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Ligand-induced conformational changes in a SMALP-encapsulated GPCR.

Authors
  • Routledge, Sarah J.1
  • Jamshad, Mohammed2
  • Little, Haydn A.2
  • Lin, Yu-Pin2
  • Simms, John1
  • Thakker, Alpesh1
  • Spickett, Corinne M.1
  • Bill, Roslyn M.1
  • Dafforn, Tim R.2
  • Poyner, David R.1
  • Wheatley, Mark3, 4
  • 1 Life and Health Sciences, Aston University, Birmingham B4 7ET, UK
  • 2 School of Biosciences, University of Birmingham, Birmingham B15 2TT, UK
  • 3 Centre for Sport, Exercise and Life Sciences, Alison Gingell Building, Faculty of Health and Life Sciences, Coventry University, Coventry CV1 2DS, UK
  • 4 Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, UK
Type
Published Article
Journal
Biochimica et Biophysica Acta. Biomembranes
Publisher
Elsevier
Publication Date
Jun 01, 2020
Volume
1862
Issue
6
Identifiers
DOI: 10.1016/j.bbamem.2020.183235
PMID: 32126232
PMCID: PMC7156913
Source
PubMed Central
Keywords
License
Unknown

Abstract

• Conformational changes in the A2AR monitored in a nano-scale membrane disc (SMALP). • Profile of phospholipids in A2AR-SMALP similar to the plasma membrane. • A partially-active conformation of A2AR is supported in a SMALP. • Inverse agonist induced dose-dependent conformational transitions in A2AR-SMALP. • In contrast to inverse agonist, agonist induced only small conformational changes.

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