A constitutively activating mutation alters the dynamics and energetics of a key conformational change in a ligand-free G protein-coupled receptor

Hisao Tsukamoto, David Farrens

Research output: Contribution to journalArticle

23 Citations (Scopus)

Abstract

Background: Constitutively active mutations (CAMs) affect the dynamics of G protein-coupled receptors (GPCRs), through undefined mechanisms. Results: Site-directed fluorescence labeling (SDFL) studies find a CAM (M257Y) alters the dynamics of the GPCR ligand-free opsin. Conclusion: The M257Y CAM alters the dynamics of the conversion between active and inactive opsin conformations. Significance: SDFL can be used to gain insights into how CAMs affect the dynamics of G protein-coupled receptors.

Original languageEnglish (US)
Pages (from-to)28207-28216
Number of pages10
JournalJournal of Biological Chemistry
Volume288
Issue number39
DOIs
StatePublished - Sep 27 2013

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G-Protein-Coupled Receptors
Ligands
Opsins
Mutation
Labeling
Fluorescence
Conformations

ASJC Scopus subject areas

  • Biochemistry
  • Cell Biology
  • Molecular Biology

Cite this

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AB - Background: Constitutively active mutations (CAMs) affect the dynamics of G protein-coupled receptors (GPCRs), through undefined mechanisms. Results: Site-directed fluorescence labeling (SDFL) studies find a CAM (M257Y) alters the dynamics of the GPCR ligand-free opsin. Conclusion: The M257Y CAM alters the dynamics of the conversion between active and inactive opsin conformations. Significance: SDFL can be used to gain insights into how CAMs affect the dynamics of G protein-coupled receptors.

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