CHARACTERIZATION OF VASOACTIVE-INTESTINAL-PEPTIDE RECEPTORS IN HUMAN LIVER

被引：18

作者：

RODRIGUEZHENCHE, N ^{[1
]}

RODRIGUEZPENA, MS ^{[1
]}

GUIJARRO, LG ^{[1
]}

PRIETO, JC ^{[1
]}

机构：

[1] UNIV ALCALA DE HENARES, DEPT BIOQUIM & BIOL MOLEC, UNIDAD NEUROENDOCRINOL MOLEC, E-28871 ALCALA DE HENARES, SPAIN

来源：

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH | 1994年 / 1221卷 / 02期

关键词：

VASOACTIVE INTESTINAL PEPTIDE (VIP); VIP RECEPTOR; G PROTEIN; ADENYLYL CYCLASE; HUMAN LIVER;

D O I：

10.1016/0167-4889(94)90013-2

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：

The stoichiometric, pharmacological and molecular properties of vasoactive intestinal peptide (VIP) receptors have been analyzed in human liver membranes and compared in parallel with those in rat liver membranes. The binding of [I-125]VIP was rapid, saturable and specific. The stoichometric data indicated the presence of two classes of binding sites in both human and rat liver membranes with K-d values of 0.22 (human) and 0.20 (rat) nM for the high-affinity site, and 27.3 (human) and 3.6 (rat) nM for the low-affinity site. Tracer binding was displaced by structurally related peptides with an order of potency: VIP = PACAP-27 > helodermin > secretin in human liver, and VIP = PACAP-27 = helodermin > secretin in rat liver. GTP inhibited [I-125]VIP binding in a dose-dependent manner suggesting the involvement of a G protein in the signal transduction pathway. Cross-linking experiments revealed an apparent molecular mass for the VIP-receptor complex that was 67500 +/- 2700 and 50500 +/- 900 in human and rat preparations, respectively. VIP receptors were functional, since VIP stimulated adenylyl cyclase activity in a dose dependent manner with similar efficacy but different potency in human (ED(50) = 1.2 nM) and rat (ED(50) = 5.8 nM) liver membranes.

引用

页码：193 / 198

页数：6

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