Howard A D, Feighner S D, Cully D F, Arena J P, Liberator P A, Rosenblum C I, Hamelin M, Hreniuk D L, Palyha O C, Anderson J, Paress P S, Diaz C, Chou M, Liu K K, McKee K K, Pong S S, Chaung L Y, Elbrecht A, Dashkevicz M, Heavens R, Rigby M, Sirinathsinghji D J, Dean D C, Melillo D G, Patchett A A, Nargund R, Griffin P R, DeMartino J A, Gupta S K, Schaeffer J M, Smith R G, Van der Ploeg L H
Merck Research Laboratories, Rahway, NJ 07065, USA.
Science. 1996 Aug 16;273(5277):974-7. doi: 10.1126/science.273.5277.974.
Small synthetic molecules termed growth hormone secretagogues (GHSs) act on the pituitary gland and the hypothalamus to stimulate and amplify pulsatile growth hormone (GH) release. A heterotrimeric GTP-binding protein (G protein)-coupled receptor (GPC-R) of the pituitary and arcuate ventro-medial and infundibular hypothalamus of swine and humans was cloned and was shown to be the target of the GHSs. On the basis of its pharmacological and molecular characterization, this GPC-R defines a neuroendocrine pathway for the control of pulsatile GH release and supports the notion that the GHSs mimic an undiscovered hormone.
一种被称为生长激素促分泌素(GHSs)的小型合成分子作用于垂体和下丘脑,以刺激并放大脉冲式生长激素(GH)的释放。猪和人类垂体以及下丘脑弓状腹内侧和漏斗部的一种异源三聚体GTP结合蛋白(G蛋白)偶联受体(GPC-R)被克隆出来,并被证明是GHSs的作用靶点。基于其药理学和分子特征,这种GPC-R定义了一条用于控制脉冲式GH释放的神经内分泌途径,并支持了GHSs模拟一种未被发现的激素这一观点。