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相关概念视频

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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Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

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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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Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

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Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
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Intracellular Hormone Receptors01:08

Intracellular Hormone Receptors

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Lipid-soluble hormones diffuse across the plasma and nuclear membrane of target cells to bind to their specific intracellular receptors. These receptors act as transcription factors that regulate gene expression and protein synthesis in the target cell
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Types of Receptors: Internal Receptors01:07

Types of Receptors: Internal Receptors

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Many cellular signals are hydrophilic and cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind intracellular receptors that reside within the cell cytoplasm or nucleus. Many mammalian steroid hormones and nitric oxide (NO) gas use this cell signaling mechanism.
Similar to membrane-bound receptors, the binding of a ligand to the intracellular receptor of causes a conformational change in the...
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Internal Receptors01:31

Internal Receptors

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Many cellular signals are hydrophilic and therefore cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind to internal, or intracellular, receptors that reside within the cell. Many mammalian steroid hormones use this mechanism of cell signaling, as does nitric oxide (NO) gas.
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Biochemical Reconstitution of Steroid Receptor•Hsp90 Protein Complexes and Reactivation of Ligand Binding
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人类的葡萄糖皮质体受体.

Nicolas C Nicolaides1, George P Chrousos1

  • 1Division of Endocrinology, Metabolism and Diabetes, First Department of Pediatrics, National and Kapodistrian University of Athens Medical School, 'Aghia Sophia' Children's Hospital, Athens, Greece; Division of Endocrinology and Metabolism, Center of Clinical, Experimental Surgery and Translational Research, Biomedical Research Foundation of the Academy of Athens, Athens, Greece; University Research Institute of Maternal and Child Health and Precision Medicine and UNESCO Chair on Adolescent Health Care, National and Kapodistrian University of Athens Medical School, Athens, Greece.

Vitamins and hormones
|September 17, 2023
PubMed
概括

葡萄糖皮质激素,由下丘脑-垂体-上腺 (HPA) 轴和昼夜节律调节,是关键的类固醇激素. 本综述详细介绍了人类葡萄糖皮质体受体 (GR),其结构,功能和健康和疾病中的信号.

关键词:
克鲁索斯综合征是什么 克鲁索斯综合征葡萄糖皮质体受体异型.葡萄糖皮质类药物是什么人类葡萄糖皮质类受体受体发生NR3C1基因突变的基因突变在NR3C1基因多态化中.

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科学领域:

  • 内分泌学 在内分泌学.
  • 分子生物学分子生物学
  • 遗传学 是一个遗传学.

背景情况:

  • 葡萄糖皮质激素是上腺皮质产生的类固醇激素.
  • 它们是生理功能的关键调节者,由下丘脑-垂体-上腺 (HPA) 轴和昼夜节律控制.
  • 葡萄糖皮质体通过与葡萄糖皮质体受体 (GR) 结合来发挥其作用.

研究的目的:

  • 总结关于人类葡萄糖皮质体受体 (GR) 的当前知识.
  • 为GR结构,表达,功能和信号提供洞察力.
  • 讨论GR在正常生理和病理条件中的作用.

主要方法:

  • 审查当前的科学文献.
  • 结合了来自细胞,分子和计算结构生物学的发现.
  • 考虑表观遗传机制.

主要成果:

  • 葡萄糖皮质体受体 (GR) 是一个无处不在的转录因子,影响着高达20%的哺乳动物基因组.
  • 对GR的分子机制的理解有了显著的进步.
  • 人们越来越认识到GR在各种生理和病理状态中的参与.

结论:

  • 人类的葡萄糖皮质体受体 (GR) 在调节基因转录和生理过程中发挥着核心作用.
  • 生物学和表观遗传学的进步提高了我们对GR信号的理解.
  • 这种知识对于理解和管理与葡萄糖皮质体功能相关的疾病至关重要.