Conductance of P2X<sub>4</sub>purinergic receptor is determined by conformational equilibrium in the transmembrane region

DOI Web Site PubMed 被引用文献11件 参考文献50件 オープンアクセス
  • Yuichi Minato
    Graduate School of Pharmaceutical Sciences, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan;
  • Shiho Suzuki
    Graduate School of Pharmaceutical Sciences, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan;
  • Tomoaki Hara
    Graduate School of Pharmaceutical Sciences, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan;
  • Yutaka Kofuku
    Graduate School of Pharmaceutical Sciences, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan;
  • Go Kasuya
    Department of Biological Sciences, Graduate School of Science, The University of Tokyo, Bunkyo-ku, Tokyo 113-0033, Japan;
  • Yuichiro Fujiwara
    Department of Physiology, Graduate School of Medicine, Osaka University, 2-2 Yamadaoka, Suita, Osaka 565-0871, Japan;
  • Shunsuke Igarashi
    Institute for Innovation, Ajinomoto, Kawasaki 210-8681, Japan;
  • Ei-ichiro Suzuki
    Institute for Innovation, Ajinomoto, Kawasaki 210-8681, Japan;
  • Osamu Nureki
    Department of Biological Sciences, Graduate School of Science, The University of Tokyo, Bunkyo-ku, Tokyo 113-0033, Japan;
  • Motoyuki Hattori
    State Key Laboratory of Genetic Engineering, Collaborative Innovation Center of Genetics and Development, Department of Physiology and Biophysics, School of Life Sciences, Fudan University, Yangpu District, Shanghai 200438, China;
  • Takumi Ueda
    Graduate School of Pharmaceutical Sciences, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan;
  • Ichio Shimada
    Graduate School of Pharmaceutical Sciences, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan;

書誌事項

公開日
2016-04-11
資源種別
journal article
DOI
  • 10.1073/pnas.1600519113
公開者
Proceedings of the National Academy of Sciences

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説明

<jats:title>Significance</jats:title><jats:p>Partial agonists of ligand-gated ion channels reportedly offer clinical advantages over antagonists and full agonists in antidepressant and smoking-cessation treatment. In the cases of P2X purinergic receptors, the currents evoked by α,β-methylene ATP are lower than the currents evoked by ATP. Here, our NMR analyses revealed that the transmembrane region and the membrane side of the lower body exist in conformational equilibrium between the closed and open conformations, with slower exchange rates than the chemical shift difference (<100 s<jats:sup>-1</jats:sup>), and that the small population of the open conformation of zebrafish P2X<jats:sub>4</jats:sub>purinergic receptor causes the partial activation in the α,β-methylene ATP-bound state. These findings provide insights into the mechanism underlying the partial activation of P2X<jats:sub>4</jats:sub>receptors and other ligand-gated ion channels.</jats:p>

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