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Wyszukujesz frazę "GPCR" wg kryterium: Temat

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    Wyświetlanie 1-5 z 5
    Tytuł:
    Interaction of class A G protein-coupled receptors with G protein.
    Autorzy:
    Ślusarz, Rafał
    Ciarkowski, Jerzy
    Powiązania:
    https://bibliotekanauki.pl/articles/1043328.pdf
    Data publikacji:
    2004
    Wydawca:
    Polskie Towarzystwo Biochemiczne
    Tematy:
    GPCR class A
    GPCR activation
    G protein
    Opis:
    A model for interaction of class A G protein-coupled receptor with the G protein Gα subunit is proposed using the rhodopsin-transducin (RD/Gt) prototype. The model combines the resolved interactions/distances, essential in the active RD*/Gt system, with the structure of Gtα C-terminal peptide bound to RD* while stabilizing it. Assuming the interactions involve conserved parts of the partners, the model specifies the conserved Helix 2 non-polar X- - -X, Helix 3 DRY and Helix 7/8 NP- -Y- - F RD* motifs interacting with the Gtα C-terminal peptide, in compliance with the structure of the latter. A concomitant role of Gtα and Gtγ>C-termini in stabilizing RD* could possibly be resolved assuming a receptor dimer as requisite for G protein activation.
    Źródło:
    Acta Biochimica Polonica; 2004, 51, 1; 129-136
    0001-527X
    Pojawia się w:
    Acta Biochimica Polonica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Molecular docking-based test for affinities of two ligands toward vasopressin and oxytocin receptors.
    Autorzy:
    Ślusarz, Rafał
    Kaźmierkiewicz, Rajmund
    Giełdoń, Artur
    Lammek, Bernard
    Ciarkowski, Jerzy
    Powiązania:
    https://bibliotekanauki.pl/articles/1044173.pdf
    Data publikacji:
    2001
    Wydawca:
    Polskie Towarzystwo Biochemiczne
    Tematy:
    simulated annealing
    bioligand docking
    GPCR receptor/bioligand interaction
    molecular dynamics
    Opis:
    Molecular docking simulations are now fast developing area of research. In this work we describe an effective procedure of preparation of the receptor-ligand complexes. The amino-acid residues involved in ligand binding were identified and described.
    Źródło:
    Acta Biochimica Polonica; 2001, 48, 1; 131-135
    0001-527X
    Pojawia się w:
    Acta Biochimica Polonica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Targets for majority of drugs: G protein-coupled receptors - their structure and interaction with bioligands
    Autorzy:
    Ciarkowski, J.
    Czaplewski, C.
    Pasenkiewicz-Gierula, M.
    Powiązania:
    https://bibliotekanauki.pl/articles/1953953.pdf
    Data publikacji:
    1998
    Wydawca:
    Politechnika Gdańska
    Tematy:
    G protein-coupled receptor
    molecular modelling
    GPCR/bioligand interaction
    molecular dynamics
    membrane
    Opis:
    G protein-coupled receptors (GPCRs) are the most frequent targets for many drugs. They form the largest superfamily of integral membrane proteins, of which more than 1000 members have the following common features: (i) All GPCRs form 7 hydrophobic a-helices of length ~38A (25 amino acids, 7 turns) along a single chain. The consecutive helices alternatively cross the membrane, starting from the extracellular side, so that they form a heptahelical transmembrane domain interwoven with 6 loops, of which the even ones plus the N-terminus create the receptor's extracellular domain while the odd ones plus the C-terminus form its intracellular domain. (ii) All GPCRs are stimulated by diverse extracellular (primary) signals. (iii) Stimulated GPCRs convey the primary signals via their transmembrane and intracellular domains to the cytosolic peripheral heterotrimeric GTP-binding proteins (G proteins), mediating the signal's further transduction to various cellular second messenger systems. A current status of structural studies on GPCRs, consisting of low ~7.5A resolution experimental structures and supplementary molecular modeling, is outlined. Subsequently, some results of authors' own work on studying essential interactions of the V2 vasopressin renal receptor (V2R) with its agonist [Arg8]Vasopressin (AVP) and selected antagonists are presented, as well as their possible impact on the biological signal transduction is discussed. Finally, perspectives for future developments are sketched.
