Journal Article FZJ-2017-05147

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Membrane potentials regulating GPCRs: insights from experiments and molecular dynamics simulations

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2016
Elsevier Science Amsterdam [u.a.]

Current opinion in pharmacology 30, 44 - 50 () [10.1016/j.coph.2016.06.011]

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Abstract: G-protein coupled receptors (GPCRs) form the largest class of membrane proteins in humans and the targets of 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 sensitivity 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.

Classification:

Contributing Institute(s):
  1. Zelluläre Biophysik (ICS-4)
Research Program(s):
  1. 551 - Functional Macromolecules and Complexes (POF3-551) (POF3-551)

Appears in the scientific report 2017
Database coverage:
Medline ; Creative Commons Attribution CC BY 4.0 ; OpenAccess ; BIOSIS Previews ; BIOSIS Reviews Reports And Meetings ; Ebsco Academic Search ; IF < 5 ; JCR ; NCBI Molecular Biology Database ; SCOPUS ; Science Citation Index Expanded ; Thomson Reuters Master Journal List ; Web of Science Core Collection
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Document types > Articles > Journal Article
Institute Collections > IBI > IBI-1
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ICS > ICS-4
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Open Access

 Record created 2017-07-25, last modified 2021-01-29