Characterization of zeta (zeta): a new opioid receptor involved in growth.
Characterization of zeta (zeta): a new opioid receptor involved in growth.
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zeta（zeta）的表征：一种参与生长的新阿片受体。
DOI：
10.1016/0006-8993(89)91192-x
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发表时间：
1989
期刊：
影响因子：
2.9
通讯作者：
McLaughlin,PJ
中科院分区：
文献类型：
--
作者：
Zagon,IS;Goodman,SR;McLaughlin,PJ
内源性阿片样物质系统（即，阿片样物质和阿片样物质受体）已知在神经癌中起作用。使用[3 H]-[Met 5]脑啡肽，一种参与生长的有效配体，在移植到A/Jax小鼠的S20 Y神经母细胞瘤匀浆中检测到特异性和可饱和结合;数据符合单个结合位点。Scatchard分析得到a Kd为0.49 nM，结合容量为5.32 fmol/mg蛋白。结合依赖于蛋白质浓度、时间、温度和pH，并且对Na+和鸟嘌呤核苷酸敏感。最佳的结合需要蛋白酶抑制剂，和预处理的肿瘤匀浆与胰蛋白酶显着降低[3 H]-[Met 5]脑啡肽结合，这表明结合位点是蛋白质的性质。置换实验表明，[Met 5]脑啡肽是[3 H]-[Met 5]脑啡肽的最有效的置换剂;对μ、δ、κ、δ和σ具有选择性的其他配体没有高度竞争性。考虑到[Met 5]脑啡肽作为正常和异常生长的有效调节剂的功能意义，并且[Met 5]脑啡肽识别的受体与任何先前描述的受体都不相似，本研究已经证明了与细胞和组织增殖相关的称为zeta（zeta）（来自希腊语“Zoe”，生命）的新阿片受体的存在。
Endogenous opioid systems (i.e., opioids and opioid receptors) are known to play a role in neural cancer. Using [3H]-[Met5]enkephalin, a potent ligand involved in growth, specific and saturable binding was detected in homogenates of S20Y neuroblastoma transplanted into A/Jax mice; the data fit a single binding site. Scatchard analysis yielded aKdof 0.49 nM and a binding capacity of 5.32 fmol/mg protein. Binding was dependent on protein concentration, time, temperature, and pH, and was sensitive to Na+and guanine nucleotides. Optimal binding required protease inhibitors, and pretreatment of the tumor homogenates with trypsin markedly reduced [3H]-[Met5]enkephalin binding, suggesting that the binding site was proteinaceous in character. Displacement experiments indicated that [Met5]enkephalin was the most potent displacer of [3H]-[Met5]enkephalin; other ligands selective for μ, δ, κ, ɛ, and σ were not highly competitive. Given the functional significance of [Met5]enkephalin as a potent regulator of normal and abnormal growth, and that the receptor recognized by [Met5]enkephalin does not resemble any previously described, the present study has demonstrated the presence of a new opioid receptor termed zeta (ζ) (from the Greek ‘Zoe’, life) related to the proliferation of cells and tissues.