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首页> 外文期刊>Neuron >Allosteric Modulation of GPCRs: New Insights and Potential Utility for Treatment of Schizophrenia and Other CNS Disorders
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Allosteric Modulation of GPCRs: New Insights and Potential Utility for Treatment of Schizophrenia and Other CNS Disorders

机译：GPCR的变构调制：用于治疗精神分裂症和其他CNS疾病的新见解和潜在效用

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摘要

G-protein-coupled receptors (GPCRs) play critical roles in regulating brain function. Recent advances have greatly expanded our understanding of these receptors as complex signaling machines that can adopt numerous conformations and modulate multiple downstream signaling pathways. While agonists and antagonists have traditionally been pursued to target GPCRs, allosteric modulators provide several mechanistic advantages, including the ability to distinguish between closely related receptor subtypes. Recently, the discovery of allosteric ligands that confer bias and modulate some, but not all, of a given receptor's downstream signaling pathways can provide pharmacological modulation of brain circuitry with remarkable precision. In addition, allosteric modulators with unprecedented specificity have been developed that can differentiate between subpopulations of a given receptor subtype based on the receptor's dimerization state. These advances are not only providing insight into the biological roles of specific receptor populations, but hold great promise for treating numerous CNS disorders.
机译：G蛋白偶联受体（GPCR）在调节脑功能方面发挥着关键作用。最近的进展极大地扩展了我们对这些受体的理解，作为可以采用多种构象的复杂信号机并调制多个下游信号通路。虽然传统上是追查GPCR的激动剂和拮抗剂，但颠覆调节剂提供了几种机制优势，包括区分密切相关的受体亚型的能力。最近，发现赋予偏置和调节一些但不是全部，给定受体的下游信号传导途径的颠覆配体的发现可以提供脑电路的药理调制，具有显着的精度。此外，已经开发出具有前所未有的特异性的变构调节剂，其可以在基于受体的二聚化状态的给定受体亚型的亚型之间分化。这些进步不仅提供了对特定受体人群的生物学作用的洞察力，而且对治疗众多CNS疾病具有很大的希望。

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  • 来源
    《Neuron》 |2017年第3期|共16页
  • 作者

    Foster Daniel J.; Conn P. Jeffrey;

  • 作者单位

    Vanderbilt Univ Dept Pharmacol Nashville TN 37232 USA;

    Vanderbilt Univ Dept Pharmacol Nashville TN 37232 USA;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 神经病学;
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