Ion channel regulation by G proteins

Kevin D Wickman, David E. Clapham

Research output: Contribution to journalArticle

327 Citations (Scopus)

Abstract

Ion channels are poised uniquely to initiate, mediate, or regulate such distinct cellular activities as action potential propagation, secretion, and gene transcription. In retrospect, it is not surprising that studies of ion channels have revealed considerable diversities in their primary structures, regulation, and expression. From a functional standpoint, the various mechanisms coopted by cells to regulate channel activity are particularly fascinating. Extracellular ligands, membrane potential, phosphorylation, ions themselves, and diffusible second messengers are all well-established regulators of ion channel activity. Heterotrimeric GTP-binding proteins (G proteins) mediate many of these types of ion channel regulation by stimulating or inhibiting phosphorylation pathways, initiating intracellular cascades leading to elevation of cytosolic Ca2+ or adenosine 3',5'-cyclic monophosphate levels, or by generating various lipid-derived compounds. In some cases, it seems that activated G protein subunits can interact directly with ion channels to elicit regulation. Although there is currently little direct biochemical evidence to support such a mechanism, it is the working hypothesis for the most-studied G protein-regulated ion channels.

Original languageEnglish (US)
Pages (from-to)865-885
Number of pages21
JournalPhysiological Reviews
Volume75
Issue number4
DOIs
StatePublished - Jan 1 1995
Externally publishedYes

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Ion Channels
GTP-Binding Proteins
Phosphorylation
Heterotrimeric GTP-Binding Proteins
Protein Subunits
Second Messenger Systems
Cyclic AMP
Membrane Potentials
Action Potentials
Ions
Ligands
Lipids
Genes

Cite this

Ion channel regulation by G proteins. / Wickman, Kevin D; Clapham, David E.

In: Physiological Reviews, Vol. 75, No. 4, 01.01.1995, p. 865-885.

Research output: Contribution to journalArticle

Wickman, Kevin D ; Clapham, David E. / Ion channel regulation by G proteins. In: Physiological Reviews. 1995 ; Vol. 75, No. 4. pp. 865-885.
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