English
norskBrowsing Det helsevitenskapelige fakultet by Author "Gabrielsen, Mari"
Now showing items 1-11 of 11
-
The 5-HT1E receptor. Receptor structure and ligand interactions.
(Master thesis; Mastergradsoppgave, 2006-12-08)5-HT (5-Hydroxytryptamine; Serotonin) is the neurotransmitter with the highest number of known receptors in humans, and the importance of 5-HT is also reflected in the number of species using 5-HT as a signalling molecule and the number of 5-HT receptors found within each species. 15 human 5-HT receptors have at this date been characterised and classified into seven 5-HT receptor families. Six of ... -
Exploring Conformational Dynamics of the Extracellular Venus flytrap Domain of the GABA B Receptor: A Path-Metadynamics Study
(Journal article; Tidsskriftartikkel; Peer reviewed, 2020-04-01)γ-Aminobutyric acid (GABA) is the main inhibitory neurotransmitter in the central nervous system (CNS). Dysfunctional GABAergic neurotransmission is associated with numerous neurological and neuropsychiatric disorders. The GABA<sub>B</sub> receptor (GABA<sub>B</sub>-R) is a heterodimeric class C G protein-coupled receptor (GPCR) comprised of GABA<sub>B1a/b</sub> and GABA<sub>B2</sub> subunits. The ... -
The GABAB Receptor - Structure, Ligand Binding and Drug Development
(Journal article; Tidsskriftartikkel; Peer reviewed, 2020-07-07)The γ-aminobutyric acid (GABA) type B receptor (GABA<sub>B</sub-R) belongs to class C of the G-protein coupled receptors (GPCRs). Together with the GABA<sub>A</sub> receptor, the receptor mediates the neurotransmission of GABA, the main inhibitory neurotransmitter in the central nervous system (CNS). In recent decades, the receptor has been extensively studied with the intention being to understand ... -
Homology Modeling of Human <gamma>-Butyric Acid Transporters and the Binding of Pro-drugs 5-Aminolevulinic Acid and Methyl Aminolevulinic Acid used in Photodynamic Therapy
(Journal article; Tidsskriftartikkel; Peer reviewed, 2013)Photodynamic therapy (PDT) is a safe and effective method currently used in the treatment of skin cancer. In ALA-based PDT, 5-aminolevulinic acid (ALA), or ALA esters, are used as pro-drugs to induce the formation of the potent photosensitizer protoporphyrin IX (PpIX). Activation of PpIX by light causes the formation of reactive oxygen species (ROS) and toxic responses. Studies have indicated that ... -
Homology Modeling of Transporter Proteins
(Journal article; Tidsskriftartikkel; Peer reviewed, 2023-03-24)Membrane transporter proteins are divided into channels/pores and carriers and constitute protein families of physiological and pharmacological importance. Several presently used therapeutic compounds elucidate their effects by targeting membrane transporter proteins, including anti-arrhythmic, anesthetic, antidepressant, anxiolytic and diuretic drugs. The lack of three-dimensional structures of ... -
Identification of novel serotonin transporter compounds by virtual Screening
(Journal article; Tidsskriftartikkel; Peer reviewed, 2014-02-12)The serotonin (5-hydroxytryptamine, 5-HT) transporter (SERT) plays an essential role in the termination of serotonergic neurotransmission by removing 5-HT from the synaptic cleft into the presynaptic neuron. It is also of pharmacological importance being targeted by antidepressants and psychostimulant drugs. Here, five commercial databases containing approximately 3.24 million drug-like compounds ... -
In Silico Methods for the Discovery of Orthosteric GABAB Receptor Compounds
(Journal article; Tidsskriftartikkel; Peer reviewed, 2019-03-07)The GABA<sub>B</sub> receptor (GABA<sub>B</sub>-R) is a heterodimeric class C G protein-coupled receptor comprised of the GABA<sub>B1a/b</sub> and GABA<sub>B2</sub> subunits. The endogenous orthosteric agonist γ-amino-butyric acid (GABA) binds within the extracellular Venus flytrap (VFT) domain of the GABA<sub>B1a/b</sub> subunit. The receptor is associated with numerous neurological and ... -
Ligand-guided homology modelling of the GABAb2 subunit of the GABAb receptor
(Journal article; Tidsskriftartikkel; Peer reviewed, 2017-03-21)γ-aminobutyric acid (GABA) is the main inhibitory neurotransmitter in the central nervous system, and disturbances in the GABAergic system have been implicated in numerous neurological and neuropsychiatric diseases. The GABA<sub>B</sub> receptor is a heterodimeric class C G protein-coupled receptor (GPCR) consisting of GABA<sub>B1a/b</sub> and GABA<sub>B2</sub> subunits. Two GABA<sub>B</sub> receptor ... -
Structure, function and inhibition of the serotonin transporter studied by molecular docking, -dynamics and virtual screening
(Doctoral thesis; Doktorgradsavhandling, 2011-09-16)Den tre-dimensjonale (3D) strukturen til serotonin-transporteren er ukjent og arbeidet som beskrives i avhandlingen er basert på teoretiske 3D-modeller av transporteren. Modellene har blitt brukt til å simulere bevegelsene i transporterstrukturen som skjer når serotonin transporteres samt til å studere hvordan forbindelser som blokkerer transporten binder til transporteren. For å gjøre det sistnevnte ... -
Substrate binding and translocation of the serotonin transporter studied by docking and molecular dynamics simulations
(Journal article; Tidsskriftartikkel; Peer reviewed, 2011-06-14)The serotonin (5-HT) transporter (SERT) plays an important role in the termination of 5-HT-mediated neurotransmission by transporting 5-HT away from the synaptic cleft and into the presynaptic neuron. In addition, SERT is the main target for antidepressant drugs, including the selective serotonin reuptake inhibitors (SSRIs). The three-dimensional (3D) structure of SERT has not yet been determined, ... -
Synthesis, in vitro and in vivo biological evaluation of new oxysterols as modulators of the liver X receptors
(Journal article; Tidsskriftartikkel; Peer reviewed, 2016-07-26)Liver X Receptor (LXR) modulators have shown potential as drugs since they target genes affecting metabolism and fatty acid synthesis. LXR antagonists are of particular interest since they are able to reduce the synthesis of complex fatty acids and glucose uptake. Based on molecular modeling, five new cholesterol mimics were synthesized, where four contained a hydroxyl group in the 22-S-position. ...
