Akademik Veri Yönetim Sistemi
6th International Drug Design Congress, İstanbul, Türkiye, 13 - 15 Aralık 2018
G protein-coupled receptors (GPCRs) are membrane proteins that mediate physiological
response to a diverse array of stimuli. In humans, they mediate the action of hundreds of
peptide hormones, sensory stimuli, odorants, neurotransmitters, and chemokines. GPCRs also
are targets for ~40% of all currently marketed pharmaceuticals. These receptors traditionally
been thought to act as monomeric units. However, recent evidence suggests that GPCRs may
form dimers as part of their normal trafficking and function. While the formation of GPCR
dimers/oligomers have been reported to play important roles in regulating receptor
expression, ligand binding, and second messenger activation, less is known about how GPCR
dimers interact with other proteins such as G-proteins and Arrestin.
We are interested in studiying the interactions between GPCRs and effect of this dimerization
on G-protein dimerization. Our group also focus on the mechanisms of receptor-arrestin
binding in live cells using Föster resonance energy transfer (FRET) and bimolecular
fluorescence complementation (BiFC) assays. We designed and developed tagged receptors,
G-proteins and Arrestin proteins using Green florescent protein variants that can be used in
imaging studies. These constructs are suitable for testing drug candidates and/or analyze
protein-protein interfaces for GPCRs or G-protein dimers.