERIZATION OF THE INTRACELLULAR SIGNALLING PATHWAY ACTIVATED BY TLQP-21." Doctoral thesis, Università degli Studi di Milano-Bicocca, 2017. http://hdl.handle.net/10281/158161.

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L’obesità è una condizione patologica per la quale non è stato ancora possibile identificare un trattamento farmacologico efficace. Il controllo dell’appetito è regolato da diversi fattori, la cui integrazione da parte dell’ipotalamo risulta nella generazione di specifiche risposte che regolano il bilancio energetico. TLQP-21 è un neuro-peptide coinvolto nella regolazione di diverse funzioni fisiologiche, incluso metabolismo, diabete, dolore e funzioni gastriche. Nonostante la recente identificazione di due potenziali recettori per TLQP-21, ad oggi, il meccanismo d’azione con cui agisce quest

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Holmes, Steven P. "The characterization, functional expression, and localization of the first arthropod myokinin receptor from the southern cattle tick, Boophilus microplus (Acari: ixodidae)." Diss., Texas A&M University, 2003. http://hdl.handle.net/1969.1/60.

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Myokinins are invertebrate neuropeptides with myotropic and diuretic activity. The lymnokinin receptor from the snail Lymnaea stagnalis was the only previously identified myokinin receptor. A cDNA encoding a neuropeptide receptor was cloned from the southern cattle tick, Boophilus microplus. The deduced amino acid sequence was 40 % identical to the lymnokinin receptor. The receptor transcript is present in all tick life stages as determined by semiquantitative RT-PCR. When expressed in mammalian CHO-K1 cells, myokinins at nanomolar concentrations induced increases in intracellular calcium a

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Sohn, Johann. "IDENTIFICATION AND CHARACTERIZATION OF CONTACT SITES BETWEEN HUMAN FOLLICLE STIMULATING HORMONE AND THE FOLLICLE STIMULATING HORMONE RECEPTOR." UKnowledge, 2005. http://uknowledge.uky.edu/gradschool_diss/270.

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Follicle stimulating hormone (FSH) comprises an ?? subunit and a ?? subunit,whereas the FSH receptor consists of two halves with distinct functions, the N-terminalextracellular exodomain and C-terminal membrane associated endodomain. FSH initiallybinds to exodomain, and the resulting FSH/exodomain complex modulates the endodomainand generates signal. However, it has been difficult to determine which subunit of FSHcontacts the exodomain or endodomain, and in what orientation FSH interacts with them.To address these crucial issues, the receptor was Ala-scanned and the hormone subunitswere probed

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McCaffrey, Rebecca. "IDENTIFICATION AND CHARACTERIZATION OF CONTACT SITES BETWEEN HUMAN CHORIONIC GONADOTROPIN AND THE AMINO TERMINAL REGION OF THE LUTEINIZING HORMONE/CHORIOGONADOTROPIN RECEPTOR." UKnowledge, 2002. http://uknowledge.uky.edu/gradschool_theses/204.

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The luteinizing hormone / choriogonadotropin receptor (LH/CG-R) is a member of theG protein-coupled receptor family. The LH/CG-R has seven transmembrane helices, threeexoloops, three cytoloops, a C-terminal tail, and an extensive N-terminal exodomain. Theexodomain is capable of binding hormone with high affinity without hormone action. Previousstudies have shown that the amino-terminal region of the LH/CG receptor contacts both subunitsof human chorionic gonadotropin (hCG). In particular, three residues (Leu20, Cys22, and Gly24)were found to be crucial for hormone binding. In this thesis work,

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Preißler, Julia. "Die gliale Relevanz des G-Protein-gekoppelten Rezeptors 34." Doctoral thesis, Universitätsbibliothek Leipzig, 2015. http://nbn-resolving.de/urn:nbn:de:bsz:15-qucosa-167010.

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In der vorliegenden Arbeit wurde die Funktion des G-Protein-gekoppelten Rezeptors 34 (GPR34) in Mikroglia untersucht. Dieser Rezeptor weist eine hohe Expression auf Gliazellen auf, jedoch ist über dessen Aufgabe innerhalb dieser Zellpopulation bisher nichts bekannt. In bisherigen Arbeiten wurde dem GPR34 eine Rolle in der Immunantwort zugeschrieben. Knock-out (ko)-Mäuse, welche mit Cryptococcus neoformans infiziert wurden, zeigten im Vergleich zum infizierten Wildtyp (wt) eine deutlich höhere Pathogenlast in verschiedenen Geweben u.a. im Gehirn, was für eine inadäquate Immunantwort spricht. In

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Bittencourt, Fabiola M. "Examination of the Function of the Murine Cytomegalovirus Encoded G Protein-Coupled Receptor M33 in vivo." University of Cincinnati / OhioLINK, 2014. http://rave.ohiolink.edu/etdc/view?acc_num=ucin1397234044.

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Jin, Hongjun. "Structural and functional investigation of human chemokines and applications of human chemokines in blocking HIV-1 entry." [College Station, Tex. : Texas A&M University, 2007. http://hdl.handle.net/1969.1/ETD-TAMU-2430.

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Alice, Brown. "Allosteric Coupling in the Dimeric Calcium Sensing Receptor." Thesis, The University of Sydney, 2017. http://hdl.handle.net/2123/17738.

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The Calcium Sensing Receptor (CaSR) is a Class C GPCR that supports systemic calcium homeostasis by sensing and responding to small fluctuations in serum calcium (Ca2+o). It was hypothesised Cys-236 in the Venus Fly Trap Domain (VFTD) and Cys-561 in the Cysteine-Rich Domain (CRD) participate in an interdomain disulfide bond that is required for signal transmission. C236S, C561S, and C236S/C561S CaSR constructs were generated to eliminate the predicted disulfide and were analysed. While the mutant receptors failed to respond to VFTD-binding agonists and modulators, receptor activation was obs

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Kunisue, Sumihiro. "Roles of the Orphan Receptor Gpr176-mediated G-protein Signaling in the Central Circadian Clock." Kyoto University, 2019. http://hdl.handle.net/2433/242672.

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Ghimire, Ganga D., ガンガＤ. ギミレ, Kenichiro Imai, et al. "Physicochemical properties of amino acid sequences of G-proteins for understanding GPCR-G-protein coupling." Chem-Bio Informatics Society, 2006. http://hdl.handle.net/2237/9277.

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