人类甘丙肽受体GalR2的克隆与表达

Cloning and expression of the human galanin receptor GalR2.

作者信息

Bloomquist B T, Beauchamp M R, Zhelnin L, Brown S E, Gore-Willse A R, Gregor P, Cornfield L J

机构信息

Institute for Metabolic Disorders, Bayer Corporation, West Haven, Connecticut 06516, USA.

出版信息

Biochem Biophys Res Commun. 1998 Feb 13;243(2):474-9. doi: 10.1006/bbrc.1998.8133.

DOI:10.1006/bbrc.1998.8133

PMID:9480833

Abstract

Galanin is a peptide hormone which modulates a wide variety of physiological processes, including secretion, muscle contraction, cognitive function, the reproductive axis, and feeding. Two galanin receptor subtypes, GalR1 and GalR2, have been cloned; however, for GalR2 only the rat sequence has been reported in the literature. Our cloning of human GalR2 reveals its amino acid sequence to be 85% identical to rat GalR2 and 39% identical to human GalR1. Binding of [125I]galanin to the human GalR2 receptor transiently expressed in COS-7 cells was saturable (Kd = 0.24 nM +/- 0.06 nM) with a receptor density of 383 +/- 66 fmol/mg protein. Human galanin(1-30) bound with high affinity to the human GalR2 receptor, with a Ki value of 0.86 +/- 0.12 nM. With the identification of a second galanin receptor subtype, the specific functions of human galanin receptor subtypes can now begin to be addressed.

摘要

甘丙肽是一种肽类激素，可调节多种生理过程，包括分泌、肌肉收缩、认知功能、生殖轴和进食。已克隆出两种甘丙肽受体亚型，即GalR1和GalR2；然而，关于GalR2，文献中仅报道了大鼠的序列。我们克隆的人GalR2显示其氨基酸序列与大鼠GalR2的一致性为85%，与人类GalR1的一致性为39%。[125I]甘丙肽与在COS-7细胞中瞬时表达的人GalR2受体的结合是可饱和的（Kd = 0.24 nM ± 0.06 nM），受体密度为383 ± 66 fmol/mg蛋白质。人甘丙肽（1-30）与人GalR2受体具有高亲和力结合，Ki值为0.86 ± 0.12 nM。随着第二种甘丙肽受体亚型的鉴定，现在可以开始研究人甘丙肽受体亚型的具体功能了。