Search for dissertations about: "Allosteric Modulators"

Showing result 1 - 5 of 8 swedish dissertations containing the words Allosteric Modulators.

2. 1. Structure-based Virtual Screening for Ligands of G Protein-coupled Receptors : Design of Allosteric and Dual-Target Modulators

   Author : Stefanie Kampen; Jens Carlsson; Peter Kolb; Uppsala universitet; []
   Keywords : NATURVETENSKAP; NATURAL SCIENCES; G protein-coupled receptors; Polypharmacology; Molecular Docking; Structure-based Drug Design; Parkinson’s Disease; Virtual Screening; Allosteric Modulators; Bioinformatics; Bioinformatik;

   Abstract : G protein-coupled receptors (GPCRs) are integral membrane proteins responsible for signal transduction of extracellular stimuli into the cell. Because of their widespread distribution throughout the human body and important roles in physiological processes, GPCRs are prominent drug targets and approximately 34% of all approved drugs interact with members of this superfamily. READ MORE

4. 2. Free Fatty Acid Receptor 2 - A G protein coupled receptor with unique signaling properties in neutrophils

   Author : Simon Lind; Göteborgs universitet; []
   Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Neutrophils; G protein coupled receptors; Free Fatty Acid Receptor 2; GPR43; Allosteric modulation; Transactivation; Cross-talk; Biased signalling; Functional selectivity;

   Abstract : The overall aim of the PhD thesis was to determine the role of neutrophil pattern recognition receptors in the initiation and resolution of inflammatory processes. Neutrophil pattern recognition receptors such as the formyl peptide receptors (FPRs) and the short free fatty acid receptors (FFARs) belong to the family of G protein coupled receptors (GPCR). READ MORE

5. 3. Allosteric modulation of pentameric ligand-gated ion channels by general anesthetics

   Author : Stephanie A. Heusser; Erik Lindahl; Pierre-Jean Corringer; Stockholms universitet; []
   Keywords : NATURVETENSKAP; NATURAL SCIENCES; Biochemistry; biokemi;

   Abstract : Pentameric ligand-gated ion channels (pLGICs) are key components of fast synaptic transmission and are targets of neuroactive drugs such as benzodiazepines, alcohol and muscle relaxants. Although early theories of general anesthesia suggested non-specific lipid interaction as the mechanism of anesthetic action, it has now become evident that they too bind to pLGICs. READ MORE

6. 4. Simulating Functional Cycles and Drug Modulation in Ligand-gated Ion Channels

   Author : Yuxuan Zhuang; Erik Lindahl; Grace Brannigan; Stockholms universitet; []
   Keywords : NATURVETENSKAP; NATURAL SCIENCES; ion channels; molecular dynamics; markov state model; lipid modulation; nicotinic receptor; protein conformational transitions; Biophysics; biofysik;

   Abstract : Understanding the intricate motions and conformational changes that govern biological processes remains a fascinating and challenging endeavor. The research presented in this thesis aims to elucidate the dynamic processes underlying biological functions, specifically focusing on the dynamics of pentameric ligand-gated ion channels (pLGICs), which play a crucial role in signal transduction within the brain. READ MORE

7. 5. Elucidating the Gating Mechanism of Cys-Loop Receptors

   Author : Özge Yoluk; Erik Lindahl; Philip Biggin; KTH; []
   Keywords : NATURVETENSKAP; NATURAL SCIENCES; ion channel; gating; simulation; molecular dynamics; receptor; cys-loop; modelling; Teoretisk kemi och biologi; Theoretical Chemistry and Biology; Biological Physics; Biologisk fysik;

   Abstract : Cys-loop receptors are membrane proteins that are key players for the fast synaptic neurotransmission. Their ion transport initiates new nerve signals after activation by small agonist molecules, but this function is also highly sensitive to allosteric modulation by a number of compounds such as anesthetics, alcohol or anti-parasitic agents. READ MORE