A bioactive peptide from the transmembrane 5 intracellular loop 3 region of the human 5HT1a receptor

被引：10
|
作者：
Hayataka, K [1 ]
O'Connor, MF [1 ]
Kinzler, N [1 ]
Weber, JT [1 ]
Parker, KK [1 ]
机构：
[1] Univ Montana, Sch Pharm, Dept Pharmaceut Chem, Missoula, MT 59812 USA
来源：
BIOCHEMISTRY AND CELL BIOLOGY-BIOCHIMIE ET BIOLOGIE CELLULAIRE | 1998年 / 76卷 / 04期
关键词：
serotonin; 5HT1a receptor; G protein; cAMP; loop peptide;
D O I：
10.1139/bcb-76-4-657
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
15 amino acid peptide from the transmembrane 5 - intracellular loop 3 region of the human 5HT1a receptor produced concentration-dependent decreases in agonist binding. This result is consistent with a competitive interaction between peptide, receptor, and G protein at the receptor - G protein interface. Bombesin and a 13 amino acid peptide from the carboxyl terminus region of the receptor were inactive. Additionally, the peptide decreased forskolin-mediated cAMP elevation. Overall, these results suggest that amino acid residues from this region of the receptor are involved in receptor - G protein coupling and that G protein is activated by the receptor.
引用
收藏
页码：657 / 660
页数：4
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