The 5-HT3 receptor--the relationship between structure and function.
The 5-HT3 receptor--the relationship between structure and function.
复制标题
5-HT3受体 - 结构与功能之间的关系。
DOI：
10.1016/j.neuropharm.2008.08.003
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发表时间：
2009-01
影响因子：
4.7
通讯作者：
Peters JA
中科院分区：
文献类型：
--
作者：
Barnes NM;Hales TG;Lummis SC;Peters JA
5-羟色胺 3 型 (5-HT3) 受体是 Cys 环超家族的阳离子选择性离子通道。中枢和周围神经系统中 5-HT3 受体的激活引起神经元兴奋和神经递质释放。在此，我们回顾一下5-HT3受体的结构与功能之间的关系。 5-HT3A 和 5-HT3B 亚基是 5-HT3 受体的成熟组成部分，但额外的 HTR3C、HTR3D 和 HTR3E 基因扩大了该家族内分子多样性的潜力。对 5-HT3 受体亚基结构与离子选择性和单通道电导之间关系的研究发现了一个有助于离子渗透和选择性的新结构域（细胞内 MA 延伸）。受体胞外域的常规和非天然氨基酸诱变揭示了主环 (A-C) 和互补环 (D-F) 内的残基，这些残基对配体结合至关重要。需要进一步研究的领域是神经元内源性 5-HT3 受体的亚基组成及其在中枢神经系统内的区域表达。最后，我们描述了最近的研究，这些研究已经确定了许多影响 5-HT3 受体功能或表达的 HTR3A 和 HTR3B 基因多态性，并考虑了它们与（病理）生理学的相关性。
The 5-hydroxytryptamine type-3 (5-HT3) receptor is a cation-selective ion channel of the Cys-loop superfamily. 5-HT3 receptor activation in the central and peripheral nervous systems evokes neuronal excitation and neurotransmitter release. Here, we review the relationship between the structure and the function of the 5-HT3 receptor. 5-HT3A and 5-HT3B subunits are well established components of 5-HT3 receptors but additional HTR3C, HTR3D and HTR3E genes expand the potential for molecular diversity within the family. Studies upon the relationship between subunit structure and the ionic selectivity and single channel conductances of 5-HT3 receptors have identified a novel domain (the intracellular MA-stretch) that contributes to ion permeation and selectivity. Conventional and unnatural amino acid mutagenesis of the extracellular domain of the receptor has revealed residues, within the principle (A-C) and complementary (D-F) loops, which are crucial to ligand binding. An area requiring much further investigation is the subunit composition of 5-HT3 receptors that are endogenous to neurones, and their regional expression within the central nervous system. We conclude by describing recent studies that have identified numerous HTR3A and HTR3B gene polymorphisms that impact upon 5-HT3 receptor function, or expression, and consider their relevance to (patho)physiology.
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影响因子：
5.5
作者：
Brown, AM;Hope, AG;Peters, JA
通讯作者：
Peters, JA
影响因子：
4.8
作者：
Castillo, M;Mulet, J;Criado, M
通讯作者：
Criado, M
影响因子：
4.8
作者：
Cheng, Aixin;Bollan, Karen A.;Connolly, Christopher N.
通讯作者：
Connolly, Christopher N.
影响因子：
4.7
作者：
BUFTON, KE;STEWARD, LJ;BARNES, NM
通讯作者：
BARNES, NM
影响因子：
3.6
作者：
Brüss, M;Barann, M;Bönisch, H
通讯作者：
Bönisch, H