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相关概念视频

Receptor Downregulation in MVBs01:15

Receptor Downregulation in MVBs

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Multivesicular bodies (MVBs) are mature endosomes that sort ubiquitinated proteins and then fuse with lysosomes to degrade the sorted proteins. Epidermal growth factor (EGF) and its receptor (EGFR) form a complex that can be internalized through endocytosis, sorted into an MVB, and later degraded.
The EGFR can initiate signaling pathways that  lead to cell proliferation, migration, and differentiation. Overexpression of EGFR  stimulates cells to proliferate. Excessive  EGFR...
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G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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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.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
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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.
GPCRs are also called heptahelical,...
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Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

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Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
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Leaky Scanning02:28

Leaky Scanning

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During most eukaryotic translation processes, the small 40S ribosome subunit scans an mRNA from its 5' end until it encounters the first start AUG codon. The large 60S ribosomal subunit then joins the smaller one to initiate protein synthesis. The location of the translation initiation is largely determined by the nucleotides near the start codon as there may be multiple translation initiation sites present on the mRNA.  Marilyn Kozak discovered that the sequence RCCAUGG (where R...
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Diversity of Antigen Receptors01:28

Diversity of Antigen Receptors

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Antigen receptors are essential components of the immune system crucial in defending the body against foreign invaders. These receptors are present on the surface of B and T cells, enabling them to recognize antigens and mount an appropriate immune response.
Before encountering any antigen, lymphocytes express these receptors. On B cells, the antigen receptor is a membrane-bound antibody molecule called BCR; on T cells, it is a T cell receptor or TCR. B and T cell receptors are composed of two...
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相关实验视频

Updated: Jul 11, 2025

Visualizing Genetic Variants, Short Targets, and Point Mutations in the Morphological Tissue Context with an RNA In Situ Hybridization Assay
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Visualizing Genetic Variants, Short Targets, and Point Mutations in the Morphological Tissue Context with an RNA In Situ Hybridization Assay

Published on: August 14, 2018

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小心接收器变体的变种

Julien Hanson1

  • 1Laboratory of Molecular Pharmacology, GIGA-Molecular Biology of Diseases and Center for Interdisciplinary Research on Medicines (CIRM), University of Liège, Liège B-4000, Belgium.

Journal of medicinal chemistry
|November 17, 2023
PubMed
概括

与MAS相关的G蛋白结合受体 (MRGPRs) 是治疗疼痛和的关键药物标. 开发这些受体的选择性连接体,特别是灵长类特定的连接体,至关重要,但由于它们的孤儿性质,具有挑战性.

科学领域:

  • 神经科学是一个神经科学.
  • 药理学 药理学是指药理学的学科.
  • 遗传学 是一个遗传学.

背景情况:

  • 与MAS相关的G蛋白结合受体 (MRGPRs) 是一种复杂的家族,存在于感觉神经元中.
  • 大多数MRGPR是孤儿受体,缺乏已知的内源配体.
  • 这对它们的治疗发展构成了重大障碍.

研究的目的:

  • 突出MRGPRs作为药物点的治疗潜力.
  • 为MRGPR研究应对稀缺和非选择性配体的挑战.
  • 为了强调对强大的配体的需求,特别是针对灵长类动物特有的MRGPRX亚家族.

主要方法:

  • 摘要中没有说明研究中使用的方法.
  • 该研究的重点是MRGPRs的表征和潜力.
  • 联结体的发现和验证被暗示为研究的关键领域.

主要成果:

  • MRGPRs显示出作为和恶感等疾病的药物点的巨大潜力.
  • 缺乏强效和选择性的配体阻碍了MRGPRs的研究和治疗应用.
  • 灵长类动物特有的MRGPRX亚家族特别受到连接物稀缺的影响.

更多相关视频

Determining the Likelihood of Variant Pathogenicity Using Amino Acid-level Signal-to-Noise Analysis of Genetic Variation
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Determining the Likelihood of Variant Pathogenicity Using Amino Acid-level Signal-to-Noise Analysis of Genetic Variation

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Screening for Functional Non-coding Genetic Variants Using Electrophoretic Mobility Shift Assay EMSA and DNA-affinity Precipitation Assay DAPA
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Screening for Functional Non-coding Genetic Variants Using Electrophoretic Mobility Shift Assay EMSA and DNA-affinity Precipitation Assay DAPA

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相关实验视频

Last Updated: Jul 11, 2025

Visualizing Genetic Variants, Short Targets, and Point Mutations in the Morphological Tissue Context with an RNA In Situ Hybridization Assay
10:57

Visualizing Genetic Variants, Short Targets, and Point Mutations in the Morphological Tissue Context with an RNA In Situ Hybridization Assay

Published on: August 14, 2018

10.7K
Determining the Likelihood of Variant Pathogenicity Using Amino Acid-level Signal-to-Noise Analysis of Genetic Variation
07:15

Determining the Likelihood of Variant Pathogenicity Using Amino Acid-level Signal-to-Noise Analysis of Genetic Variation

Published on: January 16, 2019

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Screening for Functional Non-coding Genetic Variants Using Electrophoretic Mobility Shift Assay EMSA and DNA-affinity Precipitation Assay DAPA
11:35

Screening for Functional Non-coding Genetic Variants Using Electrophoretic Mobility Shift Assay EMSA and DNA-affinity Precipitation Assay DAPA

Published on: August 21, 2016

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结论:

  • 克服连接体稀缺性对于释放MRGPRs治疗潜力至关重要.
  • 对开发选择性配体的进一步研究对于推进基于MRGPR的疗法至关重要.
  • 针对MRGPRs,特别是灵长类特异性的MRGPRs,为治疗感官神经元疾病提供了有前途的途径.