    Źródło:
    TASK Quarterly. Scientific Bulletin of Academic Computer Centre in Gdansk; 1998, 2, 4; 583-599
    1428-6394
    Pojawia się w:
    TASK Quarterly. Scientific Bulletin of Academic Computer Centre in Gdansk
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Molecular modelling study of the role of cholesterol in the stimulation of the oxytocin receptor.
    Autorzy:
    Politowska, Ewa
    Kaźmierkiewicz, Rajmund
    Wiegand, Volker
    Fahrenholz, Falk
    Ciarkowski, Jerzy
    Powiązania:
    https://bibliotekanauki.pl/articles/1044168.pdf
    Data publikacji:
    2001
    Wydawca:
    Polskie Towarzystwo Biochemiczne
    Tematy:
    cholesterol
    AutoDock 2.4
    cholecystokinin receptor type β
    oxytocin receptor
    GPCR
    sterols
    Opis:
    Cholesterol, an integral component of membranes in Eucaryota, is a modifier of membrane properties. In vivo studies have demonstrated that cholesterol can also modulate activities of some G protein-coupled receptors (GPCRs), which are integral membrane proteins. This can result either from an effect of cholesterol on the membrane fluidity or from specific interactions of the membrane cholesterol with the receptor, as recently demonstrated for the cholecystokinin type β (CCKRβ) or the oxytocin receptor (OTR). Using molecular modelling, we studied conformational preferences of cholesterol and several of its analogues. Subsequently, we simulated the distributions of their preferred conformations around the surface of OTR, CCKRβ and a chimeric oxytocin/cholecystokinin receptor. Consequently, we suggest residues on the surface of OTR which are potentially significant in the OTR/cholesterol interaction.
    Źródło:
    Acta Biochimica Polonica; 2001, 48, 1; 83-93
    0001-527X
    Pojawia się w:
    Acta Biochimica Polonica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Emerging role of alternative splicing of CRF1 receptor in CRF signaling
    Autorzy:
    Żmijewski, Michał
    Slominski, Andrzej
    Powiązania:
    https://bibliotekanauki.pl/articles/1040411.pdf
    Data publikacji:
    2010
    Wydawca:
    Polskie Towarzystwo Biochemiczne
    Tematy:
    corticotropin-releasing factor
    corticotropin-releasing factor receptor type 1
    G-proteins
    GPCR
    hypothalamus-pituitary-adrenal axis
    skin stress
    Opis:
    Alternative splicing of mRNA is one of the most important mechanisms responsible for an increase of the genomic capacity. Thus the majority of human proteins including G protein-coupled receptors (GPCRs) possess several isoforms as a result of mRNA splicing. The corticotropin-releasing factor (CRF) and its receptors are the most proximal elements of hypothalamic-pituitary-adrenal axis (HPA) - the central machinery of stress response. Moreover, expression of CRF and regulated activity of CRF receptor type 1 (CRF1) can also play an important role in regulation of local stress response in peripheral tissues including skin, gastrointestinal tract or reproductive system. In humans, expression of at least eight variants of CRF1 mRNA (α, β, c, d, e, f, g and h) was detected and alternative splicing was found to be regulated by diverse physiological and pathological factors including: growth conditions, onset of labor, during pregnancy or exposure to ultraviolet irradiation. The pattern of expression of CRF1 isoforms is cell type specific and recently has been linked to observed differences in responsiveness to CRF stimulation. In the proposed model of regulation of CRF-signaling, isoform CRF1α plays a central role. Other isoforms modulate its activity by oligomerization, leading to alteration in receptor trafficking, localization and function. Co-expression of CRF1 isoforms modulates sensitivity of cells to the ligands and influences downstream coupling to G-proteins. The other possible regulatory mechanisms include fast mRNA and/or protein turnover or decoy receptor function of CRF1 isoforms. Taken together, alternative splicing of CRF1 can represent another level of regulation of CRF-mediated stress responses at the central and peripheral levels. Chronic stress or malfunction of the HPA-axis have been linked to numerous human pathologies, suggesting that alternative splicing of CRF1 receptor could represent a promising target for drugs development.
    Źródło:
    Acta Biochimica Polonica; 2010, 57, 1; 1-13
    0001-527X
    Pojawia się w:
    Acta Biochimica Polonica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
      Wyświetlanie 1-5 z 5

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