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Dissertations / Theses on the topic 'Receptores GPCR'

Author: Grafiati

Published: 4 June 2021

Last updated: 1 February 2022

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1

Prischich, Davia. "Development and applications of photoswitchable small molecules and peptides to control protein-protein interactions and GPCR activity." Doctoral thesis, Universitat de Barcelona, 2021. http://hdl.handle.net/10803/671019.

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Photopharmacology is an emerging field that relies on the development of photosensitive compounds to enable precise spatiotemporal control over endogenous proteins. Photochromic ligands· are designed to respond to specific wavelengths of light with a reversible change of structure that enhances or diminishes their activity or affinity towards the desired target. Applications are expected to lead to safer treatments in medicine and to innovative tools to investigate complex signalling networks in biology. Thus, in this thesis we aimed at further expanding the spec

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2

Callén, Herrero Lucía. "Expresión, función y heteromerización de receptores de cannabinoides CB(2) en el sistema nervioso central." Doctoral thesis, Universitat de Barcelona, 2012. http://hdl.handle.net/10803/101513.

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Dentro del sistema endocannabinoide, los receptores de cannabinoides, hasta ahora clonados y caracterizados, son principalmente dos: el de tipo 1 (CB1R) y el de tipo 2 (CB2R). A pesar de que el CB1R se ha determinado ampliamente en el sistema nervioso central (CNS) y su acción se ha visto mediante de una gran variedad de procesos cognitivos y neurológicos, al receptor CB2 se le había atribuido, desde su clonación, una presencia exclusivamente periférica y un papel fundamental en el sistema inmunológico. Sin embargo, en los últimos años, no han sido desdeñables el número de publicaciones orien

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3

Kerr, Daniel Shikanai. "Ric-8B, uma GEF putativa do sistema olfatório, interage com Gαolf, Gβ1 e Gγ13." Universidade de São Paulo, 2008. http://www.teses.usp.br/teses/disponiveis/46/46131/tde-22122008-092032/.

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O sistema olfatório de mamíferos é capaz de detectar milhares de substâncias químicas diferentes, mesmo em baixas concentrações. Um odorante disperso no ar pode se ligar a um receptor olfatório (OR) iniciando o processo de detecção. Os ORs são membros da super família de receptores acoplados a proteína G (GPCRs). Apesar de a via de transdução de sinal de odorantes estar bem descrita, pouco se sabe sobre os seus moduladores. Em 2005, nosso laboratório identificou RIC-8B como um possível fator de troca de nucleotídeos de guanina (GEF) que poderia amplificar a atividade da proteína G olfatória (G

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4

Moreno, Guillén Estefanía. "Heterómeros de receptores de dopamina. Nuevos mecanismos para la regulación de la transmisión dopaminérgica." Doctoral thesis, Universitat de Barcelona, 2012. http://hdl.handle.net/10803/81924.

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El Objetivo General de esta Tesis ha sido investigar la formación y función de heterómeros entre receptores de dopamina y otros receptores que puedan estar implicados en la regulación de la transmisión dopaminérgica, como receptores de galanina, histamina, adrenérgicos o receptores sigma-1. Basándonos en que tanto la galanina como la dopamina modulan la liberación de acetilcolina en el hipocampo, se ha demostrado que los receptores de dopamina de la familia D1 (receptores D1 y D5) pueden formar heterómeros con los receptores de galanina Gal1 y Gal2 y se ha estudiado la función de estos heteróm

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5

Casallanovo, Fabio. "Estudos conformacionais de seqüências hidrofóbicas de domínios de receptores acoplados a proteínas G (GPCR) e da proteína G. Um estudo de CD e espectroscopia de fluorescência." Universidade de São Paulo, 2004. http://www.teses.usp.br/teses/disponiveis/46/46131/tde-22092015-154017/.

