Perry H M, Chappel J C, Bellorin-Font E, Tamao J, Martin K J, Teitelbaum S L
J Biol Chem. 1984 May 10;259(9):5531-5.
In this article we demonstrate receptors for parathyroid hormone in circulating mononuclear leukocytes using the radioiodinated analogue (8,18 norleucine, 34 tyrosine) bPTH 1-34 (bovine parathyroid hormone 1-34). Specific binding, which is reversible and saturable, equilibrates within 5 min at 0-4 degrees C with a calculated KD of 8.9 X 10(-11) M. This binding has a pH maximum of 7.0, is magnesium-dependent, and is inversely related to medium calcium concentration. Such binding is completely inhibited by simultaneous addition of 4 ng/ml of bovine parathyroid hormone 1-34, 5 ng/ml of bovine parathyroid hormone 1-84, or 5 ng/ml (8,18 norleucine, 34 Tyr) of 3-34 bPTH, but is unaffected by a biologically inactive parathyroid hormone fragment or other unrelated peptide hormones. Cyclic AMP accumulation increases 3-fold after 5 min exposure of mononuclear leukocytes to bPTH 1-34 in concentrations as low as 1 X 10(-9) M. Lymphocytes appear to be the circulating cells which interact with PTH as indicated by the observations that: 1) lymphocyte-enriched preparations bind three times as much radioligand/cell as do mixed mononuclear leukocytes, 2) monocytes, platelets, granulocytes, and erythrocytes do not bind PTH, and 3) monocytes, but not lymphocytes, degrade the hormone.
在本文中,我们使用放射性碘化类似物(8,18-去甲亮氨酸,34-酪氨酸)bPTH 1-34(牛甲状旁腺激素1-34)证明了循环单核白细胞中存在甲状旁腺激素受体。特异性结合是可逆且可饱和的,在0-4℃下5分钟内达到平衡,计算出的解离常数KD为8.9×10⁻¹¹M。这种结合在pH值为7.0时达到最大值,依赖于镁,并且与培养基钙浓度呈负相关。同时加入4 ng/ml的牛甲状旁腺激素1-34、5 ng/ml的牛甲状旁腺激素1-84或5 ng/ml(8,18-去甲亮氨酸,34-酪氨酸)的3-34 bPTH可完全抑制这种结合,但不受生物活性无的甲状旁腺激素片段或其他无关肽激素的影响。单核白细胞暴露于低至1×10⁻⁹M浓度的bPTH 1-34 5分钟后,环磷酸腺苷积累增加3倍。淋巴细胞似乎是与甲状旁腺激素相互作用的循环细胞,这一点可通过以下观察结果表明:1)富含淋巴细胞的制剂比混合单核白细胞结合的放射性配体/细胞多三倍;2)单核细胞、血小板、粒细胞和红细胞不结合甲状旁腺激素;3)单核细胞而非淋巴细胞会降解该激素。