Novel insights into histamine H-2 receptor biology

被引:90
作者
DelValle, J [1 ]
Gantz, I [1 ]
机构
[1] UNIV MICHIGAN, MED CTR, DEPT INTERNAL MED, ANN ARBOR, MI 48109 USA
来源
AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY | 1997年 / 273卷 / 05期
关键词
biogenic amine; G protein; signal transduction;
D O I
10.1152/ajpgi.1997.273.5.G987
中图分类号
R57 [消化系及腹部疾病];
学科分类号
摘要
Histamine exerts multiple biological actions through one of three receptor subtypes (H-1, H-2, and H-3). This review focuses on new developments regarding the structure and function of the H-2 receptor. In addition to the important role this receptor plays in stimulating gastric acid secretion, recent studies have demonstrated that it is also involved in regulating gastrointestinal motility and intestinal secretion. The potential role of the H-2 receptor in regulating cell growth and differentiation has also been added to the list of actions this biogenic amine may exert in both normal and transformed tissues. Molecular cloning of the gene indicates that it has the structural characteristics of a heptahelical G protein-linked receptor. Site-directed mutagenesis studies of this receptor reveal the presence of key amino acids within the third and fifth transmembrane domains that are critical for ligand recognition. Molecular approaches have also shed light on the structural components of the H-2 receptor important in regulating desensitization and internalization. Although the H-2 receptor was classically thought to couple to the adenylate cyclase pathway, recent work with the cloned receptor indicates that it can also activate the phosphoinositide signaling cascade through an independent G protein-dependent mechanism. The novel observation that histamine may stimulate c-fos gene expression lends further support to the possible role of this receptor in regulating cell growth and differentiation.
引用
收藏
页码:G987 / G996
页数:10
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