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O estudo fitoquímico do extrato etanólico de caules adultos de Araucaria angustifólia resultou no isolamento e identificação da vanilina, p-hidroxibenzaldeído, coniferaldeído, dois isoflavonóides (cabreuvina e irisolidona), quatro lignanas (pinoresinol, eudesmina, lariciresinol e 9\'-O-acetato de lariciresinol) e β-sitosterol. Foi desenvolvido um protocolo para a obtenção de calos, a partir de caules de plântulas estioladas, dos quais foram isolados e caracterizados mistura de isômeros E e Z do p-cumarato de octadecila e do ferulato de octadecila.<br>Phytochemical investigations carried o

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6

Gandía, Sánchez Jorge. "Oligomerización del receptor A2A de adenosina: interpretando el receptorsoma." Doctoral thesis, Universitat de Barcelona, 2013. http://hdl.handle.net/10803/134352.

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Los receptores acoplados a proteína G (GPCR) conforman la familia de receptores de membrana más grande. El numeroso y variado tipo de señales que detectan han otorgado a estos receptores un alto interés farmacológico. Además, las interacciones entre diferentes tipos de GPCR formando complejos oligoméricos dan lugar a complejos con características bioquímicas diferenciadas de los protómeros que los forman. En esta Tesis Doctoral se han estudiado diferentes aspectos derivados este tipo de interacciones, centrando estos experimentos alrededor del receptor A2A de adenosina (A2AR), un importante ne

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7

Meira, Guilherme Louzada Silva. "Analíse da expressão do receptor olfativo M93 em sistemas heterólogos." Universidade de São Paulo, 2004. http://www.teses.usp.br/teses/disponiveis/46/46131/tde-31082016-115408/.

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O sistema olfatório de mamífero pode discriminar milhares de odores presentes no meio ambiente. Aproximadamente 1000 diferentes receptores olfatórios (ORs) são expressos no epitélio olfatório (OE) do nariz, Os ORs detectam os odores e transmitem os sinais resultantes para o bulbo olfatório (OB) no cérebro. Os ORs pertencem a super família dos receptores acoplados a proteína G (GPCR) e apresentam sete domínios transmembrânicos putativos. Por razões desconhecidas, os ORs são retidos no retículo endoplasmático quando expressos em linhagens de células de mamíferos heterólogas. Provavelmente, prote

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8

Troupiotis-Tsaïlaki, Anastassia. "Lipid-GPCR interactions: from activation of sphingosine-1-phosphate receptors to modulation of vasopressin V2 receptor function." Doctoral thesis, Universite Libre de Bruxelles, 2015. http://hdl.handle.net/2013/ULB-DIPOT:oai:dipot.ulb.ac.be:2013/216727.

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GPCRs form the largest family of membrane proteins in human genome and mediate signal transmission in a wide panel of essential physiological processes, and they are thus a major source of pharmaceutical targets. Investigating GPCR interactions with their cognate ligands and their membrane environment is crucial to understand their function at a molecular level. While major breakthroughs in the determination of high resolution structures of GPCRs in inactive and active states have shed a new light on the structural basis of GPCR activation process, complementary approaches are needed to invest

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9

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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10

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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11

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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12

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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13

Diness, Frederik. "Solid-phase reactions of N-carbamyliminium ions : from amino aldehydes to on-bead GPCR-screening /." Cph. ; Valby : Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences : Center for solid-phase organic combinatiorial chemistry, Carlsberg Laboratory, 2006. http://www.dfuni.dk/index.php/Frederik-Diness/3031/0/.

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14

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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15

Nanekar, R. (Rahul). "Biochemical and biophysical studies on adenosine receptors and their interaction partners." Doctoral thesis, Oulun yliopisto, 2016. http://urn.fi/urn:isbn:9789526211022.

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Abstract Adenosine receptors are heterotrimeric guanine nucleotide-binding (G protein)-coupled receptors (GPCRs) that mediate the effects of the endogenous agonist adenosine. The adenosine A3 receptor (A3R) is the least explored among the four human adenosine receptor subtype members (A1, A2A, A2B and A3) and it is implicated in both neuroprotective and neurodegenerative effects. During the course of this work, the production of the recombinant human A3R in yeast and insect cells was evaluated and heteromerization between the human adenosine A2A receptor (A2AR) and the dopamine D2 receptor (D2

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16

Park, Jung Hee. "Crystal structure of ligand-free G-protein-coupled receptor opsin." Doctoral thesis, Humboldt-Universität zu Berlin, Mathematisch-Naturwissenschaftliche Fakultät I, 2010. http://dx.doi.org/10.18452/16049.

