Activation of orphan receptors by the hormone relaxin
Activation of orphan receptors by the hormone relaxin
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DOI：
10.1126/science.1065654
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发表时间：
2002-01-25
期刊：
影响因子：
56.9
通讯作者：
Hsueh, AJW
中科院分区：
文献类型：
--
作者：
Hsu, SY;Nakabayashi, K;Hsueh, AJW
松弛素是一种对怀孕期间生殖和其他组织的生长和重塑非常重要的激素。尽管松弛蛋白的结合部位广泛分布，但其受体的性质一直难以捉摸。在这里，我们证明了两个孤儿异三聚体鸟嘌呤核苷酸结合蛋白(G蛋白)偶联受体，LGR7和LGR8，能够通过不同于结构上相关的胰岛素和胰岛素样生长因子家族配体的依赖腺苷3‘，5’-磷酸(CAMP)的途径来介导松弛素的作用。用LGR7的可溶性配体结合区治疗产前小鼠会导致分娩延迟。这两种松弛素受体的广泛和不同的分布意味着它们在生殖、脑、肾、心血管和其他功能中的作用。
Relaxin is a hormone important for the growth and remodeling of reproductive and other tissues during pregnancy. Although binding sites for relaxin are widely distributed, the nature of its receptor has been elusive. Here, we demonstrate that two orphan heterotrimeric guanine nucleotide binding protein (G protein)-coupled receptors, LGR7 and LGR8, are capable of mediating the action of relaxin through an adenosine 3',5'-monophosphate (cAMP)-dependent pathway distinct from that of the structurally related insulin and insulin-like growth factor family ligand. Treatment of antepartum mice with the soluble ligand-binding region of LGR7 caused parturition delay. The wide and divergent distribution of the two relaxin receptors implicates their roles in reproductive, brain, renal, cardiovascular, and other functions.