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首页> 外文期刊>Life sciences >CHARACTERIZATION OF THE HUMAN OXYTOCIN RECEPTOR STABLY EXPRESSED IN 293 HUMAN EMBRYONIC KIDNEY CELLS
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CHARACTERIZATION OF THE HUMAN OXYTOCIN RECEPTOR STABLY EXPRESSED IN 293 HUMAN EMBRYONIC KIDNEY CELLS

机译：稳定表达于293种人胚肾细胞中的人催产素受体的特性

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The human oxytocin (OT) receptor was stably expressed in 293 embryonic kidney cells (293/OTR), characterized pharmacologically and compared to human uterine myometrial receptors. The cloned receptor is expressed at a reasonably high density (0.82 fmole/mu g protein) and exhibits high affinity for [H-3]OT (K-d=0.32 nM), similar to the value found in human myometrial tissue. The rank-order of potency for various antagonist and agonist ligands from several structural classes is also similar between the cloned and native receptor, as seen in a comparison of their inhibitory constants for [3H]OT binding. Agonist affinity at the cloned OT receptor is decreased by guanine nucleotide analogs, demonstrating functional G-protein-coupling. The OT receptor in 293 cells, like in human myometrium, is also coupled to the inositol phosphate pathway. In 293/OTR cells, OT stimulates inositol phosphate accumulation with an EC(50)=4.1 nM, an effect blocked by a potent and selective OT antagonist, L-366,948. Additionally, the cloned receptor in 293 cells desensitizes to high concentrations of OT, similar to the desensitization in myometrial tissue and also described for several other G-protein-coupled receptors. These results illustrate the utility of the 293 cell line for expressing human OT receptors in an environment quite comparable to the native myometrial tissue. [References: 17]
机译：人催产素（OT）受体在293胚胎肾细胞（293 / OTR）中稳定表达，具有药理学特性，并与人子宫肌层受体进行了比较。克隆的受体以相当高的密度（0.82 fmole /μg蛋白）表达，并且对[H-3] OT具有高亲和力（K-d = 0.32 nM），类似于在人类肌层组织中发现的值。从几种结构类别的各种拮抗剂和激动剂配体的效价等级在克隆的受体和天然受体之间也相似，从它们对[3H] OT结合的抑制常数的比较中可以看出。鸟嘌呤核苷酸类似物降低了对克隆的OT受体的激动剂亲和力，表明功能性G蛋白偶联。像人类子宫肌层一样，293细胞中的OT受体也与肌醇磷酸途径偶联。在293 / OTR细胞中，OT以EC（50）= 4.1 nM刺激肌醇磷酸积累，这种作用被有效的选择性OT拮抗剂L-366,948阻断。此外，在293细胞中克隆的受体对高浓度的OT脱敏，类似于子宫肌层组织中的脱敏，并且还针对其他几种G蛋白偶联受体进行了描述。这些结果说明了在与天然子宫肌层组织相当的环境中293细胞系用于表达人OT受体的效用。 [参考：17]

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