Analysis of G Protein and β-Arrestin Activation in Chemokine Receptors Signaling

Alessandro Vacchini, Marta Busnelli, Bice Chini, Massimo Locati, Elena Monica Borroni

Research output: Chapter in Book/Report/Conference proceedingChapter

Abstract

Chemokines are key regulators of leukocyte migration and play fundamental roles in immune responses. The chemokine system includes a set of over 40 ligands which engage in a promiscuous fashion a panel of over 25 receptors belonging to a distinct family of 7 transmembrane-domain receptors (7TM) widely expressed on a variety of cells. Although responses evoked by chemokine receptors have long been considered the result of balanced activation of the G protein- and β-arrestin-dependent signaling modules, evidence is accumulating showing that these receptors are capable, as other 7TMs, to activate different signaling modules in a ligand- and cell/tissue-specific manner. This biased signaling, or functional selectivity, confers a hitherto largely uncharacterized level of complexity to the chemokine system and challenges our present understanding of its redundancy. At the same time, it also provides new insights of relevance for chemokine receptors targeting drug development plans. Here, we provide current methods to study biased signaling of chemokine receptors by dissecting G proteins and β-arrestins activation upon chemokine stimulation.

Original languageEnglish
Title of host publicationMethods in Enzymology
PublisherAcademic Press Inc.
Pages421-440
Number of pages20
Volume570
DOIs
Publication statusPublished - 2016

Publication series

NameMethods in Enzymology
Volume570
ISSN (Print)00766879
ISSN (Electronic)15577988

Keywords

  • Biased signaling
  • Chemokine
  • Chemokine receptors
  • G proteins
  • β-Arrestins

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology

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