The long-acting vasoactive intestinal polypeptide agonist RO 25-1553 is highly selective of the VIP2 receptor subclass

被引：137

作者：

Gourlet, P ^{[1
]}

Vertongen, P ^{[1
]}

Vandermeers, A ^{[1
]}

VandermeersPiret, MC ^{[1
]}

Rathe, J ^{[1
]}

DeNeef, P ^{[1
]}

Waelbroeck, M ^{[1
]}

Robberecht, P ^{[1
]}

机构：

[1] FREE UNIV BRUSSELS, SCH MED, DEPT BIOCHEM & NUTR, B-1070 BRUSSELS, BELGIUM

来源：

PEPTIDES | 1997年 / 18卷 / 03期

关键词：

RO; 25-1553; selectivity; VIP2 receptor agonist; ADENYLATE-CYCLASE; FUNCTIONAL-CHARACTERIZATION; SUP-T1; LYMPHOBLASTS; PEPTIDE AGONIST; IN-VITRO; PACAP; HELODERMIN; CLONING; CELLS; EXPRESSION;

D O I：

10.1016/S0196-9781(96)00322-1

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：

RO 25-1553 is a synthetic VIP analogue that induced a longlasting relaxation of tracheal and bronchial smooth muscles as well as a reduction of edema and eosinophilic mobilization during pulmonary anaphylaxis. In the present study, we tested in vitro the capacity of RO 25-1553 to occupy the different VIP/PACAP receptor subclasses and to stimulate adenylate cyclase activity. The cellular models tested expressed one single receptor subtype: Chinese hamster ovary (CHO) cells transfected with the rat recombinant PACAP I, rat VIP1, and human VIP2 receptors; SUP T1 cells expressing the human VIP2 and HCT 15 and LoVo cells expressing the human VIP1 receptor. RO 25-1553 was threefold more potent than VIP on the human VIP2 receptor, 100- and 600-fold less potent than VIP on the rat and human VLP1 receptors, respectively, and 10-fold less potent than VIP and 3000-fold less potent than PACAP on the PACAP I receptor. RO 25-1553 was a full agonist on the VIP2, the PACAP I, and the rat recombinant VIP1 receptor but a partial agonist only on the human VIP1 receptor. Thus, RO 25-1553 is a highly selective agonist ligand for the VIP2 receptor subclass. (C) 1997 Elsevier Science Inc.

引用

页码：403 / 408

页数：6

共 30 条

[1] PROPERTIES OF VASOACTIVE-INTESTINAL-PEPTIDE RECEPTORS AND BETA-ADRENOCEPTORS IN THE MURINE RADIATION LEUKEMIA-VIRUS-INDUCED LYMPHOMA CELL-LINE BL/VL3 [J].

ABELLO, J ;

DAMIEN, C ;

DENEEF, P ;

TASTENOY, M ;

HOOGHE, R ;

ROBBERECHT, P ;

CHRISTOPHE, J .

EUROPEAN JOURNAL OF BIOCHEMISTRY, 1989, 183 (02) :263-267

[2]

BOLIN DR, 1992, BIOMED RES-TOKYO, V13, P25

[3]

BOLIN DR, 1989, PEPTIDES CHEM BIOL, P208

[4] PRESENCE OF HIGHLY SELECTIVE RECEPTORS FOR PACAP (PITUITARY ADENYLATE-CYCLASE ACTIVATING PEPTIDE) IN MEMBRANES FROM THE RAT PANCREATIC ACINAR CELL-LINE AR-4-2J [J].

BUSCAIL, L ;

GOURLET, P ;

CAUVIN, A ;

DENEEF, P ;

GOSSEN, D ;

ARIMURA, A ;

MIYATA, A ;

COY, DH ;

ROBBERECHT, P ;

CHRISTOPHE, J .

FEBS LETTERS, 1990, 262 (01) :77-81

[5] TYPE-I RECEPTORS FOR PACAP (A NEUROPEPTIDE EVEN MORE IMPORTANT THAN VIP) [J].

CHRISTOPHE, J .

BIOCHIMICA ET BIOPHYSICA ACTA, 1993, 1154 (02) :183-199

[6] PROPERTIES OF THE VIP-PACAP TYPE-II RECEPTOR STABLY EXPRESSED IN CHO CELLS [J].

CICCARELLI, E ;

VILARDAGA, JP ;

DENEEF, P ;

DIPAOLO, E ;

WAELBROECK, M ;

BOLLEN, A ;

ROBBERECHT, P .

REGULATORY PEPTIDES, 1994, 54 (2-3) :397-407

[7] PHARMACOLOGICAL PROPERTIES OF 2 RECOMBINANT SPLICE VARIANTS OF THE PACAP TYPE-I RECEPTOR, TRANSFECTED AND STABLY EXPRESSED IN CHO CELLS [J].

CICCARELLI, E ;

SVOBODA, M ;

DENEEF, P ;

DIPAOLO, E ;

BOLLEN, A ;

DUBEAUX, C ;

VILARDAGA, JP ;

WAELBROECK, M ;

ROBBERECHT, P .

EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION, 1995, 288 (03) :259-267

[8] HUMAN INTESTINAL VIP RECEPTOR - CLONING AND FUNCTIONAL EXPRESSION OF 2 CDNA-ENCODING PROTEINS WITH DIFFERENT N-TERMINAL DOMAINS [J].

COUVINEAU, A ;

ROUYERFESSARD, C ;

DARMOUL, D ;

MAORET, JJ ;

CARRERO, I ;

OGIERDENIS, E ;

LABURTHE, M .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1994, 200 (02) :769-776

[9]

COUVINEAU A, 1994, VASOACTIVE INTESTINA, P129

[10] ADENYLATE-CYCLASE ACTIVATION BY VIP-HELODERMIN AND HISTAMINE H-2 RECEPTORS IN HUMAN THP-1 MONOCYTES MACROPHAGES - A POSSIBLE ROLE IN THE REGULATION OF SUPEROXIDE ANIONS PRODUCTION [J].

GESPACH, C ;

CHEDEVILLE, A ;

HURBAINKOSMATH, I ;

HOUSSET, B ;

DERENNE, JP ;

ABITA, JP .

REGULATORY PEPTIDES, 1989, 26 (02) :158-158

← 1 2 3 →