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Structure of an agonist-bound human A₂A adenosine receptor

Academic Article
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Overview

related to degree

  • Wu, Huixian, Ph.D. in Chemistry, Scripps Research 2010 - 2014
  • Xu, Fei, Ph.D. in Biophysics, Scripps Research 2006 - 2011

authors

  • Xu, Fei
  • Wu, Huixian
  • Katritch, Vsevolod
  • Han, G. W.
  • Jacobson, K. A.
  • Gao, Z. G.
  • Cherezov, Vadim
  • Stevens, Raymond

publication date

  • April 2011

journal

  • Science  Journal

abstract

  • Activation of G protein-coupled receptors upon agonist binding is a critical step in the signaling cascade for this family of cell surface proteins. We report the crystal structure of the A(2A) adenosine receptor (A(2A)AR) bound to an agonist UK-432097 at 2.7 angstrom resolution. Relative to inactive, antagonist-bound A(2A)AR, the agonist-bound structure displays an outward tilt and rotation of the cytoplasmic half of helix VI, a movement of helix V, and an axial shift of helix III, resembling the changes associated with the active-state opsin structure. Additionally, a seesaw movement of helix VII and a shift of extracellular loop 3 are likely specific to A(2A)AR and its ligand. The results define the molecule UK-432097 as a "conformationally selective agonist" capable of receptor stabilization in a specific active-state configuration.

subject areas

  • Adenosine
  • Adenosine A2 Receptor Agonists
  • Binding Sites
  • Crystallography, X-Ray
  • Humans
  • Hydrogen Bonding
  • Ligands
  • Models, Molecular
  • Opsins
  • Protein Conformation
  • Protein Structure, Secondary
  • Receptor, Adenosine A2A
  • Rhodopsin
  • Triazines
  • Triazoles
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Identity

PubMed Central ID

  • PMC3086811

International Standard Serial Number (ISSN)

  • 0036-8075

Digital Object Identifier (DOI)

  • 10.1126/science.1202793

PubMed ID

  • 21393508
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Additional Document Info

start page

  • 322

end page

  • 327

volume

  • 332

issue

  • 6027

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