CLONING, SEQUENCING, AND EXPRESSION OF HUMAN GONADOTROPIN-RELEASING-HORMONE (GNRH) RECEPTOR
CLONING, SEQUENCING, AND EXPRESSION OF HUMAN GONADOTROPIN-RELEASING-HORMONE (GNRH) RECEPTOR
复制标题
DOI：
10.1016/0006-291x(92)91556-6
复制
发表时间：
1992-11-30
影响因子：
3.1
通讯作者：
NEILL, JD
中科院分区：
文献类型：
--
作者：
KAKAR, SS;MUSGROVE, LC;NEILL, JD
促性腺激素释放激素是一种下丘脑十肽，刺激促性腺激素从垂体前叶释放。在治疗上，人垂体GnRH受体是用于抑制前列腺癌的激动剂的靶标。在这里，我们报告的cDNA代表这种受体的分离。它编码一种跨膜拓扑结构与其他G蛋白偶联的7跨膜受体相似的蛋白质。克隆受体的结合研究表明，高亲和力和药理学性质与天然人垂体GnRH受体相似。北方杂交和逆转录酶/PCR分析表明，其mRNA在垂体、卵巢、睾丸、乳腺和前列腺中表达，而在肝脏和脾脏中不表达。人GnRH受体cDNA的可用性应允许设计用于治疗应用的改进的类似物。
Gonadotropin releasing hormone is a hypothalamic decapeptide that stimulates the release of gonadotropic hormones from the anterior pituitary gland. Therapeutically, the human pituitary GnRH receptor is the target of agonists used in the suppression of prostate cancer. Here we report the isolation of a cDNA representing this receptor. It encodes a protein with a transmembrane topology similar with that of other G protein-coupled, 7-transmembrane receptors. Binding studies of the cloned receptor demonstrate high affinity and pharmacological properties similar with the native human pituitary GnRH receptor. Northern blot and reverse transcriptase/PCR analysis revealed that its mRNA is expressed in pituitary, ovary, testis, breast, and prostate but not in liver and spleen. Availability of a human GnRH receptor cDNA should permit the design of improved analogs for therapeutic applications.