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Rhodopsin ist als Sehpigment der Photorezeptorzellen einer der am aktivsten untersuchten GPCRs. Es besteht aus dem Apoprotein Opsin und dem inversen Agonisten 11-cis-Retinal. Der inaktivierende Ligand ist in der sieben Transmembran- Helix (TM)-Struktur des Rezeptors kovalent gebunden und muss durch Licht cis/trans-isomerisiert werden, um den Rezeptor zu aktivieren. Der aktivierte Rezep-tor katalysiert den Nukleotidaustausch im G-Protein und zerfällt innerhalb von Minuten in Opsin und all-trans-Retinal. Das visuelle Pigment wird dann durch erneute Beladung des Opsins mit 11-cis-Retinal wieder

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17

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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18

Jones, Kymry Thereasa. "The role of beta-arrestin in regulating the muscarinic acetylcholine type II receptor." Diss., Atlanta, Ga. : Georgia Institute of Technology, 2007. http://hdl.handle.net/1853/24815.

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Thesis (Ph.D.)--Biology, Georgia Institute of Technology, 2008.<br>Committee Chair: Dr. Nael A. McCarty; Committee Co-Chair: Dr. Darrell Jackson; Committee Member: Dr. Alfred H. Merrill; Committee Member: Dr. Barbara D. Boyan; Committee Member: Dr. Harish Radhakrishna; Committee Member: Dr. Marion B. Sewer

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19

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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20

Vincent, Karla Kristine. "Transactivation of Beta 2 Adrenergic Receptor by Bradykinin type 2 Receptor via heterodimerization." Diss., Georgia Institute of Technology, 2009. http://hdl.handle.net/1853/37117.

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Although a long standing convention maintained that G Protein Coupled Receptors (GPCRs) exist in the plasma membrane solely as monomers, substantial work over the last two decades has demonstrated that these ubiquitous receptors can and in many cases, preferentially, exist as homodimers, heterodimers, or higher order oligomers. Often, two GPCRs of the same class heterodimerize; it is less common for two GPCRs of different signaling pathways to interact. The work presented here studied the physical and functional interaction of two GPCRs from discrete classes, the Beta 2 Adrenergic Receptor

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21

Sallander, Eva Jessica. "The mechanism of G protein coupled receptor activation: the serotonin receptors." Doctoral thesis, Universitat Pompeu Fabra, 2011. http://hdl.handle.net/10803/77901.

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Una de las principales cuestiones en farmacología molecular de los GPCR es entender los mecanismos estructurales de las siete hélices transmembrana (TM) que se producen para estabilizar ya sea Rg o los diferentes estados R*. Para entender el mecanismo que cambia el equilibrio del conjunto a un estado activo R* se construyeron tres de los receptores de la serotonina (5-HT4, 5-HT6, y 5 HT7) sobre la base de su información más reciente de cristalografía de rayos X. Dando lugar a dos modelos de cada receptor: una inactiva y otra activa. Los modelos, mejorados y evaluados con la ayuda de datos fa

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22

Xiang, Guoqing. "Signaling Through Homomeric and Heteromeric Cannabinoid CB1 receptors." VCU Scholars Compass, 2018. https://scholarscompass.vcu.edu/etd/5683.

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Cannabis (Marijuana) has multiple effects on the human body, such as analgesia, euphoria and memory impairment. Delta-9 tetrahydrocannabinol (D9-THC), the active ingredient in cannabis, binds to cannabinoid receptors, seven-transmembrane G protein-coupled receptors (GPCRs) that mediate a variety of physiological functions. GPCRs were believed to function only in homomeric forms, however, recent findings show that different GPCRs can also form heteromeric complexes that may expand their signaling properties. In this study, we focused on Cannabinoid CB1 receptor (CB1R) heteromers with the mu-opi

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23

Hunt, James. "Adhesion GPCRs : structural insights into receptor coupling." Thesis, University of Leeds, 2010. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.590267.

