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G Protein Coupled Receptors – Exploiting Flexible Conformations
European Pharmaceutical review (2012)
  • Kathryn L Chapman, Dr
  • John BC Findlay, Prof, National University of Ireland, Maynooth
  • Gemma K Kinsella, Dr, Dublin Institute of Technology

G-protein coupled receptors (GPCRs) are a diverse super-family of proteins located within the plasma membrane of eukaryotic cells which have a common architecture consisting of seven-transmembrane (7-TM) segments, connected by extracellular (ECL) and intracellular (ICL) loops. They differ from other 7-TM proteins in their ability to activate guanine-nucleotide binding proteins or β-arrestin and so initiate a signalling cascade. They have a wide range of physiological roles and provide many successful drug targets, playing a role in disorders including allergies, cardiovascular dysfunction, depression, obesity, cancer, pain, diabetes and a variety of central nervous system conditions1-3. This review will give a general overview of GPCRs and how their structures and activities can be used in drug discovery.

Publication Date
Fall September 3, 2012
Citation Information
Kathryn L Chapman, John BC Findlay and Gemma K Kinsella. "G Protein Coupled Receptors – Exploiting Flexible Conformations" European Pharmaceutical review (2012)
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