Regan J W, Kobilka T S, Yang-Feng T L, Caron M G, Lefkowitz R J, Kobilka B K
Howard Hughes Medical Institute, Duke University Medical Center, Department of Medicine, Durham, NC 27710.
Proc Natl Acad Sci U S A. 1988 Sep;85(17):6301-5. doi: 10.1073/pnas.85.17.6301.
An alpha 2-adrenergic receptor subtype has been cloned from a human kidney cDNA library using the gene for the human platelet alpha 2-adrenergic receptor as a probe. The deduced amino acid sequence resembles the human platelet alpha 2-adrenergic receptor and is consistent with the structure of other members of the family of guanine nucleotide-binding protein-coupled receptors. The cDNA was expressed in a mammalian cell line (COS-7), and the alpha 2-adrenergic ligand [3H]rauwolscine was bound. Competition curve analysis with a variety of adrenergic ligands suggests that this cDNA clone represents the alpha 2B-adrenergic receptor. The gene for this receptor is on human chromosome 4, whereas the gene for the human platelet alpha 2-adrenergic receptor (alpha 2A) lies on chromosome 10. This ability to express the receptor in mammalian cells, free of other adrenergic receptor subtypes, should help in developing more selective alpha-adrenergic ligands.
利用人血小板α2 - 肾上腺素能受体基因作为探针,从人肾cDNA文库中克隆出一种α2 - 肾上腺素能受体亚型。推导的氨基酸序列与人血小板α2 - 肾上腺素能受体相似,并且与鸟嘌呤核苷酸结合蛋白偶联受体家族其他成员的结构一致。该cDNA在哺乳动物细胞系(COS - 7)中表达,并结合了α2 - 肾上腺素能配体[3H]萝芙辛。用多种肾上腺素能配体进行的竞争曲线分析表明,该cDNA克隆代表α2B - 肾上腺素能受体。该受体的基因位于人类4号染色体上,而人血小板α2 - 肾上腺素能受体(α2A)的基因位于10号染色体上。这种在不含其他肾上腺素能受体亚型的哺乳动物细胞中表达该受体的能力,应有助于开发更具选择性的α - 肾上腺素能配体。