在Gloeobacter violaceus中确定布洛的结合部位 带离子通道
Elham Pirayesh1, Hoa Quynh Do1, Garren Ferreira1
1Medical Student Summer Research Program, School of Medicine, Texas Tech University Health Sciences Center, Lubbock, TX, 79430 USA.
bioRxiv : the preprint server for biology
|October 24, 2023
概括
布普罗抑制了联结离子通道. 研究人员在细菌通道同类物中确定了一个特定的结合部位,揭示了布洛.
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.
- 结构生物学 结构生物学
背景情况:
- 布普罗是一种抗抑郁药和戒烟辅助剂.
- 它影响神经递质载体和带离子通道 (pLGICs).
- 布鲁在PLGIC上确切的结合部位和机制尚不清楚.
研究的目的:
- 为了研究布洛普对PLGICs的抑制作用.
- 通过一种 prokaryotic 同类模型来识别布洛的结合部位.
主要方法:
- 检查了布洛在Gloeobacter violaceus联接离子通道 (GLIC) 中的抑制作用.
- 在GLIC中使用单氨基酸替代物.
- 采用了两电极电压记录.
主要成果:
- 布鲁抑制了GLIC电流,其强度为14.9 ± 2.0μM.
- 在M1跨膜段的残留物T214中确定了一个结合点.
- 这个部位涉及M1和M3中的残留物,类似于其他脂性分子结合部位.
结论:
- 布鲁在临床相关度下抑制GLIC.
- 这项研究阐明了PLGICs上布洛的特定结合部位.
- 这些发现有助于更好地了解布洛普里昂的作用机制和潜在的非目标效应.
更多相关视频
相关概念视频
Ligand-Gated Ion Channel Receptor: Gating Mechanism
2.3K
Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
2.3K
Ligand Binding and Linkage
4.8K
Allosteric proteins have more than one ligand binding site; the binding of a ligand to any of these sites influences the binding of ligands to the other sites. When a protein is allosteric, its binding sites are called coupled or linked. In the case of enzymes, the site that binds to the substrate is known as the active site and the other site is known as the regulatory site. When a ligand binds to the regulatory site, this leads to conformational changes in the protein that can influence...
4.8K
G-protein Coupled Receptors
120.0K
G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
120.0K
G-Protein Gated Ion Channels
4.6K
GPCRs are primarily responsible for our sense of smell, taste, and vision. The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory...
Sensory...
4.6K
Ligand-gated Ion Channels
12.4K
Ligand-gated ion channels are transmembrane proteins with a channel for ions to pass through and a binding site for a ligand. The channel opens only when a ligand attaches to the binding site.
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that...
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that...
12.4K
Ligand Binding Sites
12.9K
Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
12.9K


