SUPERACTIVE LIPOPHILIC PEPTIDES DISCRIMINATE MULTIPLE VASOACTIVE-INTESTINAL-PEPTIDE RECEPTORS

被引：0
|
作者：
GOZES, I
LILLING, G
GLAZER, R
TICHER, A
ASHKENAZI, IE
DAVIDSON, A
RUBINRAUT, S
FRIDKIN, M
BRENNEMAN, DE
机构：
[1] TEL AVIV UNIV,SACKLER SCH MED,DEPT HUMAN GENET,IL-69978 TEL AVIV,ISRAEL
[2] TEL AVIV UNIV,SACKLER SCH MED,DEPT HUMAN GENET,IL-69978 TEL AVIV,ISRAEL
[3] WEIZMANN INST SCI,DEPT ORGAN CHEM,IL-76100 REHOVOT,ISRAEL
[4] NICHHD,DEV NEUROBIOL LAB,DEV & MOLEC PHARMACOL SECT,BETHESDA,MD 20892
来源：
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS | 1995年 / 273卷 / 01期
关键词：
D O I：
暂无
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
To distinguish vasoactive intestinal peptide (VIP) receptors in the brain-mediating neurotransmission and neurotrophism, potent VIP analogues were designed. Using a single amino acid substitution and the addition of a fatty acyl moiety, an analogue was devised that exhibited both a 100-fold greater potency than VIP and specificity for a VIP receptor associated with neuronal survival. This VIP agonist increased neuronal survival via a cAMP-independent mechanism. Identical chemical modification of a prototype VIP antagonist (Met-Hybrid, Neurotensin(6-11)-VIP7-28) also resulted in a 100-fold greater potency in blocking VIP-mediated increases in neuronal survival. Blockade of circadian activity rhythms was limited to VIP antagonists that could inhibit VIP-mediated increases in cAMP. These lipophilic peptides provide novel tools in receptor discrimination and drug design.
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收藏
页码：161 / 167
页数：7
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