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G-protein coupled receptors (GPCRs) are a diverse superfamily of membrane proteins. They have a wide range of physiological roles and include many successful drug targets. Sequencing of the human genome has revealed a distinct subfamily of GPCRs known as Adhesion GPCRs. These receptors possess unusually large extracellular N-terminal domains which are believed to be involved in cell-cell adhesion. Few data are available which demonstrate that these receptors are able to couple to G-proteins, their classification as GPCRs is primarily based on homology and predicted topology. These receptors ar

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24

Sheffler, Douglas James. "The Regulation of G Protein-Coupled Receptor (GPCR) Signal Transduction by p90 Ribosomal S6 Kinase 2 (RSK2)." Connect to text online, 2006. http://rave.ohiolink.edu/etdc/view?acc%5Fnum=case1130777469.

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25

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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26

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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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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28

Sreedharan, Smitha. "Functional Characterization of Centrally Expressed Solute Carriers and G Protein-Coupled Receptors." Doctoral thesis, Uppsala universitet, Funktionell farmakologi, 2011. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-156832.

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Transmembrane proteins are gatekeepers of the cells; controlling the transport of substrates as well as communicating signals among cells and between the organelles and cytosol. Solute carriers (SLC) and G protein-coupled receptors (GPCR) are the largest family of membrane transporters and membrane receptors respectively. The overall aim of this thesis was to provide a basic understanding of some of the novel SLCs and GPCRs with emphasis on expression, transport property, evolution and probable function. The first part of the thesis directs towards the study of some novel solute carriers. In a

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29

Runesson, Johan. "Galanin receptor ligands." Licentiate thesis, Stockholms universitet, Institutionen för neurokemi, 2009. http://urn.kb.se/resolve?urn=urn:nbn:se:su:diva-59743.

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In the nervous system galanin primarily displays a modulatory role. The galaninergic system consists of a number of bioactive peptides with a highly plastic expression pattern and three different receptors. The lack of receptor subtype selective ligands and antibodies have severely hampered the charac-terization of this system. Therefore, most of the knowledge has been drawn from experiments with transgenic animals, which has given some major conclusions, despite the compensatory effects seen in several animal studies. Therefore, the production of subtype selective ligands is of great importan

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Park, Gyu. "Receptor influences in GIRK current activation and desensitization." VCU Scholars Compass, 2011. http://scholarscompass.vcu.edu/etd/2513.

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G protein-coupled receptors (GPCRs) are seven-transmembrane domain receptors that sense extracellular signal and activate intracellular signaling pathways. Metabotropic glutamate receptor 2 (mGluR2) is one of the GPCRs coupled to Gi/o proteins whose Gβγ subunits stimulate G protein-gated inwardly rectifying K+ channels (GIRKs). Previous experiments demonstrated that in planar lipid bilayer both active forms of G proteins [Gα (GTPγS-stimulated) and Gβγ subunits] were required to activate GIRK channels in the absence of the receptor, but surprisingly, the Gβγ subunit alone could activate GIRK ch

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Gloriam, David E. "G Protein-Coupled Receptors; Discovery of New Human Members and Analyses of the Entire Repertoires in Human, Mouse and Rat." Doctoral thesis, Uppsala : Acta Universitatis Upsaliensis : Universitetsbiblioteket [distributör], 2006. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-6745.

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Johansson, Lisa. "Calcium and Phospholipases in Orexin Receptor Signaling." Doctoral thesis, Uppsala : Acta Universitatis Upsaliensis : Univ.-bibl. [distributör], 2008. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-8613.

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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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Deliu, Elena. "GPER/GPR30 Estrogen Receptor: A Target for Pain Modulation." Diss., Temple University Libraries, 2012. http://cdm16002.contentdm.oclc.org/cdm/ref/collection/p245801coll10/id/194862.

