人类V3垂体加压素受体的克隆与特性分析
Cloning and characterization of the human V3 pituitary vasopressin receptor.
作者信息
de Keyzer Y, Auzan C, Lenne F, Beldjord C, Thibonnier M, Bertagna X, Clauser E
机构信息
INSERM CJF92-08, Institut Cochin de Génétique Moléculaire, University René Descartes, Paris, France.
出版信息
FEBS Lett. 1994 Dec 19;356(2-3):215-20. doi: 10.1016/0014-5793(94)01268-7.
Arginine-vasopressin (AVP) plays a determinant role in the normal ACTH response to stress in mammals. We cloned a human cDNA coding a 424 amino acid G-protein coupled receptor structurally related to the vasopressin/oxytocin receptor family. When expressed in COS cells, this receptor binds AVP with a high affinity (Kd = 0.55 +/- 0.13 nM) and is functionally coupled to phospholipase C. Competition studies with peptidic or non peptidic AVP analogues reveal that it is pharmacologically distinct from V1a and V2 AVP receptors and therefore it is designated V3. RT-PCR analysis shows that the human V3 receptor is expressed in normal pituitary and also in kidney, but is undetectable in liver, myometrium and adrenal gland. Northern blot analysis reveals a approximately 4.8 kb messenger in human corticotropic pituitary adenomas.
精氨酸加压素（AVP）在哺乳动物对应激的正常促肾上腺皮质激素（ACTH）反应中起决定性作用。我们克隆了一个人类cDNA，其编码一种与加压素/催产素受体家族结构相关的含424个氨基酸的G蛋白偶联受体。当在COS细胞中表达时，该受体以高亲和力（Kd = 0.55 +/- 0.13 nM）结合AVP，并在功能上与磷脂酶C偶联。用肽类或非肽类AVP类似物进行的竞争研究表明，它在药理学上与V1a和V2 AVP受体不同，因此被命名为V3。逆转录-聚合酶链反应（RT-PCR）分析显示，人类V3受体在正常垂体以及肾脏中表达，但在肝脏、子宫肌层和肾上腺中未检测到。Northern印迹分析显示，在人类促肾上腺皮质激素垂体腺瘤中有一个约4.8 kb的信使核糖核酸。
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