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Transducer Mechanism: G Protein–Coupled Receptors01:30

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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
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Some receptors remain unoccupied even when an agonist produces a maximal response. Such empty ones are called spare receptors. In presence of spare receptors the maximum effect of an agonist drug is achieved with fewer than 100% of the receptors being occupied. To determine the presence of spare receptors, scientists often compare the concentration of the drug needed to produce 50% of the maximum effect (EC50) with the concentration of the drug needed to occupy 50% of the receptors (Kd). If the...
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Cell-surface receptors, also known as transmembrane receptors, are cell surface, membrane-anchored (integral) proteins that bind to external ligand molecules. This type of receptor spans the plasma membrane and performs signal transduction, converting an extracellular signal into an intracellular signal. Ligands that interact with cell-surface receptors do not have to enter the cell that they affect. Cell-surface receptors are also called cell-specific proteins or markers because they are...
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G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
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在任何场合都能接受

Darrell J Irvine1

  • 1David H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, USA; Department of Biological Engineering, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, USA; Department of Materials Science & Engineering, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, USA; The Ragon Institute of MGH, Massachusetts Institute of Technology and Harvard University, 400 Technology Square, Cambridge, Massachusetts 02139, USA; Center for HIV/AIDS Vaccine Immunology and Immunogen Discovery, La Jolla, CA 92037, USA; Howard Hughes Medical Institute, Chevy Chase, Maryland 20815, USA.

Cell
|February 13, 2016
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概括

科学家们设计了合成的Notch受体来控制细胞信号. 这一突破允许在各种细胞类型中独立管理细胞输入和输出.

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科学领域:

  • 细胞生物学
  • 合成生物学
  • 生物技术

背景情况:

  • 细胞表面受体介导细胞与环境之间的通信.
  • 具有可控制的输入和输出独立于自然细胞通路的工程受体仍然是一个重大挑战.

研究的目的:

  • 开发一种用于细胞表面受体的新系统.
  • 实现对工程接收器输入和输出的独立控制.

主要方法:

  • 使用合成的Notch受体作为工程系统的基础.
  • 在不同类型的细胞中证明了系统的功能.

主要成果:

  • 成功创建了一个允许独立控制受体输入和输出的系统.
  • 设计的受体与内源信号通路的直角运作.

结论:

  • 研发的合成Notch受体系统提供了精确控制细胞功能的强大工具.
  • 这项技术对基于细胞的疗法和合成生物学应用具有广泛的影响.