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Turning G proteins on and off using peptide ligands

Academic Article
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Overview

authors

  • Ja, William
  • Wiser, O.
  • Austin, R. J.
  • Jan, L. Y.
  • Roberts, R. W.

publication date

  • 2006

journal

  • ACS Chemical Biology  Journal

abstract

  • Intracellular Galpha subunits represent potential therapeutic targets for a number of diseases. Here we describe three classes of new molecules that modulate G protein signaling by direct targeting of Galpha. Using messenger RNA display, we have identified unique peptide sequences that bind Galpha i1 . Functionally, individual peptides were found that either enhance or repress basal levels of G protein-activated inwardly rectifying potassium (GIRK) channel signaling, a downstream effector of G protein activation, indicating that the peptides directly turn G proteins on or off in vivo . A third functional class acts as a signaling attenuator; basal GIRK channel activity is unaffected but responses to repeated G protein activation are reduced. These data demonstrate that G protein-directed ligands can achieve physiological effects similar to those resulting from classical receptor targeting and may serve as leads for developing new classes of therapeutics.

subject areas

  • Amino Acid Sequence
  • Biochemistry
  • Cell Line
  • DNA, Complementary
  • Electrophysiology
  • G Protein-Coupled Inwardly-Rectifying Potassium Channels
  • GTP-Binding Proteins
  • Gene Expression Regulation
  • Humans
  • Immunoprecipitation
  • Ligands
  • Molecular Sequence Data
  • Peptides
  • Sequence Homology, Amino Acid
  • Signal Transduction
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Identity

PubMed Central ID

  • PMC2802464

International Standard Serial Number (ISSN)

  • 1554-8929

Digital Object Identifier (DOI)

  • 10.1021/cb600345k

PubMed ID

  • 17168552
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Additional Document Info

start page

  • 570

end page

  • 574

volume

  • 1

issue

  • 9

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