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Pharmacology<br>Ph.D.<br>The G protein-coupled estrogen receptor GPER/GPER1, also known as GPR30, was originally cloned as an orphan receptor and later shown to be specifically activated by 17-ß-estradiol. This has led to its classification as an estrogen receptor and expanded the perspective on the mechanisms underlying the rapid estrogenic effects reported over the years. GPER is strongly expressed in the central nervous system and peripheral tissues and appears to be involved in a wide variety of physiological and pathological processes. Estrogens are known to alter the processing of nocice

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Ehrlich, Aliza Toby. "The dissection of the molecular mechanism underlying the facilitative action of prostaglandin E receptor EP1 on dopamine D1 receptor-induced cAMP production." 京都大学 (Kyoto University), 2013. http://hdl.handle.net/2433/180537.

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Marcott, Pamela F. "Mechanisms of dopamine D2-receptor activation across the striatum." Case Western Reserve University School of Graduate Studies / OhioLINK, 2017. http://rave.ohiolink.edu/etdc/view?acc_num=case1502719812531202.

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Mohammed, Kader Hamno. "Development of a label-free biosensor method for the identification of sticky compounds which disturb GPCR-assays." Thesis, Uppsala universitet, Institutionen för biologisk grundutbildning, 2013. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-220645.

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It is widely known that early estimates about the binding properties of drug candidates are important in the drug discovery process. Surface plasmon resonance (SPR) biosensors have become a standard tool for characterizing interactions between a great variety of biomolecules and it offers a unique opportunity to study binding activity. The aim of this project was to develop a SPR based assay for pre-screening of low molecular weight (LMW) drug compounds, to enable filtering away disturbing compounds when interacting with drugs. The interaction between 47 LMW compounds and biological ligands we

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Aloia, Amanda Louise, and amanda aloia@hotmail com. "Expression, Purification and Crystallisation Studies with the M2 Muscarinic and H1 Histamine Receptors." Flinders University. Biological Sciences, 2008. http://catalogue.flinders.edu.au./local/adt/public/adt-SFU20080709.132140.

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This thesis describes the expression of three human seven transmembrane receptors: the M2 Muscarinic; H1 Histamine and 5HT2A Serotonin receptors, in the baculovirus/insect cell expression system. Purification trials werre conducted on the M2 Muscarinic and H1 Histamine receptors. Preliminary crystallisation attempts were made with the H1 receptor.

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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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Haris, Shaikh Lalarukh. "The role of G-protein coupled receptors (GPCRs), LGR5 and GPR61 in aldosterone production." Thesis, University of Cambridge, 2015. https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.709218.

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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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Dezi, Cristina. "Modeling of 5-HT2A and 5-HT2C receptors and of theirs complexes with actual and potential antypsichotic drugs." Doctoral thesis, Universitat Pompeu Fabra, 2008. http://hdl.handle.net/10803/7127.

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La presente tesis "Modelling of 5-HT2A and 5-HT2C receptors and of their complexes with actual and potential antipsychotic drugs" tiene como objetivo de profundizar los conocimientos actuales sobre el mecanismo de acción de los fármacos antipsicóticos. En este proyecto de larga duración, se han construidos modelos computacionales de los receptores 5-HT2A y 5-HT2C, utilizando un nuevo protocolo de modelización basado sobre los datos experimentales de otras proteínas GPCR de la misma familia. Las estructuras 3D se han validado e utilizado en estudios de acoplamiento ligando-receptor, simulacione

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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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Dromey, Jasmin Rachel. "Elucidating novel aspects of hypothalamic releasing hormone receptor regulation." University of Western Australia. School of Medicine and Pharmacology, 2008. http://theses.library.uwa.edu.au/adt-WU2008.0133.

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[Truncated abstract] G-protein coupled receptors (GPCRs) form one of the largest superfamilies of cell-surface receptors and respond to a vast range of stimuli including light, hormones and neurotransmitters. Although structurally similar, GPCRs are regulated by many diverse proteins, which allow the specific functions of each receptor to be carried out. This thesis focussed on two well-documented GPCRs, the thyrotropin releasing hormone receptor (TRHR) and gonadotrophin-releasing hormone receptor (GnRHR), which control the thyroid and reproductive endocrine pathways respectively. Although eac

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Cordomí, Montoya Arnau. "Molecular dynamics simulations of seven-transmembrane receptors." Doctoral thesis, Universitat Politècnica de Catalunya, 2008. http://hdl.handle.net/10803/6464.

