肾上腺素能受体的结构、功能及调节
Structure, function, and regulation of adrenergic receptors.
作者信息
Strosberg A D
机构信息
Laboratoire d'Immuno-Pharmacologie Moléculaire, Institut Cochin de Génétique Moléculaire, Paris, France.
出版信息
Protein Sci. 1993 Aug;2(8):1198-209. doi: 10.1002/pro.5560020802.
Abstract
Adrenergic receptors for adrenaline and noradrenaline belong to the large multigenic family of receptors coupled to GTP-binding proteins. Three pharmacologic types have been identified: alpha 1-, alpha 2-, and beta-adrenergic receptors. Each of these has three subtypes, characterized by both structural and functional differences. The alpha 2 and beta receptors are coupled negatively and positively, respectively, to adenylyl cyclase via Gi or Gs regulatory proteins, and the alpha 1 receptors modulate phospholipase C via the Go protein. Subtype expression is regulated at the level of the gene, the mRNA, and the protein through various transcriptional and postsynthetic mechanisms. Adrenergic receptors constitute, after rhodopsin, one of the best studied models for the other receptors coupled to G proteins that are likely to display similar structural and functional properties.
摘要
肾上腺素和去甲肾上腺素的肾上腺素能受体属于与GTP结合蛋白偶联的大型多基因受体家族。已鉴定出三种药理学类型：α1-、α2-和β-肾上腺素能受体。其中每一种都有三个亚型，其特征在于结构和功能上的差异。α2和β受体分别通过Gi或Gs调节蛋白与腺苷酸环化酶负性和正性偶联，而α1受体通过Go蛋白调节磷脂酶C。亚型表达通过各种转录和合成后机制在基因、mRNA和蛋白质水平上受到调控。肾上腺素能受体是继视紫红质之后，对其他与G蛋白偶联的受体进行研究的最佳模型之一，这些受体可能具有相似的结构和功能特性。
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本文引用的文献
1
2
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Mol Pharmacol. 1993 Apr;43(4):548-55.
3
Altered phosphorylation and desensitization patterns of a human beta 2-adrenergic receptor lacking the palmitoylated Cys341.缺乏棕榈酰化半胱氨酸341的人β2-肾上腺素能受体的磷酸化和脱敏模式改变。
EMBO J. 1993 Jan;12(1):349-56. doi: 10.1002/j.1460-2075.1993.tb05663.x.
4
Tissue distribution of beta 3-adrenergic receptor mRNA in man.人β3 - 肾上腺素能受体mRNA的组织分布
J Clin Invest. 1993 Jan;91(1):344-9. doi: 10.1172/JCI116191.
5
A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model.β2肾上腺素能受体的突变诱导激活状态。扩展三元复合物模型。
J Biol Chem. 1993 Mar 5;268(7):4625-36.
6
Differentiation of receptor systems activated by sympathomimetic amines.拟交感胺激活的受体系统的分化
Nature. 1967 May 6;214(5088):597-8. doi: 10.1038/214597a0.
7
Purification and characterization of the beta-adrenergic receptor kinase.β-肾上腺素能受体激酶的纯化与特性分析
J Biol Chem. 1987 Jul 5;262(19):9026-32.
8
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Cell. 1987 Jun 19;49(6):855-63. doi: 10.1016/0092-8674(87)90623-4.
9
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