Delporte C, Poloczek P, Gossen D, Tastenoy M, Winand J, Christophe J
Department of Biochemistry and Nutrition, Medical School, Université Libre de Bruxelles, Belgium.
Eur J Pharmacol. 1991 May 25;207(1):81-8. doi: 10.1016/s0922-4106(05)80041-0.
We characterized in membranes from the human neuroblastoma cell line NB-OK-1, an ANP-R1 receptor (Mr 130 kDa) for the atrial natriuretic peptide (ANP). This receptor recognized biologically active forms of ANP with high affinity but showed no affinity for truncated ANP forms. It was functional in that binding correlated with guanylate cyclase activation (a 2-fold increase in Vmax) with the following rank order of potency: rat ANP-(99-126) greater than human ANP-(99-126) greater than human ANP-(102-126) greater than porcine BNP (brain natriuretic peptide). The enzyme required free Mn2+ in addition to the Mn-GTP substrate (Km of about 0.3 mM for both basal and ANP-stimulated activity). In the presence of dithiothreitol, the dose-response curve of guanylate cyclase activation was shifted rightward by a factor of 30. ANP-R1 receptors were upregulated through protein synthesis in cells exposed to 1 mM carbamylcholine or 1 mM dibutyryl cyclic AMP for 8-24 h (ANP was ineffective).
我们对人神经母细胞瘤细胞系NB - OK - 1的膜进行了表征，发现了一种用于心房利钠肽（ANP）的ANP - R1受体（分子量130 kDa）。该受体以高亲和力识别具有生物活性的ANP形式，但对截短的ANP形式无亲和力。它具有功能，因为结合与鸟苷酸环化酶激活相关（Vmax增加2倍），其效力顺序如下：大鼠ANP - (99 - 126) > 人ANP - (99 - 126) > 人ANP - (102 - 126) > 猪脑钠肽（BNP）。除了Mn - GTP底物外，该酶还需要游离的Mn2 +（基础活性和ANP刺激活性的Km约为0.3 mM）。在二硫苏糖醇存在下，鸟苷酸环化酶激活的剂量反应曲线向右移动了30倍。在暴露于1 mM氨甲酰胆碱或1 mM二丁酰环AMP 8 - 24小时的细胞中，通过蛋白质合成上调了ANP - R1受体（ANP无效）。
