Membrane Potentials Regulating GPCRs: Insights From Experiments and Molecular Dynamics Simulation

Owen Vickery, Jan-Philipp Machtens, Ulrich Zachariae (Lead / Corresponding author)

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18 Citations (Scopus)
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Abstract

G-protein coupled receptors (GPCRs) form the largest class of membrane pro-teins in humans and are targeted by most present drugs. Membrane potential is one of the defining characteristics of living cells. Recent work has shown that the membrane voltage, and changes thereof, modulates signal transduction and ligand binding in GPCRs. As it may allow differential signalling patterns depending on tissue, cell type, and the excitation status of excitable cells, GPCR voltage sen-sitivity could have important implications for their pharmacology. This review summarises recent experimental insights on GPCR voltage regulation and the role of molecular dynamics simulations in identifying the structural basis of GPCR voltage-sensing. We discuss the potential significance for drug design on GPCR targets from excitable and non-excitable cells.
Original languageEnglish
Pages (from-to)44-50
Number of pages7
JournalCurrent Opinion in Pharmacology
Volume30
Early online date27 Jul 2016
DOIs
Publication statusPublished - Oct 2016

Keywords

  • gating charge
  • biomolecular simulation
  • membrane voltage
  • signal transduction
  • membrane surface receptors

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