相关实验视频
Updated: Feb 2, 2026

05:05
Preparation of High-Temperature Sample Grids for Cryo-EM
Published on: July 26, 2021
4.3K
低温EM显示了两个完全长度的5-HT3A受体的不同类型
Sandip Basak1, Yvonne Gicheru1, Shanlin Rao2
1Department of Physiology and Biophysics, Case Western Reserve University, Cleveland, OH, USA.
Nature
|November 8, 2018
概括
5-HT3A 血清素受体是抗恶心药物的点,在血清素结合时会发生形状变化. 这些结构变化激活了道,揭示了新的离子透途径.
科学领域:
- 神经科学
- 结构生物学
- 药理学
背景情况:
- 5-HT3A 血清素受体是化疗和放射治疗中使用的抗药的主要点.
- 了解受体在配体结合时的构造变化对于其功能调节至关重要.
研究的目的:
- 阐明5-HT3A受体被胺激活的分子机制.
- 提供高分辨率的结构洞察到受体的独特形状.
主要方法:
- 在3.32 Å和3.89 Å分辨率下,全长5-HT3A受体的X射线晶体学.
- 分子动力学模拟来补充结构数据.
主要成果:
- 确定了两种不同的5-HT3A受体与血清素结合.
- 在细胞外和膜外域中诱导显著的扭曲运动.
- 一个165 Å的透通道被打开,在TMD-ICD接口上有新的侧面门户.
结论:
- 这项研究揭示了通过全域形状变化激活5-HT3A受体通道的机制.
- 发现了新的侧门,为离子透和功能调节提供了新的见解.
- 结构数据为合理设计向治疗提供了基础.
相关概念视频
Drugs Affecting GI Tract Motility: Serotonin Receptor Agonists
985
Serotonin, a crucial neurotransmitter synthesized by enterochromaffin cells, plays a cardinal role in regulating gastrointestinal (GI) motility. With over 90% of the body's total serotonin in the GI tract, its influence on digestive processes is profound. Serotonin is swiftly released upon various stimuli, such as food boluses or certain drugs, triggering intrinsic sensory neurons in the myenteric plexus and extrinsic vagal and spinal sensory neurons. This leads to the activation of the...
985
Conformity
48.2K
Conformity is the change in a person’s behavior to go along with the group, even if that person does not agree with the group.
48.2K
Internal Receptors
74.7K
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.
74.7K
Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists
668
5-HT3 receptor antagonists, such as dolasetron, granisetron (Kytril), ondansetron (Zofran), and palonosetron (Axoli), are crucial in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. These drugs selectively block 5-HT3 receptors in the visceral vagal and spinal afferent nerves, chemoreceptor trigger zone, and the vomiting center. They have a rapid onset of action and can be given as a single dose before chemotherapy. Ondansetron and granisetron, in particular,...
668
Receptor-mediated Endocytosis
110.9K
Overview
110.9K
Conformations of Butane
18.1K
Unlike ethane and propane that have only two major conformations, butane has more than two conformers. The staggered form of butane in which the bulky methyl groups on the two carbons are placed on opposite sides, that is, at a dihedral angle of 180°, is the lowest energy, most stable form — called the anti conformer. This conformation is stabilized due to the absence of steric repulsion between the largely spaced out methyl groups. The other two staggered conformations are...
18.1K

