小鼠和大鼠松弛素受体作为富含亮氨酸重复序列的人G蛋白偶联受体7的新型直系同源物的鉴定与表征。

Identification and characterization of the mouse and rat relaxin receptors as the novel orthologues of human leucine-rich repeat-containing G-protein-coupled receptor 7.

Scott D J, Layfield S, Riesewijk A, Morita H, Tregear G W, Bathgate R A D

Howard Florey Institute, University of Melbourne, Parkville, Victoria, Australia.

Clin Exp Pharmacol Physiol. 2004 Nov;31(11):828-32. doi: 10.1111/j.1440-1681.2004.04075.x.

Abstract

Relaxin is an extracellular matrix (ECM)-remodelling hormone that is functionally important in reproductive tissues, brain, lung and heart. 2. Recently, the human relaxin receptor was identified as leucine-rich repeat-containing G-protein-coupled receptor 7 (LGR7). 3. Using human LGR7 as a template, we identified mouse and rat LGR7 orthologues in the Celera and National Centre for Biotechnology Information databases. 4. At the protein level, mouse and rat LGR7 share 85.2 and 85.7% identity with human LGR7, respectively. 5. Mouse LGR7 mRNA was detected in all tissues where relaxin binding is observed. 6. Mouse and rat LGR7 bound [33P]-relaxin with high affinity and, upon relaxin treatment, both receptors stimulated cAMP production in transfected HEK 293T cells. 7. These results indicate that mouse and rat LGR7 are the relaxin receptors in these species. 8. The actions of relaxin in rodents are well characterized, providing an established platform for research into the molecular pharmacology of the highly conserved relaxin receptor.

摘要

松弛素是一种细胞外基质（ECM）重塑激素，在生殖组织、大脑、肺和心脏中具有重要功能。2. 最近，人类松弛素受体被鉴定为富含亮氨酸重复序列的G蛋白偶联受体7（LGR7）。3. 以人类LGR7为模板，我们在Celera和美国国立生物技术信息中心数据库中鉴定出小鼠和大鼠的LGR7直系同源物。4. 在蛋白质水平上，小鼠和大鼠的LGR7与人类LGR7的同一性分别为85.2%和85.7%。5. 在所有观察到松弛素结合的组织中均检测到小鼠LGR7 mRNA。6. 小鼠和大鼠的LGR7以高亲和力结合[33P] - 松弛素，并且在松弛素处理后，两种受体均能刺激转染的HEK 293T细胞中cAMP的产生。7. 这些结果表明小鼠和大鼠的LGR7是这些物种中的松弛素受体。8. 松弛素在啮齿动物中的作用已得到充分表征，为研究高度保守的松弛素受体的分子药理学提供了一个既定平台。