NMR Studies of Function-related Conformational Equilibria of GPCRs

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  • UEDA Takumi
    Graduate School of Pharmaceutical Sciences, The University of Tokyo
  • SHIMADA Ichio
    Graduate School of Pharmaceutical Sciences, The University of Tokyo

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  • NMRを用いたG蛋白質共役型受容体の機能制御メカニズムの解析
  • NMR オ モチイタ G タンパクシツ キョウヤクガタ ジュヨウタイ ノ キノウ セイギョ メカニズム ノ カイセキ

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Abstract

<p>GPCRs function as receptors for various neurotransmitters and hormones, and >30% of current drugs target GPCRs. Although substantial number of GPCR crystal structures have become available, information about GPCR features can only be partially derived from the crystallography data. NMR methods provide information about dynamics of GPCRs over a wide range of frequencies in aqueous media at near-physiological temperature, with minimal modification of the wild-type GPCR covalent structures. Here we review our recent NMR studies of the function-related conformational equilibria of GPCRs, including β2 adrenergic receptor and μ opioid receptor.</p>

Journal

  • Seibutsu Butsuri

    Seibutsu Butsuri 59 (4), 181-187, 2019

    The Biophysical Society of Japan General Incorporated Association

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