Single-molecule Imaging of GPCRs: An Application to the Drug Evaluation and Pharmacology

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  • YANAGAWA Masataka
    Cellular Informatics Laboratory, RIKEN Cluster for Pioneering Research
  • SAKO Yasushi
    Cellular Informatics Laboratory, RIKEN Cluster for Pioneering Research

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  • Gタンパク質共役型受容体の生細胞1分子計測を薬効薬理評価に応用する
  • Gタンパクシツ キョウヤクガタ ジュヨウタイ ノ ナマ サイボウ 1 ブンシ ケイソク オ ヤッコウ ヤクリ ヒョウカ ニ オウヨウ スル

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Abstract

<p>G protein-coupled receptors (GPCRs) constitute one of the largest superfamily of proteins in the human genome. Since GPCRs are major drug targets, a pharmacological evaluation of compounds on a GPCR is an important process in drug discovery. Here, we review the past trends of the in cell single-molecule measurement of GPCRs, many of which were focused on dimerization of GPCRs. Then, we introduce our recent study regarding the drug evaluation based on a general feature of a diffusion-function relationship of GPCRs. We also discuss the future applicability of the present study in pharmacology and drug screening.</p>

Journal

  • Seibutsu Butsuri

    Seibutsu Butsuri 61 (6), 366-369, 2021

    The Biophysical Society of Japan General Incorporated Association

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