Transcript G Protein Coupled Receptors - Centre for Molecular and

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
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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