Vibrational spectroscopy analysis of ligand efficacy in human M₂ muscarinic acetylcholine receptor (M₂R)

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  • 片山, 耕大
    Department of Life Science and Applied Chemistry, Nagoya Institute of Technology; OptoBioTechnology Research Center, Nagoya Institute of Technology; PRESTO, Japan Science and Technology Agency
  • 魲, 洸平
    Department of Life Science and Applied Chemistry, Nagoya Institute of Technology
  • 寿野, 良二
    Department of Medical Chemistry, Kansai Medical University
  • 木瀬, 亮次
    Graduate School of Pharmaceutical Sciences, Tohoku University
  • 辻本, 浩一
    Department of Cell Biology and Medical Chemistry, Graduate School of Medicine, Kyoto University
  • 岩田, 想
    Department of Cell Biology and Medical Chemistry, Graduate School of Medicine, Kyoto University
  • 井上, 飛鳥
    Graduate School of Pharmaceutical Sciences, Tohoku University
  • 小林, 拓也
    Department of Medical Chemistry, Kansai Medical University; Japan Agency for Medical Research and Development, Core Research for Evolutional Science and Technology (AMED-CREST)
  • 神取, 秀樹
    Department of Life Science and Applied Chemistry, Nagoya Institute of Technology; OptoBioTechnology Research Center, Nagoya Institute of Technology

説明

The intrinsic efficacy of ligand binding to G protein-coupled receptors (GPCRs) reflects the ability of the ligand to differentially activate its receptor to cause a physiological effect. Here we use attenuated total reflection-Fourier transform infrared (ATR-FTIR) spectroscopy to examine the ligand-dependent conformational changes in the human M₂ muscarinic acetylcholine receptor (M₂R)). We show that different ligands affect conformational alteration appearing at the C=O stretch of amide-I band in M2R. Notably, ATR-FTIR signals strongly correlated with G-protein activation levels in cells. Together, we propose that amide-I band serves as an infrared probe to distinguish the ligand efficacy in M₂R) and paves the path to rationally design ligands with varied efficacy towards the target GPCR.

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