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PRESENTS G Protein Coupled Receptors produced by Tim Hulsen & David Lutje Hulsik G Protein Coupled Receptors • seven transmembrane regions • hydrophobic/ hydrophilic domains • conserved residues and motifs (i.e. NPXXY) Rhodopsin with conserved residues GPCR-G protein coupling Schematic drawing of the flow of events in G protein activation. The process starts when the Arg of the DRY motif moves toward the cytosol. The signal moves `through' helix 5 to the nucleotide binding site. The GDP– GTP exchange leads to a conformational change in the switch region. This leads to dissociation of Gß and it destabilizes the region where the G protein N- and Cterminus come together with the GPCR C-terminus, which leads to G protein dissociation. • receptor gets activated by agonist • G protein binds to activated receptor • Agonist binding to receptor becomes stronger upon G protein coupling • GDP is released • G protein takes up GTP • GTP uptake triggers release of G protein from receptor Studies on GPCRs • • • • • • mutation studies spinlabel NMR cystein scanning protease studies photoaffinity Our Goals • to determine whether available data is correct • to combine research already done on GPCRs • using data from different sources to investigate GPCRs Current Activities • working with What-If • reading a lot of articles • searching for GPCRs on the web • website building • “programming” • deathmatching • superpositioning • alignment between Rhodopsin and Bacteriorhodopsin GPCR Website http://go.to/gpcr The End Fin Ende Einde Albert Verlinde Technical SetProducer Casting Decoration Director assistant David Lutje Hulsik Tim Hulsen David Mike Wim Tim GertLutje Meijnhard Hulsen Janssen Vriend Tim Hulsik Hulsen ©2000, Tim Hulsen & David Lutje Hulsik