Alpha 1-adrenergic receptor subtypes.
Alpha 1-adrenergic receptor subtypes.
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α1-肾上腺素能受体亚型。
DOI：
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发表时间：
1994
影响因子：
12.5
通讯作者：
T. Esbenshade
中科院分区：
文献类型：
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作者：
K. Minneman;T. Esbenshade
研究人员尚未就α 1-肾上腺素能受体（AR）亚型的数量和信号机制达成共识。两种天然亚型（α 1A和α 1B）可以区分，三种亚型（α 1B，α 1C和α 1D）已被克隆。其中一种克隆亚型（alpha 1D）最初被认为编码了基因组定义的alpha 1A亚型。然而，最近的数据表明，许多研究人员现在同意，α 1A亚型可能还没有被克隆。克隆受体和天然亚型之间的关系必须得到理解，并获得任何额外的cDNA克隆，然后才能清楚地定义α 1-AR亚型的药物特异性和第二信使途径。关于这些亚型的细胞和组织分布、它们的发育概况或它们的功能重要性，目前还知之甚少。分子克隆的互补DNA序列的其余亚型将有助于澄清这些亚型的数量和性质。鉴定可以选择性靶向特定亚型的药物是一个重要的目标，这可能导致许多疾病状态（包括良性前列腺增生）的治疗进展。新认识到的肾上腺素能受体的复杂性给我们带来了重要的挑战和新的治疗靶点。这一领域对医学治疗的潜在影响仍有待明确界定。
Investigators have not yet reached a consensus on the number and signaling mechanisms of alpha 1-adrenergic receptor (AR) subtypes. Two native subtypes (alpha 1A and alpha 1B) can be distinguished pharmacologically, and three subtypes (alpha 1B, alpha 1C, and alpha 1D) have been cloned. One of the cloned subtypes (alpha 1D) was originally thought to encode the pharmacologically defined alpha 1A subtype. However, recent data suggest otherwise, and many investigators now agree that the alpha 1A subtype has probably not yet been cloned. The relationship between the cloned receptors and the native subtypes must be understood, and any additional cDNA clones obtained, before the drug specificities and second messenger pathways of alpha 1-AR subtypes can be clearly defined. Little is yet known about the cellular and tissue distribution of these subtypes, their developmental profiles, or their functional importance. Molecular cloning of complementary DNA sequences for the remaining subtypes will help to clarify the number and properties of these subtypes. Identification of drugs that can selectively target particular subtypes is an important goal that may result in therapeutic advances in numerous disease states, including benign prostatic hyperplasia. The newly recognized complexity of the adrenergic receptors presents us with both important challenges and new therapeutic targets. The potential impact of this field on medical therapeutics remains to be clearly defined.