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Seven transmembrane (7-TM) G protein coupled receptors (GPCR) constitute the largest family of integral membrane proteins in eukaryotes with more than 1000 members and encoding more than 2% of the human genome. These proteins play a key role in the transmission and transduction of cellular signals responding to hormones, neurotransmitters, light and other agonists, regulating basic biological processes. Their natural abundance together with their localization in the cell membrane makes them suitable targets for therapeutic intervention. Consequently, GPCR are proteins with enormous pharmacolog

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Bjarnadóttir, Þóra Kristín. "The Gene Repertoire of G protein-coupled Receptors : New Genes, Phylogeny, and Evolution." Doctoral thesis, Uppsala University, Department of Neuroscience, 2006. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-6627.

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<p>The superfamily of G protein-coupled receptors (GPCRs) is one of the largest protein families of mammalian genomes and can be divided into five main families; <i>Glutamate</i>, <i>Rhodopsin</i>, <i>Adhesion</i>, <i>Frizzled</i>, and <i>Secretin</i>. GPCRs participate in most major physiological functions, contributing to the fact that they are important targets in drug discovery. In paper I we mined the human and mouse genomes for new <i>Adhesion</i> GPCR genes. We found two new human genes (GPR133 and GPR144) and 17 mouse <i>Adhesion</i> genes, bringing the number up to 33 human and 31 mou

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Unal, Hamiyet. "Ligand-induced conformations of extracellular loop 2 of AT1R." Cleveland State University / OhioLINK, 2010. http://rave.ohiolink.edu/etdc/view?acc_num=csu1282068466.

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Favara, David M. "The biology of ELTD1/ADGRL4 : a novel regulator of tumour angiogenesis." Thesis, University of Oxford, 2017. http://ora.ox.ac.uk/objects/uuid:0d00af0a-bb43-44bc-ba0b-1f8acbe34bc5.

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<strong>Background:</strong> Our laboratory identified ELTD1, an orphan GPCR belonging to the adhesion GPCR family (aGPCR), as a novel regulator of angiogenesis and a potential anti-cancer therapeutic target. ELTD1 is normally expressed in both endothelial cells and vascular smooth muscle cells and expression is significantly increased in the tumour vasculature. The aim of this project was to analyse ELTD1's function in endothelial cells and its role in breast cancer. <strong>Method:</strong> 62 sequenced vertebrate genomes were interrogated for ELTD1 conservation and domain alterations. A phy

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Joseph, Nerine Theresa. "Characterisation of the tissue-specific expression, pharmacology and signalling cascades activated by chicken GnRH receptor subtypes suggested evolutionary specialisation of type III cGnRH receptor function." Thesis, University of Edinburgh, 2010. http://hdl.handle.net/1842/4802.

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Variant GnRH ligand and receptor subtypes have been identified in a number of non-mammalian vertebrate species, however research into avian species GnRH systems is lacking. Two isoforms of GnRH are present in the domestic chicken, the evolutionarily conserved GnRH-II and diverged cGnRH-I. The expression of two GnRH ligands parallels the expression of two chicken GnRH receptor subtypes; cGnRH-R-I and the novel cGnRH-R-III. The occurrence of two isoforms of the receptor in the chicken raises questions about their specific biological functions and interactions with the two ligands. Differential r

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Guixà, González Ramon 1978. "Modeling the interplay between membrane lipids and GPCRs." Doctoral thesis, Universitat Pompeu Fabra, 2014. http://hdl.handle.net/10803/318169.

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La composición lipídica de las membranas celulares determina en última instancia sus propiedades biofísicas, afectando así las dinámicas y organización de proteinas transmembrana claves como los receptores acoplados a proteínas G (GPCRs). El objetivo de esta tesis es avanzar en la comprensión y el alcance de la interacción entre lípidos de membrana y GPCRs. Para ello, hemos utilizado simulaciones de dinámicas moleculares para estudiar la complejidad de las membrana biológicas y su efecto en la organización de las GPCRs. Así, hemos desarrollado on marco computacional para analizar con detalle l

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