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相关概念视频

Types of Receptors: Internal Receptors01:07

Types of Receptors: Internal Receptors

25.5K
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.
70.3K
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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Adrenergic Receptors: ɑ Subtype01:31

Adrenergic Receptors: ɑ Subtype

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Adrenoceptors are classified into α and ꞵ classes based on their potencies to catecholamine agonists. α-adrenoceptors show the following order of catecholamine potency:
Adrenaline ≥ Noradrenaline >> Isoprenaline
α-adrenoceptors are further divided into α1 and α2-adrenoceptors.
α1-Adrenoceptors: These receptors are located postsynaptically on the effector organs and cause constriction of smooth muscle mediated by activation of phospholipase...
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Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

1.4K
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:
1.4K
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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Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay
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雄激素受体 雄激素受体

Greg Van-Duyne1, Ian A Blair2, Cynthia Sprenger3

  • 1Department of Biophysics & Biochemistry, Perelman School of Medicine University of Pennsylvania, Philadelphia, PA, United States.

Vitamins and hormones
|September 17, 2023
PubMed
概括

雄激素受体 (AR) 调节男性性激素功能,是药物点. 了解AR信号的进步,包括其蛋白质形式和抵抗机制,提供了新的治疗策略.

关键词:
激进主义者的激进主义者阿尔多 - 基托减少酶.这里是Allostery.敌对者的敌对者共同监管机构 共同监管机构低温电子显微镜的使用方法质谱测量质量谱测量后翻译修改后的修改.前列腺癌是什么意思 前列腺癌是什么意思针对蛋白质溶解的木乃伊.选择性雄激素受体调节器 选择性雄激素受体调节器拼接的变种 拼接的变种类固醇5α-减少酶的使用.

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Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
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Prostate Organoid Cultures as Tools to Translate Genotypes and Mutational Profiles to Pharmacological Responses
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科学领域:

  • 分子内分泌学分子内分泌学
  • 信号通道的信号通道
  • 核受体超级家族 核受体超级家族

背景情况:

  • 雄激素受体 (AR) 是男性性发育和功能的关键转录因子.
  • AR与内源性配体表现出悖论性效应,并与其他核受体共享反应元素,造成复杂性.
  • 全长AR (AR-FL) 的高分辨率结构数据由于N端域 (NTD) 失序而具有挑战性.

研究的目的:

  • 审查最近在理解雄激素受体 (AR) 信号通路方面的进展.
  • 通过翻译后修饰和蛋白形来探索AR功能的调节.
  • 在前列腺癌等疾病中讨论与AR相关的治疗策略和抵抗机制.

主要方法:

  • 关于雄激素受体 (AR) 结构,功能和信号传导的当前文献的综述.
  • 对翻译后修改及其对AR蛋白质形式的影响的分析.
  • 检查耐药性机制和潜在的治疗干预措施.

主要成果:

  • AR功能是由各种由翻译后修改产生的蛋白质形式调节的.
  • 多蛋白质复合体内的相互作用决定了AR的转录输出.
  • 前列腺癌的耐药性与AR上调和LBD缺乏的拼接变体有关.

结论:

  • 用选择性雄激素受体调节剂 (SARMS) 或对抗剂向AR是治疗AR驱动疾病的关键.
  • 像双极性T治疗和NTD-对抗剂这样的新策略在克服AR药物耐药性方面显示出希望.
  • 对AR信号复杂性的进一步研究对于开发更有效的疗法至关重要.